A covalent BTK ternary complex compatible with targeted protein degradation
Bridging covalent ligand discovery with chimeric degrader design has emerged as a mechanism to target proteins that lack enzymatic activity or are intractable. Here, the authors use biochemical and cellular tools to deconvolute the role of covalent modification in targeted protein degradation using...
Main Authors: | James Schiemer, Andrew Maxwell, Reto Horst, Shenping Liu, Daniel P. Uccello, Kris Borzilleri, Nisha Rajamohan, Matthew F. Brown, Matthew F. Calabrese |
---|---|
Format: | Article |
Language: | English |
Published: |
Nature Portfolio
2023-03-01
|
Series: | Nature Communications |
Online Access: | https://doi.org/10.1038/s41467-023-36738-z |
Similar Items
-
Structure-Function Relationships of Covalent and Non-Covalent BTK Inhibitors
by: Rula Zain, et al.
Published: (2021-07-01) -
PB1912: BTK AND PLCG2 GENE MUTATIONS IN CHRONIC LYMPHOCYTIC LEUKEMIA PATIENTS WITH RESISTANCE TO COVALENT BTK INHIBITOR
by: Ekaterina Likold, et al.
Published: (2023-08-01) -
Non-Covalent BTK Inhibitors—The New BTKids on the Block for B-Cell Malignancies
by: Katharine L Lewis, et al.
Published: (2021-08-01) -
Discovery of a Novel Class of Covalent Dual Inhibitors Targeting the Protein Kinases BMX and BTK
by: Michael Forster, et al.
Published: (2020-12-01) -
P1239: BRUTON TYROSINE KINASE (BTK) PROTEIN DEGRADER BGB-16673 IS LESS APT TO CAUSE, AND ABLE TO OVERCOME VARIABLE BTK RESISTANCE MUTATIONS COMPARED TO OTHER BTK INHIBITORS (BTKI)
by: Xiaoyu Feng, et al.
Published: (2023-08-01)