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IDENTIFYING ALLOSTERIC INHIBITORS OF CASPASES

Award Number: F32AR052602
ORGANIZATION: NATIONAL INSTITUTE OF ARTHRITIS & MUSCULOSKELETAL & SKIN DISEASES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: PLANNING
PERIOD OF PERFORMANCE START DATE: 05/01/2005
PERIOD OF PERFORMANCE END DATE: 04/30/2008

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IDENTIFYING ALLOSTERIC INHIBITORS OF CASPASES - DESCRIPTION (provided by applicant): The long-term goal of this research proposal is to validate allosteric inhibition as a general mechanism of regulation in caspases. The specific aims of the proposal are: 1) identify small molecule inhibitors of human caspase-1, 2) determine the mechanism of allosteric inhibition in caspase-1, and 3) identify natural regulators of caspases acting through the allosteric site. The studies are to include both caspase-1 and caspase-3. Caspases are specific proteases in animals that catalyze the hydrolysis of substrates involved in inflammation and apoptosis. Caspases are implicated in multiple human diseases including arthritis, psoriasis, inflammatory bowl disease, stroke (ischemia), myocardial infarction, sepsis, spinal cord injury, Alzheimer's disease and Parkinson's disease. Previously, only active site inhibitors of caspases have been identified, but show debilitating liabilities as effective therapeutics. An alternative approach is to design inhibitors to an allosteric site that may bypass the problems associated with active site inhibitors. This research will provide further insight into the cellular regulation of caspase activity in vivo and create opportunities to develop a novel class of caspase-targeted therapeutics.


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: 2006 ( Subtotal = $55,852 )
2006	2006	UNIVERSITY OF CALIFORNIA-SAN FRANCISCO	BOX 0812	SAN FRANCISCO	CA	94143	SAN FRANCISCO	USA	Arthritis, Musculoskeletal and Skin Diseases Research	000	3	4/24/2006	NON-COMPETING CONTINUATION	$55,852
														Subtotal = $55,852

Issue Date FY: 2005 ( Subtotal = $53,492 )
2005	2005	SUNESIS PHARMACEUTICALS	3696 HAVEN AVENUE SUITE C	REDWOOD CITY	CA	94063	SAN MATEO	USA	Arthritis, Musculoskeletal and Skin Diseases Research	000	1	4/3/2005	NEW	$53,492
														Subtotal = $53,492

Grand Total All Awards = $109,344

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IDENTIFYING ALLOSTERIC INHIBITORS OF CASPASES

Award Number: F32AR052602

ORGANIZATION: NATIONAL INSTITUTE OF ARTHRITIS & MUSCULOSKELETAL & SKIN DISEASES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: PLANNING

PERIOD OF PERFORMANCE START DATE: 05/01/2005

PERIOD OF PERFORMANCE END DATE: 04/30/2008

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