Georgetown University

Other

University of Michigan

Biogen Ma Inc.

Istvan J Enyedy

Shaomeng Wang

Dajun Yang

Chen-Yong Lin

Robert B Dickson

Michael D Johnson

Zhili Xin

Edward Yin-Shiang Lin

Brian Stuart Lucas

John Howard Jones

Leonard A Smith

TeYu Chen

Kurt D Van Vloten

Andrew George Capacci

Virginia I Roxas-Duncan

Nizamettin Gul

John H Cardellina, Ii

Sheau-Ling Lee

Rebecca C Vieira

Susan M Ensel

David C H Yang

Sivanesan Dakshanamurthy

Salimuddin Shah

Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.

NRF2 activator

The invention provides potent quinolinol-based BoNT/A small-molecule inhibitors of botulinum neurotoxins, in particular ofserotype A neurotoxins. The invention also provides methods of using these small-molecule inhibitors to inhibit infections by, as well as, methods of preventing infections bythrough materials that may be ingested.

Small molecule inhibitors of botulinum neurotoxins

The invention is directed to a method of detecting a malignancy or a pre-malignant lesion in breast or other tissue, or a pathologic condition, by detecting the presence of single-chain or two-chain forms of matriptase in the tissue. The invention is further directed to a method of treating malignancies, which have the phenotype of matriptase production by administering a tumor formation inhibiting effective amount of concentrate of Bowman-Birk inhibitor (BBIC), or other matriptase inhibitor. The invention also is directed to nucleic acids encoding a matriptase protein or fragments thereof, and their use for structure elucidation and modeling to identify other inhibitors of matriptase, as well as to methods of identifying matriptase modulating agents, including activators and inhibitors.

Matriptase, a serine protease and its applications

A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is exemplified is 'compound B17'=methyl-(p-nitrophenyl)-2-propynoate.

ErbB-2 selective small molecule kinase inhibitors

The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-X. 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-Xthat 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-X, 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.

Small molecule inhibitors targeted at Bcl-2

The present invention relates to a method of inhibiting carcinoma progression wherein matriptase plays a role in a subject in need of such inhibition including administering to a subject an effective amount of a compound comprising two positively charged groups, which are the same or different. The groups are linked by a chemical group having a length of between 5 and 30 A, and preferably between 15 and 24 A. Diagnostic methods based on matriptase action and therapeutic methods involving inhibition of matriptase activity are provided.

Structure based discovery of inhibitors of matriptase for the treatment of cancer and other conditions

Growing community of inventors

Hamden, CT, United States of America

Istvan J Enyedy