Person:

Yang, Guang

BTK is a member of the TEC family of non-receptor tyrosine kinases whose deregulation has been implicated in a variety of B-cell-related diseases. We have used structure-based drug design in conjunction with kinome profiling and cellular assays to develop a potent, selective, and irreversible BTK kinase inhibitor, QL47, which covalently modifies Cys481. QL47 inhibits BTK kinase activity with an IC50 of 7 nM, inhibits autophosphorylation of BTK on Tyr223 in cells with an EC50 of 475 nM, and inhibits phosphorylation of a downstream effector PLCγ2 (Tyr759) with an EC50 of 318 nM. In Ramos cells QL47 induces a G1 cell cycle arrest that is associated with pronounced degradation of BTK protein. QL47 inhibits the proliferation of B-cell lymphoma cancer cell lines at submicromolar concentrations.

Economies in Africa, and especially Sub-Saharan Africa, have been growing more rapidly in recent years than at any time in modern history. Between 2001 and 2008, African economies grew at an increasing rate, averaging over 6% for the period. In 2010 the average economic growth rate across the continent overtook both Brazil and India." This rate of growth and development is unprecedented in recent history and has the potential for lifting millions across the continent out of poverty and moving communities and nations towards self-sustained livelihoods and economies.