Invention Grant
- Patent Title: Small molecule inhibitors targeted at Bcl-2
- Patent Title (中): 针对Bcl-2的小分子抑制剂
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Application No.: US10286085Application Date: 2002-11-01
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Publication No.: US07354928B2Publication Date: 2008-04-08
- Inventor: Shaomeng Wang , Dajun Yang , Istvan J. Enyedy
- Applicant: Shaomeng Wang , Dajun Yang , Istvan J. Enyedy
- Applicant Address: US MI Ann Arbor
- Assignee: The Regents of the University of Michigan
- Current Assignee: The Regents of the University of Michigan
- Current Assignee Address: US MI Ann Arbor
- Agent Casimir Jones, S.C.
- Main IPC: A61K31/44
- IPC: A61K31/44 ; A61K31/335 ; A61K31/135 ; A61K31/505 ; A61K31/65
Abstract:
The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.
Public/Granted literature
- US20030199489A1 Small molecule inhibitors targeted at BCL-2 Public/Granted day:2003-10-23
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