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Biotech / Medical : Biotech Valuation -- Ignore unavailable to you. Want to Upgrade?

To: Biomaven who wrote (8314)	6/10/2003 5:00:36 AM
From: nigel bates	Respond to of 52153

A logical approach to producing more Gleevec-type drugs: ...."Two of the major questions to be addressed by our laboratories are the functional consequences of the mutations we are finding, and whether these kinases are targets for drugs... A method for probing those targets ? United States Patent Application 20020146797 Kind Code A1 Shokat, Kevan M. October 10, 2002 ------------------------------------------------------------------------ Engineered protein kinases which can utilize modified nucleotide triphosphate substrates Abstract The invention relates to methods for designing inhibitors of serine/theronine kinases and tyrosine kinases, particularly MAP kinases, through the use of ATP-binding site mutants of those kinases. The methods of this invention take advantage of the fact that the mutant kinases are capable of binding inhibitory compounds of other kinases with greater affinity than the corresponding wild-type kinase. The invention further relates to the mutant kinases themselves and crystallizable co-complexes of the mutant kinase and the inhibitory compound. ------------------------------------------------------------------------ Inventors: Shokat, Kevan M.; (San Francisco, CA) Correspondence Name and Address: MORGAN LEWIS & BOCKIUS LLP 1111 PENNSYLVANIA AVENUE NW WASHINGTON DC 20004 US Assignee Name and Adress: Princeton University. Serial No.: 985157 Series Code: 09 Filed: November 1, 2001 U.S. Current Class: 435/194; 435/320.1; 435/325; 435/69.1; 536/23.2 U.S. Class at Publication: 435/194; 435/69.1; 435/325; 435/320.1; 536/23.2 Intern'l Class: C12N 009/12; C07H 021/04 ------------------------------------------------------------------------ Goverment Interests ------------------------------------------------------------------------ [0001] The U.S. Government has a paid-up license in this invention and the right in limited circumstances to require the patent owner to license others, as provided for by the terms of NSF Grant No. MCB9506929 and DHHS NCI Grant No. RO1 CA7033 1-01.... United States Patent Application 20030073218 Kind Code A1 Shokat, Kevan M. April 17, 2003 ------------------------------------------------------------------------ High affinity inhibitors for target validation and uses thereof Abstract This invention provides general methods for discovering mutant inhibitors for any class of enzymes as well as the specific inhibitors so identified. More specifically, this invention provides general methods for discovering specific inhibitors for multi-substrate enzymes. Examples of such multi-substrate enzymes include, but are not limited to, kinases and transferases. The mutant inhibitors identified by the methods of this invention can be used to highly selectively disrupt cell functions such as oncogenic transformation. In one particular example, this invention provides a Src protein kinase inhibitor, pharmaceutical compositions thereof and methods of disrupting transformation in a cell that expresses the target v-scr comprising contacting the cell with the protein kinase inhibitor. ------------------------------------------------------------------------ Inventors: Shokat, Kevan M.; (San Francisco, CA) Correspondence Name and Address: MORGAN LEWIS & BOCKIUS LLP 1111 PENNSYLVANIA AVENUE NW WASHINGTON DC 20004 US Assignee Name and Adress: Princeton University Serial No.: 044967 Series Code: 10 Filed: May 29, 2002 U.S. Current Class: 435/184; 424/94.1 U.S. Class at Publication: 435/184; 424/94.1 Intern'l Class: A61K 038/43; C12N 009/99