Rutgers, the State University of New Jersey

The Broad Institute, Inc.

Longqin Hu

Amrik Sahota

Herve Aloysius

Timothy A Lewis

Haifa Albanyan

Daigo Inoyama

Sadagopan Magesh

Lin Chen

Dhulfiqar A Abed

Ben Munoz

Lili Wang

This document discloses novel cystine analogs, methods of making cystine analogs, compositions containing cystine analogs and methods of using such analogs for inhibiting cystine stone formation and treatment of cystinuria.

Cystine diamide analogs for cystinuria

Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein

Cystine diamide analogs for the prevention of cystine stone formation in cystinuria

This patent document discloses novel compounds and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds. As direct inhibitors of Keap1-Nrf2 interaction, the compounds disclosed herein are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential dmg candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, Parkinson's, and inflammatory bowel disease including ulcerative colitis.

Small molecule direct inhibitors of KEAP1-NRF2 protein-protein interaction

The present disclosure is directed to a series of target-selective chemotherapeutic ester prodrugs comprising PSA-cleavable peptides that promote the delivery of free doxorubicin and other chemotherapeutic agents into the prostate and/or prostate tumors with greater efficiency.

Peptide linker and combination for prodrugs activated by prostate-specific antigen

Peptide-linked ester prodrugs activated by prostate-specific antigen

A method of identifying compounds as direct inhibitors of Keap1-Nrf2 interaction through high-throughput screening and lead development. The direct inhibitors of Keap1-Nrf2 interaction are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential drug candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, and Parkinson's. Novel compounds are identified and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds identified or compositions containing such compounds are also disclosed.

Direct inhibitors of Keap1-Nrf2 interaction as antioxidant inflammation modulators

Disclosed are methods and kits for identifying modulators of the Keap1-Nrf2-ARE pathway. In particular, a high throughput fluorescent polarization assay is described that identifies small molecules that inhibit the binding of a fluorescently labeled Nrf2 peptide with the kelch domain of the Keap1 protein. Also provided are probes that can be used in the described fluorescent polarization assay. The small molecules identified using the described assay are useful for combating oxidative stress-related disorders, such as those associated with cancer, emphysema, Huntington's disease, light-induced retinal damage, and stroke.

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Belle Mead, NJ, United States of America

Longqin Hu