Design of Aminobenzothiazole Inhibitors of Rho Kinases 1 and 2 by Using Protein Kinase A as a Structure Surrogate,ChemBioChem

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Design of Aminobenzothiazole Inhibitors of Rho Kinases 1 and 2 by Using Protein Kinase A as a Structure Surrogate
ChemBioChem ( IF 2.6 ) Pub Date : 2018-01-30 , DOI: 10.1002/cbic.201700547
Russell A. Judge ₁ , Anil Vasudevan ₁ , Victoria E. Scott ₁ , Gricelda H. Simler ₂ , Steve D. Pratt ₁ , Marian T. Namovic ₁ , C. Brent Putman ₁ , Ana Aguirre ₁ , Vincent S. Stoll ₁ , Mulugeta Mamo _{1,

3} , Steven I. Swann _{1,

4} , Steven C. Cassar ₁ , Connie R. Faltynek ₁ , Karen L. Kage _{1,

5} , Janel M. Boyce-Rustay _{1,

6} , Adrian D. Hobson ₂

Affiliation

Stop the ROCK: Protein kinase A was used as a protein structure surrogate to guide compound design for inhibitors of Rho kinases (ROCKs). A subset of molecules showed robust activity in a cell‐based myosin phosphatase assay and in a mechanical hyperalgesia in vivo pain model.