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US EPA CSS-HERA
Board of
Scientific
Counselors
Chemical Safety
Subcommittee
Meeting

US EPA CSS-HERA BOSC Meeting - February 2-5, 2021

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The work presented within represents US EPA Office of Research and Development research
activities. Material includes both peer reviewed, published results and work-in-progress
research. Please do not cite or quote slides.


-------
Table of Contents

Approaches and Models for Species Extrapolation (Carlie LaLone)	3

Novel in vitro Methods for Ecological Species: Evaluating Cross-species Differences in Nuclear Receptor-
Ligand Interactions (Brett Blackwell)	30

High Throughput Transcriptomics: A Multi-Species Approach (Kevin Flynn)	50

The work presented within represents US EPA Office of Research and Development research activities. Material
includes both peer reviewed, published results and work-in-progress research. Please do not cite or quote slides.


-------
The views expressed in this poster are those of the authors and do not necessarily reflect the views or policies of the U.S. EPA.

&EPA

United States
Environmental Protection
Agency

Approaches and Models for Species
Extrapolation

Carlie A. LaLone, Ph.D.
Research Bioinformaticist

Office of Research and Development

Center for Computational Toxicology and Exposure, Great Lakes Toxicology and Ecology Division

February 2nd, 2021

Cross Species Extrapolation

TOXICOKINETICS

Absorption

TOXICODYNAMICS

Elimination

Distribution

Metabolism

Bioinformatics


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A EPA

United States
Environmental Protection
Agency

Partners in Regulatory Decision-Making

• Capitalize on available data

Clean Air Act

Clean Water Act
Resource Recovery Act

Endangered Species Act
Food Quality Protection Act

Endocrine Disruptor Screening Program
Federal Insecticide, Fungicide, and Rodenticide Act
Frank R. Lautenberg Chemical Safety for the 21st Century Act
Comprehensive Environmental Response, Compensation, and Liability Act
Guidelines for Deriving Numerical National Water Quality Criteria for the Protection of Aquatic Organisms and Their Uses

Confidence in decisions, with limited data available, limited resources for testing, strong backing to reduce animal


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A EPA

United States
Environmental Protection
Agency

Stakeholder Identified Challenges

•	Limited or no toxicological data for the animal or plant species of
interest - reliance on surrogate (model organisms)

•	Impractical to generate new data for all species

•	Testing resources are limited

•	EPA directive aligns with international interest to reduce animal use

•	Ever-increasing demand to evaluate more chemicals in a timely and sometimes
expedited manner

•	Sensitivity of species must be estimated based on scientifically-sound
methods of cross-species extrapolation

•	Immense diversity of species in the wild

•	Important challenge for species listed under the Endangered Species Act

3


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AEPA

United States
Environmental Protection
Agency

Chemical Safety Evaluation

• Protect human health and the environment

• Ensure that chemicals in the marketplace are reviewed for safety

• Challenging mission:

•	Tens of thousand of chemicals are currently in use and hundreds are
introduced annually

•	Many have not been thoroughly evaluated for potential risk to human health
and the environment

• Chemicals tested across species: Even more sparse


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6


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a rpA

Strategic Approach to Species Extrapolation

United States
Environmental Protection
Agency

Computational:

Bioinformatics (Session 2 Demo)
Systematic review

Case Examples:
PEAS targets
Endocrine pathways
Pollinators

Experimental:

Site-directed mutagenesis

Attagene XS-2 Factorial assay (Dr. Blackwell)


-------
Predictive

\X 4T"

Approache:

i Sequence Structure

Function


-------
https://seqapass.epa.gov/seqapass/

Sequence Alignment to
Predict Across Species
Susceptibility

(SeqAPASS) •

s

Cf\ I 1 Society of
OV_/ 1 Toxicology

www.toxsci.oxfordjournals.org

TOXICOLOGICAI SCIENCES, 153(2), 2016, 22S-245

dot: 10.1093/toxsci/kfwl 19

Advance Access Publication Date: June 30,2016
Research article

Sequence Alignment to Predict Across Species
Susceptibility (SeqAPASS): A Web-Based Tool for
Addressing the Challenges of Cross-Species
Extrapolation of Chemical Toxicity

Carlie A. LaLone *,:L Daniel L. Villeneuve,* David Lyons,f Henry W. Helgen,*
Serina L. Robinson,5,2 Joseph A. Swintek,11 Travis W. Saari,* and
Gerald T. Ankley*

CVJSTO/i^

BUILT

^Or YO^


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What information is required for a SeqAPASS query?

United States
Environmental Protection
Agency

1.	Protein

2.	Species

Chemical-Protein Interaction

Knowledge of a sensitive or targeted species

Knowledge of the model organism used in an m vitro assay

Knowledge of the species for which the Key Event was developed

Chemical Molecular Target
in Target Species

Compare to Millions of Proteins
From housands of Species

Greater similarity = Greater likelihood that chemical can act on the protein
Line of Evidence: Predict Potential Chemical Susceptibility Across Species

10


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Flexible Analysis Based On Available Data

Level 1

Primary Amino Acid Sequence Alignments

Level 2

Conserved Functional Domain Alignments

Level 3

Critical (Close Contact) Amino Acid Conservation

seqapass.epa.gov/seqapass/



/ s

A

•* t

4

» V

4

^ J

./

./yv

./ yv*

./ Cn,-v

[ >

n

./ yv-

Gather Lines of Evidence Toward Protein Conservation


-------
SeqAPASS Predicts Likelihood of Similar
Susceptibility based on Sequence Conservation:



W

* no

no

Line(s) of evidence indicate

•	The protein is conserved

•	The protein is NOT conserved


-------
oE

United States
Environmental Protection
Agency

Evolution of the SeqAPASS tool

v5.0 (Nov. 2020): Develop visualization (Level 3), Develop Decision
Summary Report

v4.0 (2019): Improve visualization, user guidance, summary tables,
interoperability

v3.0 (2018): Develop visualization (Level 1 & 2), automate Level 3
Susceptibility Predictions

v2.0 (2017): develop Level 3 Susceptibility Predictions

vl.O (2016): Develop interface Level 1 & 2 and integrate essential
functionality

CRAWL

#1 ^	WALK

L. V	RUN


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a rpA

Strategic Approach to Species Extrapolation

United States
Environmental Protection
Agency

Computational:

