Activity-based profiling of primary brain cells identifies covalent allosteric modulators of HCN channels
Elva Ye, Alberto Russo, Roberta Castelli…·Benjamin F. Cravatt
Author
Vividion Therapeutics (United States)ORCID 0009-0000-9403-7178Unclaimed ORCID profile · follow to get notified of new preprints
7 papers
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Elva Ye, Alberto Russo, Roberta Castelli…·Benjamin F. Cravatt
Yijun Xiong, Christopher J. Reinhardt, Tracey Nguyen…·Benjamin F. Cravatt
The paper compares acrylamide and butynamide stereoprobes to identify covalent inhibitors of the actin maturation protease ACTMAP in human cancer cells.
John K. Neff, Kristen E. DeMeester, Paola K. Párraga Solórzano…·Michael U. Shiloh
The paper identifies host proteins regulating Mycobacterium tuberculosis replication in macrophages using cysteine reactivity profiling and genetic perturbation.
F. Wieland Goetzke, Steffen M. Bernard, Cheng‐Wei Ju…·Benjamin F. Cravatt
The paper develops covalent ligands that specifically target a complexoform of TRMT112, revealing partner-specific functional effects through allosteric activation of METTL5.
Joseph E. Klebba, Nilotpal Roy, Steffen M. Bernard…·Matthew P. Patricelli
The paper develops covalent inhibitors targeting the RAS binding domain of PI3Kα, showing efficacy against RAS and HER2-driven tumors without affecting glucose homeostasis.
Haoxin Li, Tiantai Ma, Jarrett R. Remsberg…·Benjamin F. Cravatt
The paper uses base editing to assess the functional impact of cysteine mutations in cancer dependency genes, identifying essential and ligandable cysteines for drug development.
Zsófia I. László, Zsolt Lele, Miklós Zöldi…·István Katona
The paper identifies ABHD4 as a mediator of developmental anoikis that protects the prenatal brain from pathological insults by eliminating abnormally detached progenitor cells.