Kinetic Optimization of Lysine-Targeting Covalent Inhibitors of HSP72
The covalent inhibition mechanism of action, which overcomes competition with high-affinity, high-abundance substrates of challenging protein targets, can deliver effective chemical probes and drugs. The success of this strategy has centered on exposed cy
Pettinger, Jonathan,Carter, Michael,Jones, Keith,Cheeseman, Matthew D.
Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design
The design and synthesis of novel adenosine-derived inhibitors of HSP70, guided by modeling and X-ray crystallographic structures of these compounds in complex with HSC70/BAG-1, is described. Examples exhibited submicromolar affinity for HSP70, were highl
Williamson, Douglas S.,Borgognoni, Jenifer,Clay, Alexandra,Daniels, Zoe,Dokurno, Pawel,Drysdale, Martin J.,Foloppe, Nicolas,Francis, Geraint L.,Graham, Christopher J.,Howes, Rob,Macias, Alba T.,Murray, James B.,Parsons, Rachel,Shaw, Terry,Surgenor, Allan E.,Terry, Lindsey,Wang, Yikang,Wood, Mike,Massey, Andrew J.
supporting information; experimental part
p. 1510 - 1513
(2009/12/25)
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