Bioinformatics (Session 2 Demo)
Systematic review

Case Examples:
PEAS targets

Endocrine pathways
Pollinators

Experimental:

Site-directed mutagenesis

Attagene XS-2 Factorial assay (Dr. Blackwell)


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Deiodinase 3: Important enzyme in thyroid function

t

Partial Match Susceptible Yes

Ml

lodothyronine Deiodination

Tetra-iodothyronine (Thyroid
Hormone T4)

Site Directed Mutagenesis to Probe SeqAPASS Level 3

Mutate hDI03

Not a Match Susceptible No

SeqAPASS Critical Amino Acid Comparison

hDI03 mutants:

Sea lamprey

Fish

Fish

Frog

Lungfish

Sea lamprey

C168G
T169S
C239S
A240R
Y257A
Y257F

Common Name

Similar Susceptibility

| Amino Acid 1 |

| Amino Acid 2 |

| Amino Acid 3 | Amino Acid 4 |

| Amino Acid 5 |

Human

¦¦











Red drum







201S

202N



Blue tilapia









195L



Tongue sole









202N



Zebra mbuna





1 i3is 1

201T

202N



Nile tilapia







201T

202N



Senegalese sole





1 1315 1

201G

202N



Ballan wrasse





1 1315 1

201S

202N



Gilthead seabream





1 1315 1

201S

202N



Monterrey platyfish









196R



Amazon molly









196R



Shortfin molly









196R



Sapphire devil





130S

200G

201N



Southern platyfish









196R



Goldlined spinefoot









202E



Torafugu









202N



Sailfin molly









202N



Threespot wrasse









182N



Princess parrotfish









169N



Striped parrotfish









157N

1 - 1

Frogs and toads









204R



Two-lined caecilian

1 - 1

t29C

1301 ]



20 IP



Puerto Rican coqui







201C |

202R

Caecilians



09C

BOT

200C ~]

201P



Tropical clawed frog





13 IT

' 201C '

202R



African clawed frog





L29T

I99C ]

200R



Gabon caecilian

1 r |



131T

2G1C J

202P



American bullfrog







-0-C

203R



Coelacanth





d 1

202C

203F



Sea lamprey



1 1430 1

| I44S |



2I6P

1 233A I

Human Deiodinase 3 Enzyme


-------
Strategic Approach to Species Extrapolation

Computational:

Bioinformatics (Session 2 Demo)
Systematic review

Case Examples:
PEAS targets

Endocrine pathways
Pollinators

Experimental:

Site-directed mutagenesis

Attagene XS-2 Factorial assay (Dr. Blackwell)


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vvEPA

U.S. EPA Toxicity Forecaster ('l bxCast)

U.S. EPA ToxCast Program:

US EPA ToxCast Program: Uses mammalian cell-based assays to rapidly screen chemicals, identify putative molecular
targets, and identify those most likely to be endocrine disruptors

%

Key Questions for Consideration:

•	How well does this mammalian-based prioritization approach reasonably reflect potential impacts on other
vertebrates?

•	Can we expect chemicals that interact with mammalian receptors to also interact with receptors of other speciesf 7


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vvEPA

Hierarchal Framework for Evaluating Pathway
Conservation Using Existing Evidence

Analysis of structure
across species using in
silico computational tools

$trytfural Conservation (Molewlar Initiating Event)

¦ In silico approaches (e.g.. for proteins)

•	Primary ammo a Environ Toxicol Chern. 2016 Nov;35(11):2806-2816. doi: 10.1002/etc.3456. Epub 2016 Jun 28,

Evaluation of the scientific underpinnings for
identifying estrogenic chemicals in nonmammalian
taxa using mammalian test systems

Gerald T Ankley 1, Carlie A LaLone 2, L Earl Gray 3, Daniel L Villeneuve 2, Michael W Hornung 1

What other important endocrine targets
have a large base of pre-existing structural,
molecular target, and toxicity data?

-> Androgen Receptor (AR)

18


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Assess?ngAR Conservation Across Species Using the SeqAPASSTool



Invertebrates

Level 1: Analysis of AR Primary
Amino Acid Sequence
910 species
evaluated

A





1 if II III I 1| I I I I lit
fUi lit J!lmnIiia8fsiUrrn! Hfi

" " !i " " J S J



s i I =? =

S S

Vertebrates

I i u i

m a

Species Taxonomic Class

I 1

Invertebrates

Level 2: AR Ligand Binding
Domain
907 species

•



- • evaluated

i

1
1
1
•

I

• m

1
t

• II
»

1

0 1

¦

|j. Aw

			a	

1

~ • ~ A



infill f
• I Ml

s *

fWipPPWIW

HIT

H

3.

Level 3: Analysis of Conservation of
Individual Amino Acid Residues
250 species evaluated

Taxonomic Group

# of Spp.

Shared
Susceptibility

Mammals

117/1

Yes/No

Lizards, Snakes

11

Yes

Turtles

3

Yes

Birds

58

Yes

Crocodiles,

A

VaC

Alligators



i es

Amphibians

13

Yes

Coelacanths

2

Yes

Eel-shaped

1

Yes

Bony Fish

87/1

Yes/No

Sharks, Rays

4

Yes

Lungfish

2

Yes

Across all three levels, SeqAPASS results suggest conservation of
AR across vertebrate species

Overall, these predictions suggest that chemicals that bind and
activate AR in mammalian-based assays, are likely to interfere with
AR in other vertebrate species

Line of evidence for pathway conservation

Species Taxonomic Class

19


-------
Evaluating Existing Data to Extrapolate High-Throughput Androgen
Receptor Screening Data Across Species

Fewer Resources
*

Structural Conservation (Molecular Initiating Event)

¦ In silico approaches (e.g., for proteins)

•	Primary amino acid

•	Functional domain

•	Individual residues involved in chemical binding

Less Certainty

t

- I

Functional Conservation (Cellular Response)

¦ In vitro assays

•	Competitive binding assays

•	Transcriptional activation assays

I

Comparative Analyses (Organism Response)

In vivo studies

• Apical responses to chemicals
and adverse outcomes

More Resources

Greater Certainty

Evidence for Pathway Conservation

> Environ Toxicol Chem. 2016 Nov;35(11}:2806-2816. doi: 10.1002/etc.3456. Epub 2016 Jun 28.

