University of Michigan

Denzil Bernard

Shaomeng Wang

Hacer Karatas

Yali Dou

Elizabeth Townsend

Liu Liu

Angelo Aguilar

Jianfeng Lu

Liyue Huang

Haibin Zhou

Shilin Xu

Yi Sun

Tianfeng Xu

Ke Zheng

Fang Cao

Ke Zhang

Compounds of formula (I) as inhibitors of DCN1 and compositions containing the same are disclosed. Methods of using the DCN1 inhibitors in the treatment of diseases and conditions wherein inhibition of DCN1 provides a benefit, like oxidative stress-related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

Small molecule DCN1 inhibitors and therapeutic methods using the same

The present disclosure provides compounds by Formula (I): (Formula (I)) and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R, R, R, A, G, X, and Y are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat a condition or disorder responsive to menin inhibition such as cancer. 

Piperidines as menin inhibitors

Peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed.

Inhibition of WDR5 interaction with its binding partners

Cyclic peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed.

Cyclized peptidomimetic small molecule inhibitors of the WDR5 and MLL1 interaction

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Ann Arbor, MI, United States of America

Denzil Bernard