Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model-Reference-Cited by-同舟云学术

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Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model

Published:2024-05-15 Issue:11 Volume:67 Page:8708-8729
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Braun Marie-Gabrielle¹^ORCID,Ashkenazi Avi¹,Beveridge Ramsay E.²,Castanedo Georgette¹,Wallweber Heidi Ackerly¹,Beresini Maureen H.¹,Clark Kevin R.¹,De Bruyn Tom¹^ORCID,Fu Liqiang³,Gibbons Paul¹,Jiang Fan⁴,Kaufman Susan¹,Kan David¹,Kiefer James R.¹,Leclerc Jean-Philippe²,Lemire Alexandre²,Ly Cuong¹,Segal Ehud¹,Sims Jessica¹,Wang Weiru¹,Wei Wentao⁴,Zhao Liang²,Schwarz Jacob B.¹^ORCID,Rudolph Joachim¹^ORCID

Affiliation:

1. Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

2. Paraza Pharma Inc., 2525 Ave. Marie-Curie, Montreal, QC, Canada H4S 2E1

3. WuXi AppTec Co., Ltd., Shanghai 200131, P. R. China

4. VIVA Biotech, No. 735, Ziping Road, Pudong New Area, Shanghai 201321, China

Publisher

American Chemical Society (ACS)

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.3c02425

Reference24 articles.

1. The Unfolded Protein Response: From Stress Pathway to Homeostatic Regulation

2. Protein misfolding in the endoplasmic reticulum as a conduit to human disease

3. Integrating the mechanisms of apoptosis induced by endoplasmic reticulum stress

4. ER Stress Triggers Apoptosis by Activating BH3-Only Protein Bim

5. Opposing unfolded-protein-response signals converge on death receptor 5 to control apoptosis

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