Evaluation of the scientific underpinnings for
identifying estrogenic chemicals in nonmammalian
taxa using mammalian test systems

Gerald T Ankley 1, Carlie A LaLone 2, L Earl Gray 3, Daniel L Villeneuve 2, Michael W Hornung 2

¦I

K

Systematic Literature Review: A type of literature review that
uses systematic methods to collect secondary data, critically
appraise research studies, and synthesize findings

Using existing evidence (literature), we can evaluate the
scientific basis of our cross-species predictions

Advances in data science can improve this workflow

Gathering in vivo and in vitro data from vertebrate species
exposed to known androgenic compounds provides
additional lines of evidence for the conservation of the
biological pathway across species

20


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Evaluating Existing Data to Extrapolate High-Throughput Androgen Receptor
Screening Data Across Species

SeqAPASS Evaluation of Structural
Conservation Across Species

Systematic Evaluation of In Vitro
Cross-Species Data

Conserved?
Yes
No



Systematic Evaluation of In Vivo
^ Cross-Species Data

Weight of Evidence for Pathway
Conservation Across Species for
Defined Risk Assessment
Applications

Apply pathway to other targets of interest

Repeat process to account for the emergence of new information

21


-------
Strategic Approach to Species Extrapolation

Computational:

Bioinformatics (Session 2 Demo)
Systematic review

Case Examples:
PEAS targets
Endocrine pathways
Pollinators

Experimental:

Site-directed mutagenesis

Attagene XS-2 Factorial assay (Dr. Blackwell)


-------
I

A EPA

United States
Environmental Protection
Agency

Sequence

MTMTLHFKASGMALLHdllQGNEltPLNRPClLKIf'ttftPLGE
VYLQ55KPAYYNYPEGAA7r£FNAAAAANAQVYGQT(5tPTO
PG 5E AAA F LG G FP P L N S VS PSPl M LLH P P P Q.LS W LQ
PMGQQVPWLE N EPSGYTVREAGPPAjVRPhiSDNfl RQGGR
£RLASTNDKGSMAME^KFTftY£^^fcyM6YH¥G'iWSC

r-..... T..^- - ^. ,.r, *y0F?t'tTr" —\ • •-1 r

KCYtVGMMKGClRXOfA^nKHKRQROOOEOftCEVO
SAGDMRAftNLWPSPLMIRRKKNSLALSnADQMVSALLfl.
EPPILySEVDfTRPFSEASMUQLOTMLADRELVHMINWAKV
PGFVDtUHDQVMLl£CAWLEiLMIGLVWRSMEHPGKLLFA
PNUl DfiNOGKCVEGMVEIFDMLL ATSSfl FRMM NlQG EEF
VaK<.l!H,NS6VYTFlSSn!(Sl£El(OHilHRVlOKIT[>TLIHlM

Structure

Function

O

Improvements
in bioinformatics

Yes or No
Susceptible or Not Susceptible

Structural-based
comparisons of similarity
Predicted binding affinity

23


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SERA

United States
Environmental Protection
Agency

Advances in Drug Discovery/Development

Structure derived

from X-ray
crystallography

Human
Protein Structure

Bio in form at ics Toolbox:

Molecular modeling
Molecular docking
Virtual screening
Molecular dynamic simulations

Ligand X

2nd





Ligand Y









Ligand Z

r

1st

24


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SERA

United States
Environmental Protection
Agency

Application to Species Extrapolation

Human

Protein Structure

Ligand X

2nd



Frog

Protein Structure





Ligand Y





/

Ligand X

2nd



1st



Turtle

Protein Structure

Ligand X



1st

Ligand Y



Bird

Protein Structure

Ligand X

2nd



Bioinformatics Toolbox:

Molecular modeling
Molecular docking
Virtual screening
Molecular dynamic simulations

1st

Fish

Protein Structure

%



2nd

3rd

Fly

Protein Structure





25


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SERA

United States
Environmental Protection
Agency

Sequence

MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGE

VYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYG

PGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQ

PHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGR

ERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSC

EGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLR

KCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVG

SAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALLA

EPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINWAKV

PGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFA

PNLLLDRNQGKCVEGMVEIFDMLLATSSRFRMMNLQGEEF

VCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLDKITDTLIHLM

Structure

n | f * r

,/VYYYN

Final model

SeqAPASS Results from Level 1

Qiieiy Sequence FASTA + FASTA from 100s
of Aligned Sequences
Across Taxa

>NP_001434.1 Protein X [Homo sapiens]
MSFSGKYQLQSQENFEAFMKAIGLPEELIQKGKDI
KGVSEIVQNGKHFKFTITAGSKVIQNEFTVGEECE
LETMTG EKVKTWQLEG DN KLVTTFKNIKSVTELN
GDIITNTMTLGDIVFKRISKRI

>NP_787011.1 Protein X [Bos taurus]

MNFSGKYQVQTQENYEAFMKAVGMPDDIIQKGK

DIKGVSEIVQNGKHFKFIITAGSKVIQNEFTLGEECE

MEFMTGEKIKAWQQEGDNKLVTTFKGIKSVTEFN

GDTVTSTMTKGDWFKRVSKRI

>KFQ76585.1 Protein X [Phoenicopterus ruber
ruber]

MSFTGKYELQSQENFEPFMKALGLPDDQIQKGKD
IKSISEIVQDGKKFKVTVTTGSKVMQNEFTIGEECD
IEMLTGEKVKAWQMEGNNRLVANLKGLKSVTEL
NGDIITHTMTMGDLTYKRISKRI

>NP_001116883.1 Protein X [Xenopus
tropicalis]

MAFAGKYELVHQENFETFMKAIGLSDELIQKGKDV
KSVTEIQQNGKHFIVTVTTGSKVLRNEFTIGEEAE
LETPTG EKVKSWKLEG DNKLWQLKAITSTTELSG
DTITHVLTLNNLVFKRVSKRV

- 100s of FASTA

Sequences

Predicting Binding Affinity

Ligands of Interest for Docking

Collect Predicted Binding Affinity

re-assembly

Protein Structure Models
From 100s of Species

Generate
Protein Structures
For 100s of species

Template	Cluster Centroid

Graphic Modified from Zhang et al„ 2019 1-TASSER gateway: A protein structure and fimction prediction server powered by XSEDE Figure 1

Iterative Threading ASSEmbly Refinement

Develop Models for 100s of Species Based on Aligned Sequences
(I-TASSER; https: zhanglab.ccnib.med.umich.edu/I-TASSER/)

