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Epigenetic Probes for HMTs

Award Number: R44TR000940
ORGANIZATION: NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 06/20/2014
PERIOD OF PERFORMANCE END DATE: 03/31/2018

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Epigenetic Probes for HMTs - ¿ DESCRIPTION (provided by applicant): Epigenetic proteins, such as histone methyltransferases represent important potential drug targets for indications like cancers, neurodegenerative disorders, and cardiovascular and metabolic diseases. At Reaction Biology Corporation ("RBC"), we are working toward the complete coverage of all epigenetic targets, including HMTs, to identify and improve epigenetic modulators that can be used in research and drug discovery. In this Phase II application, we have proposed three aims following successful Phase I studies to continue the understanding of HMTs' biological functions and as new drug targets. The aims include 1) Complete the screening of HMTs for identifying new probes and building the chemical-epigenetic data base; 2) Broader HTS and Structure-Activity Relationship (SAR) study to identify and increase the potency of NSD inhibitors; and 3) Evaluating NSD inhibitors' efficacy in cell based assays, and determining their kinetic MOAs and early DMPK/tox profiles. We'll meet the following milestones: (1) Develop and commercialize 10 or more HMT probes as general research tools for at least 5 HMTs; 2) Improve at least 2 lead compounds' potency into the nanomolar range against NSDs that have different structure scaffolds, with good cell based activity and DMPK profiles; and (3) we will be able to launch one of the largest publicly available chemical-epigenetic data bases built on the screening activities from the compound collections that include most of the FDA approved drugs, clinical trial agents, diversified libraries, and natural products.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2018 ( Subtotal = $0 )
2018	2017	REACTION BIOLOGY CORPORATION	1 GREAT VALLEY PKWY STE 2	MALVERN	PA	19355	CHESTER	USA	National Center for Advancing Translational Sciences	000	3	9/7/2018	NON-COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2017 ( Subtotal = $764,740 )
2017	2017	REACTION BIOLOGY CORPORATION	1 GREAT VALLEY PKWY STE 2	MALVERN	PA	19355	CHESTER	USA	National Center for Advancing Translational Sciences	000	3	4/4/2017	NON-COMPETING CONTINUATION	$764,740
														Subtotal = $764,740

Issue Date FY: 2016 ( Subtotal = $696,840 )
2016	2016	REACTION BIOLOGY CORPORATION	1764 LITCHFIELD TURNPIKE, 203	WOODBRIDGE	CT	06525	SOUTH CENTRAL CT	USA	National Center for Advancing Translational Sciences	000	2	3/22/2016	COMPETING CONTINUATION	$696,840
														Subtotal = $696,840

Grand Total All Awards = $1,461,580

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Epigenetic Probes for HMTs

Award Number: R44TR000940

ORGANIZATION: NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 06/20/2014

PERIOD OF PERFORMANCE END DATE: 03/31/2018

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