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DEVELOPMENT OF CONFORMATION SPECIFIC KINASE INHIBITORS

Award Number: R44CA099214
ORGANIZATION: NATIONAL CANCER INSTITUTE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 02/01/2003
PERIOD OF PERFORMANCE END DATE: 08/31/2006

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DEVELOPMENT OF CONFORMATION SPECIFIC KINASE INHIBITORS - DESCRIPTION (provided by applicant): The long-term objective of this proposal is to apply TetheringSM fragment-based drug discovery to obtain novel therapeutics for the treatment of cancer. Conformation-specific inhibitors of the kinase MEK1 provide a new class of cancer therapeutics that broadly target cancer cells at the molecular level yet are not generally cytotoxic. TetheringSM allows a greater survey of chemical diversity space than is achievable using the large compound libraries typically screened by pharmaceutical firms. TetheringSM with extenders, a variation of this approach, was used to identify high potency MEK1 inhibitors (IC50's < 0.3 microM) during Phase I. TetheringSM with extenders is particularly powerful for target classes like kinases that contain an active site that is highly conserved in one region yet significantly divergent in adjacent regions. Moreover_ this approach provides not only an efficient means of ligand discovery but also a direct path to lead optimization since the target protein is used as a template for the construction of its own inhibitor. This Phase II proposal proposes to carry forward the potent MEKI inhibitors identified in Phase I starting with 2-3 chemically distinct early lead series and ending with a clinical candidate compound for IND enabling studies.


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: 2005 ( Subtotal = $750,000 )
2005	2005	SUNESIS PHARMACEUTICALS	3696 HAVEN AVENUE SUITE C	REDWOOD CITY	CA	94063	SAN MATEO	USA	Cancer Treatment Research	000	3	9/15/2005	NON-COMPETING CONTINUATION	$750,000
														Subtotal = $750,000

Issue Date FY: 2004 ( Subtotal = $750,000 )
2004	2004	SUNESIS PHARMACEUTICALS	3696 HAVEN AVENUE SUITE C	REDWOOD CITY	CA	94063	SAN MATEO	USA	Cancer Treatment Research	000	2	9/21/2004	COMPETING CONTINUATION	$750,000
														Subtotal = $750,000

Grand Total All Awards = $1,500,000

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DEVELOPMENT OF CONFORMATION SPECIFIC KINASE INHIBITORS

Award Number: R44CA099214

ORGANIZATION: NATIONAL CANCER INSTITUTE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

PERIOD OF PERFORMANCE START DATE: 02/01/2003

PERIOD OF PERFORMANCE END DATE: 08/31/2006

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