University of Texas System

Massachusetts Institute of Technology

Chinese Academy of Sciences

University of Houston System

Rolf A Brekken

Philip E Thorpe

Sophia Ran

Thomas Kodadek

D Gomika Udugamasooriya

Ke Ding

Zhengchao Tu

Xiaomei Ren

Damith Gomika Udugamasooriya

Zhen Wang

Thomas M Wilkie

Kristina Y Aguilera

A phosphatidylserine targeted peptoid has been identified with the ability to bind to cancer cells globally and specifically. A dimer of the peptoid decreases cancer cell viability. Use of the dimerized peptoid enhances the efficacy of docetaxel. The peptoid can be used for including but not limited to diagnosing and treating cancer, diagnosing and treating a viral condition, and diagnosing and treating diabetes.

Cancer specific lipid targeted peptidomimetics

Compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in effectively inhibiting the enzymatic activity of discoidin domain receptor 1 and can be used as new therapeutic agents for preventing and treating e.g. inflammation, liver fibrosis, kidney fibrosis, lung fibrosis, skin scar, atherosclerosis, and cancer. The compound of formula I is: wherein the variables are as defined herein. 

Small-molecule inhibitors targeting discoidin domain receptor 1 and uses thereof

The present disclosure relates to methods for screening compounds for treating pancreatic ductal adenocarcinoma (PDA) using a mouse model with an Rgs16::GFP reporter. Also described are combination therapies for treating pancreatic ductal adenocarcinoma (PDA) using taxanes, gemcitabine and an Axl kinase inhibitor.

Screen and use of therapeutics for pancreatic ductal adenocarcinoma

A cell-based screen is reported can be used to identify specific receptor-binding compounds in a combinatorial library of peptoids (N-alkylglycine oligomers) displayed on beads. This strategy was applied to the isolation of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2)-binding peptoids, which were optimized to create lead compounds with high affinity for VEGFR2. One of these peptoids was shown to be an antagonist of VEGF-VEGFR2 interaction and receptor function.

High affinity VEGF-receptor antagonists

Disclosed is the surprising discovery that aminophospholipids, such as phosphatidylserine and phosphatidylethanolamine, are specific, accessible and stable markers of the luminal surface of tumor blood vessels. The present invention thus provides aminophospholipid-targeted diagnostic and therapeutic constructs for use in tumor intervention. Antibody-therapeutic agent conjugates and constructs that bind to aminophospholipids are particularly provided, as are methods of specifically delivering therapeutic agents, including toxins and coagulants, to the stably-expressed aminophospholipids of tumor blood vessels, thereby inducing thrombosis, necrosis and tumor regression.

Cancer treatment kits comprising therapeutic antibody conjugates that bind to aminophospholipids

Disclosed is the surprising discovery that aminophospholipids, such as phosphatidyserine and phosphatidylethanolamine, are specific, accessible and stable markers of the luminal surface of tumor blood vessels. The present invention thus provides aminophospholipid-targeted diagnostic and therapeutic constructs for use in tumor intervention. Antibody-therapeutic agent conjugates and constructs that bind to aminophospholipids are particularly provided, as are methods of specifically delivering therapeutic agents, including toxins and coagulants, to the stably-expressed aminophospholipids of tumor blood vessels, thereby inducing thrombosis, necrosis and tumor regression.

Targeting and imaging tumor vasculature using conjugates that bind to aminophospholipids

Methods for imaging tumor vasculature using conjugates that bind to aminophospholipids

Cancer treatment kits comprising therapeutic conjugates that bind to aminophospholipids

Disclosed are antibodies that specifically inhibit VEGF binding to only one (VEGFR2) of the two VEGF receptors. The antibodies effectively inhibit angiogenesis and induce tumor regression, and yet have improved safety due to their specificity. The present invention thus provides new antibody-based compositions, methods and combined protocols for treating cancer and other angiogenic diseases. Advantageous immunoconjugate and prodrug compositions and methods using the new VEGF-specific antibodies are also provided.

Antibody methods for selectively inhibiting VEGF

Antibody kits for selectively inhibiting VEGF

Cancer treatment compositions comprising therapeutic conjugates that bind to aminophospholipids

Combined cancer treatment methods using therapeutic conjugates that bind to aminophospholipids

Disclosed are antibodies that specifically inhibit VEGF binding to only one (VEGFR2) of the two VEGF receptors. The antibodies effectively inhibit angiogenesis and induce tumor regression, and yet have improved safety due to their specificity. The present invention thus provides new antibody-based compositions, methods and combined protocols for treating cancer and other angiogenic diseases. Advantageous immunoconjugate and prodrug compositions.

Growing community of inventors

Seattle, WA, United States of America

Rolf A Brekken