Noncovalent inhibition of C481S Bruton tyrosine kinase by GDC-0853: a new treatment strategy for ibrutinib-resistant CLL-Reference-Cited by-同舟云学术

Noncovalent inhibition of C481S Bruton tyrosine kinase by GDC-0853: a new treatment strategy for ibrutinib-resistant CLL

Published:2018-09-06 Issue:10 Volume:132 Page:1039-1049
ISSN:0006-4971
Container-title:Blood
language:en
Short-container-title:

Author:

Reiff Sean D.¹²,Muhowski Elizabeth M.¹³,Guinn Daphne¹,Lehman Amy⁴,Fabian Catherine A.¹,Cheney Carolyn¹,Mantel Rose¹,Smith Lisa¹,Johnson Amy J.¹³,Young Wendy B.⁵,Johnson Adam R.⁵,Liu Lichuan⁵,Byrd John C.¹⁴,Woyach Jennifer A.¹⁴

Affiliation:

1. Division of Hematology, Department of Internal Medicine, Comprehensive Cancer Center,

2. Medical Scientist Training Program,

3. Division of Pharmaceutics, College of Pharmacy, and

4. Center for Biostatistics, The Ohio State University, Columbus, OH; and

5. Research and Early Development, Genentech Inc., South San Francisco, CA

Abstract

Key Points Inhibition of the ibrutinib-resistant C481S BTK mutant can be achieved by the reversible BTK inhibitor GDC-0853. BTK inhibitors, which lack ITK inhibition, preserve natural killer cell–mediated cellular cytotoxicity to CD20 directed monoclonal antibodies.

Publisher

American Society of Hematology

Subject

Cell Biology,Hematology,Immunology,Biochemistry

Link

http://ashpublications.org/blood/article-pdf/132/10/1039/1406542/blood809020.pdf

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