UCSF Chimera

DockPrep Structures and Minimize Ligands

AutoDock Vina

Dock Multiple Ligands to Protein Structures

assembly

Structure


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A EPA

United States
Environmental Protection
Agency

Acknowledgements

U.S. EPA. ORD

Donovan Blatz (ORISE)

Sara Vliet (ORISE)

Sally Mayasich (ORISE)

Marissa Jensen (Univ. Minnesota Duluth)

GDIT

Thomas Transue
Cody Simmons
Audrey Wilkinson

SeqAPASS v5.0

https ://seqapass. epa. gov/ seqapass/

27


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oEPA

United States
Environmental Protection
Agency

Novel in vitro Methods for Ecological
Species: Evaluating Cross-species Differences
in Nuclear Receptor-Ligand Interactions

B.R. Blackwell, D.L. Villeneuve, G.T. Ankley, CA. La Lone, J.A. Doering

\

Office of Research and Development

Center for Computational Toxicology and Exposure, Great Lakes Toxicology and Ecology Division

Progress for o Stronger Future


-------
W|P_ chemicals in the Environment

•	Hundreds of chemicals detected in

contaminant Pathways	the environment

•	Contaminants of emerging concern
(CECs) include those with limited
toxicity data

•	Recognized as critical data gap by
stakeholders:

• OCSPP; OW; Regions: Great Lakes
National Program Office (GLNPO)

•	Effects-based monitoring a tool for
understanding impacts and potential
risks of contaminants

t\\ Runoff and
\ Discharges

Sediment

Rivers and
Streams


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SERA

United States
Environmental Protection
Agency

nvironmental Monitoring with Attagene TRANS-FACTORIAL Assay

THRal	ERa

PXR	~			' LXRa

ERRa

NURR1

HNF4a

RXRb

PPARa

RARb

RARa

PPARg

LXRb

RORb

RXRa

FXR

PPARdl	8

PXR
ERa
PPARy
GR

PPARa
RXR|3

Do the human receptors
adequately represent
sensitivity of aquatic
vertebrate receptors?

Among the most frequently detected
nuclear receptor activities in surface
water samples


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¦SEPA r	| .

Cross-species extrapolation

United States
Environmental Protection
Agency

To date, high throughput screening has been human centric

Unclear how well mammalian HTS assays represent
vertebrate diversity, let alone other phyla.

Not feasible to include all taxa in a HTS screening program.

How can we strategically select the minimum number of
representative species that cover the maximal range of
variation in sensitivity and specificity?

4


-------
AEPA

United States
Environmental Protection
Agency

Attagene EcoTox FACTORIAL Assay

t

GAL4-NR1
GAL4 RTU,



9







GAL4-NR2
GAL4RTU, ,

-



•





•





•





GAL4-NR»,
, GAL4 RTUn ,

-+¦



Evaluated
Compound

O

profiling
reporter RNAs


O
1

o
o

1

AR

Reptilian

Chrysemys picta

XM

005279527

AR

Avian

Gaiius gaiius

NM

001040090

AR

Mammalian

Homo Sapiens

NM

000044

TRa

Fish

Danio rerio

NM.

.131396.1

TRP

Danio rerio

NM

131340.1

TRa

Amphibian

Xenopus iaevis

NM

ID

-------
jg™S, Pro,action SpGC iGS S G l G Ct \ O Pi

Is the selection of one representative vertebrate from each class the
best way to cover the potential variability in sensitivity?

Could available information be used to guide a more strategic selection?

•	Documented species differences in sensitivity to ligands

•	Amino acid residues identified as critical to ligand binding in one
or more species

•	In silico analyses of conservation/variation in aa sequence using
SeqAPASS


-------
&EPA

United States
Environmental Protection
Agency

PPARy - established cross-species differences



-

->T _ «v

" W

rmKKKF

|JL

v -¦• V.'V. o

Zebrafish	]

^ Plaice	I

Sea Bream	]

Clawed Frog	HI

\

A*.

Rat
Mouse

> 200-fold difference In
transactivation of PPARy

by Rosiglitazone

Human

o

0.2

0.4	0.6	0.8	i	1.2	1.4

Relative Transactivation


-------
SERA

United States
Environmental Protection
Agency

SeqAPASS Analysis

https://seqapass.epa.gov/seqapass/

03

LT)

50

c

O)

u 40

 Zebrafish

I

Compares amino acid sequence information for
all species for which there are data in the NCBI
protein database.

•	Level 1 - Primary Sequence

•	Level 2 - Conserved domains

•	Level 3 - Individual amino acid residues

T ^



T T



i/i	i/> rb */)	 >•
< -a
o

  u

x

_ft
Q.
C O
O -C
ci y
o

2 T3 ^

Taxon


-------
mple SeqAPASS Level 3 - PPARy

•	Only 4 positions showed important differences in amino acids among PPARy

•	2 positions known to significantly alter interaction of ligand (rosiglitazone) with PPARy

Taxa

# of Species

Position 1
(Ile309)

Position 2 Position 3
(Gly312) (Cys313)

Position 4
(Tyr355)

Susceptibility
Prediction



Human

1

1

G C

Y

Yes

All Mammals 107

1

G C

Y

Yes



Mallard-type 1

1

G C

Y

Yes



Most Birds 70

1

R C

Y

No



All Reptiles 19

1

R C

Y

No

Strongly conserved among most birds,

All Amphibians 2

1

R C

F

No

amphibians, reptiles

Ancient Fishes 9

F

R C

1

No



Most Fishes 61

F

S C

1

No

More variation among various orders of

Salmonid-type 3

V

R 1

T

No

fishes than across other vertebrate

Bonytongue-type 1

F

R W

1

No

classes

Zebrafish-type 2

F

S Y

1

No

Exa

United States
Environmental Protection
Agency


-------
V'ER* Example SeqAPASS Level 3 - PPARy

United States
Environmental Protection
Agency

In silicomechanism for lack of Rosiglitazone binding to zebrafish PPARy is severe steric
hindrance from Gly312Ser and Cys313Tyr mutation

Comparing positions 312 and 313 of human to other species

Taxa

Species

Position
312

Position
313

Susceptibility
Prediction

Relative
Transactivation

Mammal

Human

G

C

Yes

1.0

Mammal

Mouse

G

C

Yes

1.2

Mammal

Rat

G

c

Yes

1.2

Amphibian

Clawed Frog

R

c

No

0.06

Fish

Sea Bream

S

c

No

<0.006

Fish

Plaice

S

c

No

<0.006

Fish

Zebrafish

S

Y

No

<0.006

10


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5-EPA —»	. A	.

