Calise Bahou , Richard Spears , Abil Aliev , Antoine Maruani , Marcos Fernandez , Faiza Javaid , Peter Szijj , James Baker and Vijay Chudasama
Chem. Commun. 2019
DOI: 10.1039/C9CC08362F
Herein we report a retro-Michael deconjugation pathway of thiol-pyridazinedione linked protein bioconjugates to provide a novel cleavable linker technology. We demonstrate that the novel pyridazinedione linker does not suffer from off-target modification with blood thiols (e.g. glutathione, human serum albumin (HSA)), which is in sharp contrast to an analogous maleimide linker.
A blog highlighting recent publications in the area of covalent modification of proteins, particularly relating to covalent-modifier drugs. @CovalentMod on Twitter, @covalentmod@mstdn.science on Mastodon, and @covalentmod.bsky.social on BlueSky
Fragment-Based Covalent Targeting of Lysines at the Allosteric Latch Site of SHP2.
Vincenzo Di Lorenzo , Noémi Csorba , Renáta Szabó , Levente Kollár , Yvette Roske , Ivan Rand̵elović , Krisztina Balázs , Tibor Vikt...
-
Xu-liang Xu, Ti-ti Ying, Xiao-wen Wu, Yun-jun Chen, Gang-ao Hu, Yu-tian Guan, Shi-yi Liu, He Wang, Mohamed Seif, Mahmoud Emam, Hong Wang, We...
-
Joseph E Klebba, Nilotpal Roy, Steffen M Bernard, Stephanie Grabow, Melissa A. Hoffman, Hui Miao, Junko Tamiya, Jinwei Wang, Cynthia Berry, ...
-
Stephanie A. Moquin, Suresh B. Lakshminarayana, Kamal Kumar Balavenkatraman, Hilmar Schiller, Allison Claas, Barun Bhhatarai, Ioannis Loisio...