6-Ethynylthieno[3,2-d]- and 6-ethynyithieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases

Analysis of the x-ray crystal structure of mono-substituted acetylenic thienopyrimidine 6 complexed with the ErbB family enzyme ErbB-4 revealed a covalent bond between the terminal carbon of the acetylene moiety and the sulfhydryl group of Cys-803 at the solvent interface. The identification of this...

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Veröffentlicht in:	Proceedings of the National Academy of Sciences - PNAS 2008-02, Vol.105 (8), p.2773
Hauptverfasser:	Wood, Edgar R, Shewchuk, Lisa M, Ellis, Byron, Brignola, Perry, Brashear, Ronald L, Caferro, Thomas R, Dickerson, Scott H, Dickson, Hamilton D, Donaldson, Kelly H, Gaul, Michael, Griffin, Robert J, Hassell, Anne M, Keith, Barry, Mullin, Robert, Petrov, Kimberly G, Reno, Michael J, Rusnak, David W, Tadepalli, Sarva M, Ulrich, John C, Wagner, Craig D, Vanderwall, Dana E, Waterson, Alex G, Williams, Jon D, White, Wendy L, Uehling, David E
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine triphosphatase Chemical compounds Enzymes Kinases Molecular structure
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