Prolonged and tunable residence time using reversible covalent kinase inhibitors

Nature Chemical Biology

Volumn 11, Issue 7, 2015, Pages 525-531

  Bradshaw, J Michael ^a   McFarland, Jesse M ^b   Paavilainen, Ville O ^b   Bisconte, Angelina ^a   Tam, Danny ^a   Phan, Vernon T ^a   Romanov, Sergei ^c   Finkle, David ^a   Shu, Jin ^a   Patel, Vaishali ^a   Ton, Tony ^a   Li, Xiaoyan ^a   Loughhead, David G ^a   Nunn, Philip A ^a   Karr, Dane E ^a   Gerritsen, Mary E ^a   Funk, Jens Oliver ^a   Owens, Timothy D ^a   Verner, Erik ^a   Brameld, Ken A ^a   Hill, Ronald J ^a   Goldstein, David M ^a   Taunton, Jack ^b   more..

^a Principia Biopharma   (United States)

^b HOWARD HUGHES MEDICAL INSTITUTE   (United States)

^c Nanosyn Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACRYLAMIDE DERIVATIVE; BRUTON TYROSINE KINASE; BRUTON TYROSINE KINASE INHIBITOR; CYSTEINE; ELECTROPHILE; FIBROBLAST GROWTH FACTOR RECEPTOR 1; INFIGRATINIB; PHOSPHOTRANSFERASE INHIBITOR; AGAMMAGLOBULINAEMIA TYROSINE KINASE; CYANOACRYLATE DERIVATIVE; DASATINIB; LIGAND; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE; PYRIMIDINE DERIVATIVE; RECOMBINANT PROTEIN; THIAZOLE DERIVATIVE;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; COVALENT BOND; DRUG CLEARANCE; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; FEMALE; HUMAN; HUMAN CELL; IN VIVO STUDY; MEAN RESIDENCE TIME; NONHUMAN; PRIORITY JOURNAL; RAT; ANIMAL; ANTAGONISTS AND INHIBITORS; B LYMPHOCYTE; CHEMISTRY; DRUG EFFECTS; ENZYME SPECIFICITY; ENZYMOLOGY; GENE EXPRESSION; GENETICS; MOLECULAR DOCKING; PATHOLOGY; PROTEIN TERTIARY STRUCTURE; SF9 CELL LINE; SPODOPTERA; SPRAGUE DAWLEY RAT; STRUCTURE ACTIVITY RELATION; SYNTHESIS; TIME FACTOR; TUMOR CELL LINE; X RAY CRYSTALLOGRAPHY;

ACRYLAMIDES; ANIMALS; B-LYMPHOCYTES; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; CYANOACRYLATES; DASATINIB; FEMALE; GENE EXPRESSION; HUMANS; LIGANDS; MOLECULAR DOCKING SIMULATION; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; PROTEIN-TYROSINE KINASES; PYRIMIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECOMBINANT PROTEINS; SF9 CELLS; SPODOPTERA; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; THIAZOLES; TIME FACTORS;

EID: 84931572829     PISSN: 15524450     EISSN: 15524469     Source Type: Journal    
DOI: 10.1038/nchembio.1817     Document Type: Article

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