Strategic Approach

United States
Environmental Protection
Agency

Similar types of analyses applied to
GR

PPARa
RXRb

Selected a group of species that should capture maximum
diversity in response for these four NRs (& genomes available)

•	Human

•	Xenopus laevis

•	Rainbow trout

•	Japanese medaka

•	Zebrafish


-------
oE

United States
Environmental Protection
Agency

Attagene EcoTox-2 Factorial assay



#

Name

Species

Latin names



1

GR

human

Homo Sapiens



2

GR

african clawed frog

Xenopus laevis



3

GR

rainbow trout

Oncorhynchus mykiss



4

GR

japanese medaka

Oryzias latipes



5

GR

Zebrafish

Danio rerio



6

PPARa

human

Homo Sapiens



7

PPARa

african clawed frog

Xenopus laevis



8

PPARa

rainbow trout

Oncorhynchus mykiss



9

PPARa

japanese medaka

Oryzias latipes



10

PPARa

Zebrafish

Danio rerio



11

PPARg

human

Homo Sapiens



12

PPARg

african clawed frog

Xenopus laevis



13

PPARg

rainbow trout

Oncorhynchus mykiss



14

PPARg

japanese medaka

Oryzias latipes



15

PPARg

Zebrafish

Danio rerio



16

RXRb

human

Homo Sapiens



17

RXRb

african clawed frog

Xenopus laevis



18

RXRb

rainbow trout

Oncorhynchus mykiss



19

RXRb

japanese medaka

Oryzias latipes



20

RXRb

Zebrafish

Danio rerio



21

ERa

human

Homo Sapiens



22

ER1

Zebrafish

Danio rerio



23

ER1

african clawed frog

Xenopus laevis





AR

human

Homo Sapiens

\—X

AR

Zebrafish

Danio rerio

•	14 chemicals in concentration-response

•	Surface water extracts

12

M-61

AR-ZF

RXRb-FR

GR-FR

RXRb-Hu

PPARa-RT

PPARg-JM

GR-JM

PPARg-FR

AR-Hu

PPARg-Hu

ERa-Hu

PPARg-ZF

PPARa-ZF

PPARg-RT

ER1-FR

GR-ZF

M-32

M-19

PPARa-Hu

GR-RT
PPARa-JM

RXRb-ZF

RXRb-RT

M-06

GR-Hu

PPARa-FR

RXRb-JM

ER1-ZF


-------
i5rSip,o,",ion Tgst Chgmica Is

Test Chemical

Target

Rosiglitazone maleate

PPARg

Tributyl phosphate

PPARg, PXR

Prednisone

GR, AR

Troglitazone

PPARg, PPARa

Zileuton

PPARg; ALOX5

Bexarotene

RxRb

Gemfibrozil

PPARa

Butachlor

GR, AR (env)

Triphenyl phosphate

PPARg (env)

Fenofibrate

PPARa

Dexamethasone NaP04GR

Triphenyltin chloride

RxR, RAR

PFOA

PPARa (env)

Potassium PFHxS

PPARa (env)


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5-EPA

Results - PPARy

United States
Environmental Protection
Agency

Rosiglitazone maleate
Troglitazone-
Triphenyltin chloride-
Triphenyl phosphate-
Tributyl phosphate-
Zileuton-





T

T

T

* ^ J>°

<§>	V

l/	J
-------
oE

United States
Environmental Protection
Agency

Results - PPARa

Gemfibrozil -

Fenofibrate-

PFOA-

Potassium PFHxS-

Log ACC
4

>
-------
Results - RXRB

United States
Environmental Protection
Agency

Bexarotene-

Triphenyltin chloride-l





























4*

v*°

&

&

O* o*



.«¦

<5-

Rainbow trout and zebrafish RXRb
were less sensitive to RXRb ligands
than the other species tested.

16


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«>EfB	nQf | ilfc r~~ Q

Environmental Protection	£_J I III	— I ^

Agency	I \ CI O U I I O	VJ I \

Predicted Susceptible

Taxa

Homo
sapiens

Xenopus
laevis

Oryzias
latipes

Oncorhynchus
mykiss

Danio rerio

Dexamethasone

Y

Y

N

N

Y

Dexamethasone NaP04
Prednisone
Butachlor































t——I——I——I——r

Log ACC	• Predictions were qualitatively accurate

4	for dexamethasone but reflected

l_gss

potent	different sensitivity, not overall

susceptibility

o

More # Need t0 nnetabolically activate
potent	prednisone to the GR-active prednisolone

complicates interpretation

17


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oE

United States
Environmental Protection
Agency

Application to Environmental Monitoring

_0J
Q.

E

03
LO


03

	<£> * <£? ^	oD'

* o


-------
AEPA ^ . .

sr1Conclusion

•	Effects-based monitoring employing human cell lines using human nuclear receptors
(hNR) are likely to yield different conclusions than if fish NRs were employed (at least
for PPARy, PPARa, RXRp, and GR).

•	Variations among different orders offish may be as substantial as across other classes
of vertebrates.

•	Different chemical-specific profiles across species were consistent with a previous
assumption that level 3 SeqAPASS analyses based on specific ligand-chemical
interactions may not apply universally across relevant chemical space.

• Complicates the ability to select a minimum number of species to capture
maximum variability in sensitivity.

Screening of additional chemicals using the XS-2 Factorial Assay may yield new insights
that improve the ability to predict cross-species susceptibility based on aa sequence.


