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Reimagining how we study biomolecules
He Y, Bae JSH, Nowak E, Outieral C, Nissley DA, Tumber A, Berridge G, Salah E, Wang Y, He W, Zhang H, Tusk S, Mathea S, Wang YJ, Grassam-Rowe A, Kukura P, Schofield CJ, O'Brien DP, Pierangelini A, Churchill GC, Lanyon-Hogg T, Ke Y, Xu Ch, Ye T, Watkins H, Ying L, Koschinski A, Solaro RJ, Tan X, Bolla JR, Wang X, Knapp S, Deane CM, Zaccolo M, Nowotny M, Lei M
Rational discovery of therapeutic PAK1 allosteric activators
31 Mar 2026
Kinase activators are difficult to develop despite their therapeutic promise. Here, we report the discovery of small-molecule p21-activated kinase 1 (PAK1) allosteric activators using a rational, peptideguided strategy targeting the autoinhibitory mechanism. These compounds exhibit therapeutic efficacy in hypertrophic cardiomyopathy, underscoring the potential of this strategy for therapeutic kinase activator discovery.
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