Prolynx LLC

University of California

Kosan Biosciences Incorporated

Bristol-myers Squibb Compnay

Aurigene Oncology Limited

Olema Pharmaceuticals, Inc.

Michelle R. Arkin

Susana Vacas

Brian R. Hearn

Peter Walter

Diego Acosta Alvear

Christopher G. Wilson

Carmela Sidrauski

Kean Hooi Ang

Mervyn Maze

Brian R Hearn

Daniel V Santi

Christopher G Wilson

Gary W Ashley

Adam Renslo

David C Myles

Michelle Arkin

Eric L Schneider

Punitha Vedantham

Steven D Dong

Susanta Samajdar

Chandregowda Venkateshappa

Shaun Fontaine

Kalisankar Bera

David Yeghikyan

Reena Chawla

Suraj Tatyasaheb Gore

Raymond A Ng

Adam R Renslo

Michelle R Arkin

Provided herein are releasable conjugates of inhibitors of DNA damage response suitable for use as therapeutic agents in the treatment of disease.

Conjugated inhibitors of DNA damage response

The present disclosure describes acylsulfonamide compounds of Formula (J), and pharmaceutically acceptable salts, compositions, methods, and uses thereof. Such compounds are believed to be therapeutically useful as KAT6A inhibitors particularly in the treatment and/or prevention of diseases and disorders mediated by KAT6A in a subject.

Acylsulfonamide KAT6A inhibitors

Provided are β-eliminative linkers suitable for the conjugation of small molecule, peptide, and protein and compounds comprising the linkers.

Conjugation linkers

Provided herein, inter alia, are compounds and methods useful for modulating the translational effects of eIF2&#x3b1; phosphorylation, the Integrated Stress Response (ISR), and the unfolded protein response (UPR); for treating diseases; for increasing protein production, and for improving long-term memory.

Modulators of the eIF2alpha pathway

Conjugates of carriers and hydrogels for controlling the biological half-life of somatostatin and its analogs are disclosed.

Conjugates of somatostatin analogues

Leptomycin-type compounds according to formula I wherein R, R, R, R, R, R, R, R, and m are as defined herein, exhibit anti-tumor activity.

Leptomycin compounds

A conjugate of an active agent and a targeting moiety having affinity for a target cell, in which the active agent has been modified by attachment of a cell membrane-impermeabilizing group so that, if the active agent so modified is cleaved from the conjugate in the blood plasma instead of inside the target cell, the cell membrane-impermeabilizing group prevents or limits entry of the modified active agent into cells, thus reducing its systemic or non-specific adverse effects, including toxicity.

Conjugates with reduced adverse systemic effects

Leptomycin-type compounds according to Formula I wherein R, R, R, R, R, R, R, R, and m are as defined herein, exhibit anti-tumor activity.

Growing community of inventors

Lafayette, CA, United States of America

Brian R Hearn