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Development of phosphorylation editing chimeras using kinase inhibitors

Award Number: R21AI178690
ORGANIZATION: NATIONAL INSTITUTE OF ALLERGY & INFECTIOUS DISEASES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 06/17/2024
PERIOD OF PERFORMANCE END DATE: 04/30/2026

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Development of phosphorylation editing chimeras using kinase inhibitors - PROJECT SUMMARY Protein post-translational modifications (PTMs) can activate, inhibit, or modify protein’s function. Small molecules that inhibit enzymes that induce PTMs (e.g., kinases for phosphorylation) are available in abundance, but methods to induce a given PTM of any protein on demand are challenging to develop. We propose to develop a new class of small molecules which will induce protein phosphorylation by using a kinase inhibitor to recruit the given kinase to phosphorylate a neo-substrate. These molecules will be formed by joining a small-molecule kinase inhibitor with a small-molecule binder of the target protein so that an active kinase is brought into proximity to the target protein to initiate phosphorylation. 1


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: 2025 ( Subtotal = $210,000 )
2025	2025	THE BROAD INSTITUTE, INC	415 MAIN ST	CAMBRIDGE	MA	02142	MIDDLESEX	USA	Allergy and Infectious Diseases Research	000	2	5/16/2025	NON-COMPETING CONTINUATION	$210,000
														Subtotal = $210,000

Issue Date FY: 2024 ( Subtotal = $252,000 )
2024	2024	THE BROAD INSTITUTE, INC	415 MAIN ST	CAMBRIDGE	MA	02142	MIDDLESEX	USA	Allergy and Infectious Diseases Research	001	1	9/11/2024	NEW	$25,200
2024	2024	THE BROAD INSTITUTE, INC	415 MAIN ST	CAMBRIDGE	MA	02142	MIDDLESEX	USA	Allergy and Infectious Diseases Research	000	1	6/17/2024	NEW	$226,800
														Subtotal = $252,000

Grand Total All Awards = $462,000

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Development of phosphorylation editing chimeras using kinase inhibitors

Award Number: R21AI178690

ORGANIZATION: NATIONAL INSTITUTE OF ALLERGY & INFECTIOUS DISEASES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

PERIOD OF PERFORMANCE START DATE: 06/17/2024

PERIOD OF PERFORMANCE END DATE: 04/30/2026

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