-------
AEPA

United States
Environmental Protection
Agency

References

•	Cavallin et al. Effects-Based Monitoring of Bioactive Chemicals Discharged to the Colorado River
before and after a Municipal Wastewater Treatment Plant Replacement Environmental Science &
Technology 2021, 55, 2, 974-984. httos://doi.org/10.1021/acs.est 0c05269

•	Lalone et al. Sequence Alignment to Predict Across Species Susceptibility (SeqAPASS): A Web-
Based Tool for Addressing the Challenges of Cross-Species Extrapolation of Chemical Toxicity.
Toxicological Sciences, Volume 153, Issue 2, October 2016, Pages 228-245,

httos://doi. org/10.1093/toxsci/kfw119

•	Medvedev et al. Harmonized cross-species assessment of endocrine and metabolic disruptors by
EcoTox FACTORIAL assay. Environmental Science & Technology 2020 54, 19, 12142-12153.
https://doi. org/10.1021/acs. est. 0c03375


-------
oEPA

United States
Environmental Protection
Agency

High Throughput Transcriptomics:
A Multi-Species Approach

Presented by Kevin Flynn
to

US EPA BOSC

Chemical Safety Subcommittee Meeting

Office of Research and Development

Center for Computational Toxicology and Exposure


-------
AEPA

United States
Environmental Protection
Agency

ORD Strategic Research Action Plan

CSS. 1.7:

Develop, evaluate, and apply non-mammalian high-throughput toxicity tests for
priority endpoints and pathways in ecological species for ecological risk assessment

CSS.4.4:

Develop rationale and case studies that apply AOPs and HTT data to inform test-order
decisions and establish scientific support for waiving testing requirements for pesticides

Office of Research and Development

Center for Computational Toxicology and Exposure


-------
oE

United States
Environmental Protection
Agency

Program Office Feedback & Support

Program Office support

•	Office of Pesticide Programs (OPP)

•	Office of Pollution Prevention and Toxics (OPPT)

EPA/ORD Partner Needs and Use

OCSPP; OW:

Ecological risk assessments address species across diverse taxonomic groups, many of which have limited or no available
data. The clear majority of HTT methods are based on either human or mammalian in vitro systems, which results in an
under-representation of pathways that are relevant and perhaps unique to non-mammalian taxa

OPP:

"The proposed research is responsive to EPA's commitment to reduce its reliance on resource intensive whole animal
testing and to better allocate limited resources to where they are most needed through the use of more effective
screening tools"

•	evaluate taxonomic domain of applicability of HTT NAMs

•	determine relevance to regulatory assessment endpoints

•	provide evidence that risk estimates across taxa are suitable

•	critical effort to turning theory into practice (risk estimates)

OPPT:

"HTT methods are required for OPPT to rapidly and efficiently screen and prioritize new and existing chemical substances
under the Toxic Substances Control Act (TSCA)."

•	meet scientific standards under section 26(h) of TSCA

•	reduce testing on vertebrates under section 4(h) of TSCA

•	determine unreasonable risk under sections 5 & 6 of TSCA

Demonstrating quantitative relationships between
transcriptomic responses and phenotypic alterations
in apical assessment endpoints across multiple taxa
will provide a compelling means of promoting the
adoption of such methods and incorporation of such
data in ecological risk assessments - OPP comment
to Eco-trans Output

The effort should provide an understanding of
how the battery of assays relate an AOP where a
molecular initiating event leads to a sequence of key
events that culminate in an adverse outcome at the
whole organism level and how such methods can be
used to effectively screen for effects across a wide
taxonomic and chemical space. OPP has a wide array
of in vivo data on pesticides and these data could
serve as a means of assessing the extent to which the
battery of assays is predictive across chemicals/taxa -
OPP comment to Eco-trans Output

OPP has a broad array of in vivo data across multiple
taxa with which to compare transcriptomic responses
once suitable linkages have been demonstrated. OPP
is interested in working with ORD to identify
"model" chemicals - OPP comment to Eco-trans
Output


-------
&EPA

United States
Environmental Protection
Agency

A Chemical Numbers Problem

U.S. EPA Strategic Plan (2018-2022), Objective 1.4,
Ensure Safety of Chemicals in the Marketplace

Problem Statement:

Tens of thousands	of chemicals

hundreds	more are introduced

Only a small fraction	has been

potential	risks to human	health

"Too many chemicals, too little data"

Office of Research and Development

Center for Computational Toxicology and Exposure


-------
£EPA

United States
Environmental Protection
Agency

A Biological Numbers Problem

Gene Coverage

ToxCast

Not in
ToxCast

"Throughout the development and execution of ToxCast and Tox21, key
limitations of the current suite of HTS assays have been identified (Tice, et
a!., 2013). The limitations include inadequate coverage of biological
targets and pathways" Thomas et al. 2019

The Eco Data Gap:

Humans are just a tiny fraction of the biological diversity we

are charged to protect.

Many genes/pathways are conserved

Unique physiology in other kingdoms, phyla, classes...

Nematodes
Chordates
Crustaceans
Arachnids

Other

Plants

Moliusks

Insects

Office of Research and Development

Center for Computational Toxicology and Exposure


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&EPA

United States
Environmental Protection
Agency

HTP Eco Assay DeveDopment

Daphnia magna	Pimephales promelas	Chironomus dilutus	Raphidocel/s subcapitata

•	Modify standard protocols and methods to allow rapid toxicity tests with small aquatic organisms in
96-well plates - 4 species

•	Conduct exposures with diverse chemicals (ex. metals, neonics, pharmaceuticals, PFAS)

•	Compare traditionally derived LC50 values to LC50 values calculated from 96-well plate-based
exposures

•	Use RNA-seq data to calculate transcriptomic-based point-of-departure (tPODs) that can be
anchored to apical responses

Office of Research and Development

Center for Computational Toxicology and Exposure


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SERA

United States
Environmental Protection
Agency

HTP Eco Assay DeveOopment

Control

Replicates /

v

A
B
C
D
E
F
G
H

V

oooooooooooo

24 h exposure

8 9 10 11 12

Phenotypic anchoring
• survival
behavior

growth?

Office of Research and Development

Center for Computational Toxicology and Exposure

Species

Guideline Test Method

Age at Start

Temp

Daphnia magna

850.1010 Aquatic Invert Acute Toxicity

72-hour

20° C

Pimephales promelas

850.1075 Fish Acute Toxicity

24-hour

25° C

Chironomus dilutus

850.1790 Chironomid Sediment Toxicity

3rd instar

20° C

Raphidoceiis subcapitata

850.4500 Aigai Toxicity

Log-phase

24° C

Exposures Design
1 ml deep 96-well plates

12 concentration - 8 replicates per concentration
1 individual per well (algae ~5 x 104 cells/ml)

24-hour static exposures
phenotypic endpoints assessed

animals: survival and behavior
algae: cell viability & division, photopigments
then after homogenization, RNA extracted for transcriptomics

Species

Time to Load Plate

Control 24-hour Survival

RNA Qty per Well

Daphnia magna

~45 minutes

72-hour

~1000 ng

Pimephales promelas

~3Q minutes

24-hour

~1500 ng

Chironomus dilutus

~60 minutes

3rd instar

~900 ng

Raphidoceiis subcapitata

~10 minutes

Log-phase

~300 ng


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SERA

United States
Environmental Protection
Agency

HTP Eco Assay DeveOopment

Toxicant

Chemical
initiator

LC50s:

Published vs 96-well Exposure

.1	1	10

Plate LC50

Office of Research and Development

Center for Computational Toxicology and Exposure

Macro-Molecular

Interactions













Cellular
Responses

Organ
Responses

TndivicIuaF
Responses

Increasing levels of biological organization

Population
Response

Linking to apical endpoints essential
Apical Endpoints

•	Survival &

•	Reproduction

•	Growth & orc?

