Ontology highlight
ABSTRACT:
INSTRUMENT(S): Orbitrap Exploris 240
ORGANISM(S): Homo Sapiens (human)
TISSUE(S): Pancreatic Duct
DISEASE(S): Adenocarcinoma,Carcinoma
SUBMITTER: Ronen Gabizon
LAB HEAD: Nir London
PROVIDER: PXD038301 | Pride | 2023-03-11
REPOSITORIES: Pride
Action | DRS | |||
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Ram_Mino_1267_1.raw | Raw | |||
Ram_Mino_1267_2.raw | Raw | |||
Ram_Mino_1267_3.raw | Raw | |||
Ram_Mino_1267_4.raw | Raw | |||
Ram_Mino_Ibrutinib_1.raw | Raw |
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Journal of the American Chemical Society 20230204 6
Electrophiles for covalent inhibitors that are suitable for in vivo administration are rare. While acrylamides are prevalent in FDA-approved covalent drugs, chloroacetamides are considered too reactive for such purposes. We report sulfamate-based electrophiles that maintain chloroacetamide-like geometry with tunable reactivity. In the context of the BTK inhibitor ibrutinib, sulfamate analogues showed low reactivity with comparable potency in protein labeling, in vitro, and cellular kinase activi ...[more]