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BICOMBINATORIAL DISCOVERY OF SMALL MOLECULE TAGS

Award Number: F32GM065048
ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: FELLOWSHIP/SCHOLARSHIP/STUDENT LOANS
PERIOD OF PERFORMANCE START DATE: 05/01/2002
PERIOD OF PERFORMANCE END DATE: 04/30/2005

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BICOMBINATORIAL DISCOVERY OF SMALL MOLECULE TAGS - DESCRIPTION: (provided by applicant) Development of a novel bicombinatorial screen will allow isolation of small molecule compounds (about 180 daltons) that interact specifically with individual intracellular proteins. By screening a combinatorial library of compounds against a combinatorial library of protein targets the chance of discovering specific compound-protein pairs will be maximized. Typically a compound must interact with a protein very strongly in order to be specific. This screen will take advantage of tethering technology, which uses a secondary disulfide tether between the small molecule and a cysteine on the protein to stabilize interacting complexes. This allows specific binding even when the interaction energy is low, so the likelihood of finding interacting molecules is dramatically increased, and the compound library can be relatively small. The compounds can be rapidly converted to fluorescent tags to study protein localization, or to affinity compounds to isolate the protein they recognize alone and in complexes. These compounds will also be useful as novel lead compounds for drug discovery. In contrast to conventional drug screens which focus on a single protein target, the bicombinatorial screen should suggest both which chemical moities are the most effective in binding proteins, and which chemical constituents confer anti-specificity. It may also be able to suggest some unexploited families of proteins that would also be suitable as drug targets.


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: 2004 ( Subtotal = $47,828 )
2004	2004	SUNESIS PHARMACEUTICALS	3696 HAVEN AVENUE SUITE C	REDWOOD CITY	CA	94063	SAN MATEO	USA	Biomedical Research and Research Training	000	3	3/22/2004	NON-COMPETING CONTINUATION	$47,828
														Subtotal = $47,828

Issue Date FY: 2003 ( Subtotal = $45,320 )
2003	2003	SUNESIS PHARMACEUTICALS	3696 HAVEN AVENUE SUITE C	REDWOOD CITY	CA	94063	SAN MATEO	USA	Biomedical Research and Research Training	000	2	6/4/2003	NON-COMPETING CONTINUATION	$45,320
														Subtotal = $45,320

Issue Date FY: 2002 ( Subtotal = $37,220 )
2002	2002	SUNESIS PHARMACEUTICALS	3696 HAVEN AVENUE SUITE C	REDWOOD CITY	CA	94063	SAN MATEO	USA	Biomedical Research and Research Training	000	1	4/25/2002	NEW	$37,220
														Subtotal = $37,220

Grand Total All Awards = $130,368

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BICOMBINATORIAL DISCOVERY OF SMALL MOLECULE TAGS

Award Number: F32GM065048

ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: FELLOWSHIP/SCHOLARSHIP/STUDENT LOANS

PERIOD OF PERFORMANCE START DATE: 05/01/2002

PERIOD OF PERFORMANCE END DATE: 04/30/2005

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