Behavior

"Imageable" measurements


-------
SERA

United States
Environmental Protection
Agency

Eco Transcriptomics Applicability

NTP

National Toxicology Program

U S. Dopartmont of Health and Human Services

NTP Research Report on

National Toxicology
Program Approach to
Genomic Dose-Response
Modeling

NTP RR 5
APRIL 2018

A.3 Global Comparison of POD and BEPOD

6

l-ioo

1	10	100	1000

Apical Potency Value with 1/2 log range

Figure 1-1. Comparison of the Most Sensitive Apical Vz Log Potency Range to the Most Sensitive GO
Biological Processes BEPOD

Data from Figure 1-Figore 13 in tins document were compiled to allow a lareer scale corrpprisoa of apical and gems set-based
biological potency estimates. The most sensitive 3pical potency values (NOAEL or BMD) frcoi guideline imorify assessments
are plotted on tie x-asis and tie BEPOD range (BMDi.-BMD-BMD-j) from die GO Biological Processes analysis from 4- or
5-day GDHS studies are plotted on the y-axis. A diagonal 1-to-l line is drawn as reference to perfect agreeivnt between tie
potency values. The points to The left of tie line demonstrate mote sensitive apical endpoims, niereas tiose to the right exhibited
more sensitive BEPODs. Overall, the apical and BEPOD \-alues strongly agree, as indicated by R: = 0.89.

Number of mammalian studies have shown short-term
transcriptomics-based PODs are predictive of apical potency.

Generally, within /2 log.

Office of Research and Development

Center for Computational Toxicology and Exposure

ELSEVIER

Toxicology and Applied Pharmacology 378 (2019) 114634

Contents lists available at ScienceDirect

Toxicology and Applied Pharmacology

journal homepage: www.elsevier.com/locate/taap



Transcriptomic points-of-departure from short-term exposure studies are
protective of chronic effects for fish exposed to estrogenic chemicals

Florence Page-Lariviere, Doug Crump, Jason M. O'Brien

Naaonai WltSife Research Center, Envimnmem and CBmiSe Change Canada. Ontario. Canada

H)

F. Pagf-Larmire. a at

A

Toxicology and Applied Pharmacology 378 (2019) 114634

/'


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SERA

United States
Environmental Protection
Agency



HTP Eco Transcriptomcs

Challenge.gov

Govern men! Challenges, Your Solutions

EcoTox TARGET Challenge

Develop high quality, low-cost tools that assess global gene expression in
common aquatic toxicity test organisms

S3 TOTAL CASH PRIZES OFFERED: $300,000
=TYPE OF CHALLENGE: Scientific

2t PARTNER AGENCIES | FEDERAL: U.S. Army Engineer Research and Development Center

12 PARTNER AGENCIES | NON-FEDERAL: DoW, Environment and Climate Change Canada, European Commission

Joint Research Centre, Syngenta

EB SUBMISSION START: 03/19/202012:00 PM ET

O SUBMISSION END: 06/15/202111:59 PM ET

Detection/analysis
technology

TARGET

EcoTox Challenge

\

&EPA

Innovation: $300,000 EPA Research Challenge Prize Available

EPA is looking for innovators who can help usher in the
next generation of Technology Advancing Rapid
Gene Expression-based Testing (TARGET).

The Agency is offering a $300,000 prize to the
company, organization, or team that can provide high
quality, low cost, technologies/platforms for evaluating
global gene expression in samples (RNA or tissue
homogenates) from four commonly used aquatic
toxicity test organisms:

*	Pimephales promelas (a fish)

¦	Daphnia magna (a crustacean)

*	Chironomous dilutus (an insect; formerly Chironomous tentans)

¦	and Raphidocelis subcapital (a green algae)

Think you have a winning technology? Learn more at:

Office of Research and Development

Center for Computational Toxicology and Exposure



Commercial
Development

4 "Solvers"



Commercially available
Low cost (<$50/sample)
High quality
Maxima! coverage

TARGET

I

EcoTox Challenge


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SERA

United States
Environmental Protection
Agency

Eco Transcriptomocs Data Analysis

Transcriptomics Analysis Workflow

•	not re-inventing the wheel

•	mirror ToxCast data analysis

BMDExpress2

Chemical +
Eco-species

Eco-

Transcnptomics

Raw data
processing

Data QC



Differential
expression
analysis



Pathway
Aggregation

Concentration Response

'• Si:

- h.#

¦i-M

¦ •>'sSV

¦¦M

te-.

Oown
Not S«)

c5H ¦
:

IS

i

* . L
x

_

34,6 H
« B

i

44 I

I E5.0

Concentration Response

Concentaaon
~ hXltDAi—MhH VIM !>L0Ta

Office of Research and Development

Center for Computational Toxicology and Exposure

symmetric, uriimodal

mud.

uniform	bi modal	multimodal

BMD Grouping

All BMDs - median
X lowest (ex. 20)

Percentile (ex. 10th)

1st mode

All BMDs from lowest GO terms or REACTOME pathways
Median BMDs from 20 lowest GO terms or REACTOME pathways


-------
&EPA

United States
Environmental Protection
Agency

Current Status

Mcc6lerating tno ^dOG of C/h6rniC3l Risk Asssssrn0nt

APCRA '.»•

^ ^" • 4*^ ~ • j6.

