SBIR/STTR Research Award

Developing Novel Arginine Biased Arrays for Epigenetic Research

Award identifier 80ea99bf22bee43b3a6bb71b32c72acfa3cca28f78f531dc8cba25ee17aafd37Awarding agency Department of Health and Human Services · National Institutes of Health

Award amount

$1,499,995

Program and phase

SBIR · Phase II

Award year

2017

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Award details

Awarding agency
Department of Health and Human Services
Branch
National Institutes of Health
Recipient company
EPICYPHER, INC.
Proposal award date
2017-08-01
Contract end date
2019-07-31
UEI
UWNWSADJYYZ3
Solicitation number
PA16-302
Topic code
400

Research abstract

PROJECT SUMMARYEpigeneticregulatorsrepresentanewfrontierindrugdiscoveryandarerapidlyattractingpharmaceuticalinterestsduetotheirremarkabledruggabilityandstrongconnectionwithhumandiseasese gmetabolicsyndromesneurodegenerativedisordersandcancersTodatetheepigenomeconsistsofoverknownproteinsHoweververyfewepigeneticmodifiersarebeingpursuedindrugdevelopmentprograms due to our limited understanding of what proteins these enzymes regulateThis narrow saturation oftheepigeneticdrugarenaisfueledbyadearthoftoolstosystematicallyidentifyandcharacterizepotentialtargetsTo aid in the discovery of novel relationships between enzymes and the proteins that they targetwe willcommercializehighcomplexityorientedpeptidearraylibrariesOPALsInPhaseIstudieswesynthesizedOPALlibrariescomprisingacorearginineROPALorlysineKOPALresiduewithflankingdegeneratesequencesoraminoacidsinbothNandCterminaldirectionsFigureanddemonstratedthatOPALsarepowerfultoolstosystematicallycharacterizetargetmotifsofwriterenzymesOurfocushereistodevelop OPALs to examinewriterenzymes that modify lysine or arginine residuesIn Phase IIEpiCypher willscale up synthesis of the unmodified KOPAL and ROPAL peptide libraries and optimize a highthroughputwell assay format for validation using methyltransferase assays developed in the Phase I studiesAimWewillalsovastlyexpandthecommercialutilityofourdiscoveryplatformontwofrontsdevelopinganonradioactive detection system and a userfriendly data analysis pipeline establishingAimandexpandingour KOPAL platform to analyze lysineacylation writer enzymesAimSeven additional lysinemodified acylgroupposttranslationalmodificationsofwhichacetylationisafoundingmemberhavebeenrecentlyidentifiede gcrotonylationbutyrylationor propionylationwhich function together with lysine acetylation toregulategeneactivationGiventhewelldescribedroleofhistoneacetylationindiseasethesenewacylationPTMsrepresentanexcitingnewfieldofepigeneticstudythathasgreatdrugdevelopmentpotentialTheinnovativediscoveryplatformdescribedhereinprovidesthefirstcomprehensivescreeningtooltostudyepigeneticwriterenzymesEpiCypherhasassembledastrongscientificteamconsistingofpioneersinthefieldofepigeneticregulationDrsMarkBedfordandScottRothbartanddetectionchemistryDrMarceyWaterstodeveloparobustversatileanduserfriendlydiscoveryplatformthatwillhaveapowerfultranslational impact on epigenetic research and therapeutic development

Technology keywords

Not reported

Other awards by this recipient

Verified by the same UEI. These are other public SBIR/STTR award pages, not a merged company record.

Awards with the same topic code

Verified by an exact topic code match. This is not a text-similarity match.

Research funding history

64 SBIR/STTR records share this UEI (2014–2025). Reported award amounts total $79,150,531. Reported amounts are not federal obligations.

Phases: Phase I, Phase II, Phase II – Direct to Phase II

Agencies: Department of Health and Human Services

Agency intelligence

Department of Health and Human Services

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