[HTML][HTML] Rational design and synthesis of a novel anti-leukemic agent targeting Bruton′ s tyrosine kinase (BTK), LFM-A13 [α-cyano-β-hydroxy-β-methyl-N-(2, 5 …
S Mahajan, S Ghosh, EA Sudbeck, Y Zheng… - Journal of Biological …, 1999 - ASBMB
In a systematic effort to design potent inhibitors of the anti-apoptotic tyrosine kinase BTK
(Bruton′ s tyrosine kinase) as anti-leukemic agents with apoptosis-promoting and
chemosensitizing properties, we have constructed a three-dimensional homology model of
the BTK kinase domain. Our modeling studies revealed a distinct rectangular binding pocket
near the hinge region of the BTK kinase domain with Leu 460, Tyr 476, Arg 525, and Asp
539 residues occupying the corners of the rectangle. The dimensions of this rectangle are …
(Bruton′ s tyrosine kinase) as anti-leukemic agents with apoptosis-promoting and
chemosensitizing properties, we have constructed a three-dimensional homology model of
the BTK kinase domain. Our modeling studies revealed a distinct rectangular binding pocket
near the hinge region of the BTK kinase domain with Leu 460, Tyr 476, Arg 525, and Asp
539 residues occupying the corners of the rectangle. The dimensions of this rectangle are …