Derive transcriptomics-based points of departure for 20 chemicals
Testing with fathead minnow only

Compare with traditional apical PODs

Evaluate hypothesis that tPODs are protective relative to apical
Includes chemicals of direct interest to Program Offices and partners

Workflow in Brief

RNA-seq data was obtained from each well; all raw reads were assembled into transcript models,
aligned with annotations, counted, normalized, and log2 transformed for each transcript

•	Low count feature filtering: any given feature had to have a count of 10 or more in a minimum of
4 samples or that feature was filtered out

•	Differentially expressed genes (DEGs) determined by NTP guidelines and transcriptomic POD
for a chemical defined as median or 10th percentile POD of all DEGs

(https://ntp.niehs.nih.gov/publications/reports/rr/rr05/index.html)

Office of Research and Development

Center for Computational Toxicology and Exposure


-------
AEPA

United States
Environmental Protection
Agency

HTP Eco Assay Development

Chemicals

Chemical Class

Rationale

Data Product Support

CuS04, IMiS04, ZnS04

metal

OW; ease of exp.; mouse & RBT data

APCRA case study; 4 eco-species

Clothianidin, Thiacloprid, Imidacloprid

Neonicotinoid

OPP

APCRA case study; 4 eco-species; Challenge

Flupyradifurone

Butenolide

OPP

APCRA case study; 4 eco-species

Sertraline, Fluoxetine, Paroxetine

SSRI

Existing data at GLTED

APCRA case study; 4 eco-species

Atrazine, simazine, cyanazine

Herbicide

Herbicide

Challenge; 4 eco-species

Methoxyfenozide, tebufenozide,
methoxyfenozide

Carbohydrazide

Insecticide

Challenge; 4 eco-species

Parathion, methidathion, fenthion

Organophosphate

mouse data

APCRA case study; 4 eco-species

dibutyl, diethylhexyl, butylbenzyl
phthalates

Phthalates

TSCA high priority

APCRA case study; 4 eco-species

~20 specific PFAS

PFAS

PFAS plus up; small # in vivo

4 eco-species

50 -100 additional

diverse

St RAP

4 eco-species

Office of Research and Development

Center for Computational Toxicology and Exposure


-------
SERA

United States
Environmental Protection
Agency

BMDiHi;

Express2J

Draft Data

A»NTP AEPA

[Sensitive apical
[tPOD] < endpoirit]



it

[tPOD]

[Sensitive apica

«<

endpoint]

¥

Chemical

Transcriptomic POD
(10th and median)

96-hour
LC50

Mortality-based
POD

CuS04

0.005 mg/L

0.03 mg/L

0.3 mg/L

0.2 mg/L

ZnS04

0.063 ug/L

0.23 ug/L

2.2 mg/L

3.2 mg/L

NiS04

0.146 mg/L

0.33 mg/L

6.2 mg/L

3.9 mg/L

Imidacloprid

0.03 ug/L

8.8 mg/L

173 mg/L

> 10 mg/L

Flupyradifurone

0.0226 ug/L

1.3 mg/L

Not in ECOTOX

> 10 mg/L

Clothianidin

0.2 ug/L

8.1 mg/L

0.5(104) mg/L

> 10 mg/L

Thiacloprid

0.036 mg/L

57.2 mg/L

104 mg/L

85 mg/L

Sertraline	0.001 mg/L 0.6 mg/L	0.1 mg/L	0.9 mg/L

Fluoxetine	0.003 |ig/L 0.02 mg/L	0.2 mg/L	0.8 mg/L

Paroxetine	0.002 mg/L	1.0 mg/L	3.5 mg/L	1.1 mg/L

Office of Research and Development

Center for Computational Toxicology and Exposure


-------
SERA

United States
Environmental Protection
Agency

Upcoming Work

Assay Development
Verify water quality parameters

•	dissolved oxygen

•	pH

•	ammonia
Chemical bioava lability

POD Calculation for CuSo4 in each Volume

BMDExpress2 Results

Volume Format



CUP

24WP

96WP

#DEGs passing NTP filters1

128/369

52/159

108/208

Median POD (mg/L)

0.0445

0.045201

0.025

CUP vs 96WP

CUP vs 24WP

24WP vs 96WP

Office of Research and Development

Center for Computational Toxicology and Exposure

Overlap of DEGs

Validation

Transcriptomics

•	Complete Challenge

•	platform development

•	genome annotation

•	Definition/Implementation of analysis pipeline

•	Assess variability focused on tPODs

•	intra/inter exposure plate

•	between exposure plates

•	appropriate replication

CuS04 — Replicate Sub sampling 12x: tPODs

0.015-

D-OIO-

_e

Q

o
9b

O-005-

O-OOO-

4	5	6

Number of Replicates


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&EPA

United States
Environmental Protection
Agency

Contributors

The "We"

ORD CCTE GLTED-MIB: Adam Biales, David Bencic, Robert Flick, John Martinson

ORD CCTE GLTED-STB: Kevin Flynn, Dan Villeneuve, Kathy Jensen, Jenna Cavallin
ORD CCTE GLTED-TTB: Russ Hockett, Teresa Norberg-King

ORD CCTE BCTD-RADB: Josh Harrill

ORD CCTE BCTD-CTBB: Logan Everett

ORISE FELLOWS: Michelle Le, Kelvin Santana-Rodriguez, Kendra Bush, Monique Hazemi

Acknowledgements

Christina Inglis, John Prindiville, Andy Nong, Jason O'Brien, Florence Page-Lariviere

I ^ | Environment and

Climate Change Canada

Environnement et
Changement climatique Canada

Office of Research and Development

Center for Computational Toxicology and Exposure


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Rpfprpnrpq

Environmental Protection	J m	I	I	I I

•	U.S. EPA Strategic Plan (2018-2022), Objective 1.4, Ensure Safety of Chemicals in the Marketplace

•	Thomas, R. S., Bahadori, T., Buckley, T. J., Cowden, J., Deisenroth, C., Dionisio, K. L.,... & Williams, A. J. (2019). The
next generation blueprint of computational toxicology at the US Environmental Protection Agency. Toxicological
Sciences, 169(2), 317-332.

•	Page-Lariviere, F., Crump, D., O'Brien, J. M. (2019). Transcriptomic points-of-departure from short-term exposure
studies are protective of chronic effects for fish exposed to estrogenic chemicals. Toxicology and Applied
Pharmacology, 378, 114634.

•	EcoTox TARGET Challenge: https://www.challenge.gov/challenge/ecotox-challenge/

•	National Toxicology Program Approach to Genomic Dose-Response Modeling:
https://ntp.niehs.nih.gov/publications/reports/rr/rr05/index.html

Office of Research and Development

Center for Computational Toxicology and Exposure


-------