Targeting the C481S Ibrutinib-Resistance Mutation in Bruton’s Tyrosine Kinase Using PROTAC-Mediated Degradation-Reference-Cited by-同舟云学术

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton’s Tyrosine Kinase Using PROTAC-Mediated Degradation

Published:2018-05-31 Issue:26 Volume:57 Page:3564-3575
ISSN:0006-2960
Container-title:Biochemistry
language:en
Short-container-title:Biochemistry

Author:

Buhimschi Alexandru D.¹,Armstrong Haley A.²,Toure Momar¹,Jaime-Figueroa Saul¹,Chen Timothy L.³,Lehman Amy M.⁴,Woyach Jennifer A.²³,Johnson Amy J.³,Byrd John C.²³,Crews Craig M.¹⁵⁶^ORCID

Affiliation:

1. Department of Molecular, Cellular, and Developmental Biology, Yale University, New Haven, Connecticut 06511, United States

2. Division of Pharmaceutics & Pharmaceutical Chemistry, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States

3. Department of Internal Medicine, Division of Hematology, The Ohio State University, Columbus, Ohio 43210, United States

4. Center for Biostatistics, The Ohio State University, Columbus, Ohio 43210, United States

5. Department of Chemistry, Yale University, New Haven, Connecticut 06520-8107, United States

6. Department of Pharmacology, Yale University, New Haven, Connecticut 06520-8066, United States

Funder

National Cancer Institute

Arvinas, Inc.

Publisher

American Chemical Society (ACS)

Subject

Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.biochem.8b00391

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4. Inactivation of PI3Kγ and PI3Kδ distorts T-cell development and causes multiple organ inflammation

5. Bruton’s tyrosine kinase (BTK) function is important to the development and expansion of chronic lymphocytic leukemia (CLL)

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