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1. (WO2016057306) RHO ASSOCIATED KINASE (ROCK) INHIBITORS AND THEIR USE IN TREATING DISEASE

Pub. No.:    WO/2016/057306    International Application No.:    PCT/US2015/053503
Publication Date: Fri Apr 15 01:59:59 CEST 2016 International Filing Date: Fri Oct 02 01:59:59 CEST 2015
IPC: A61K 38/00
C07K 2/00
C07K 4/00
C07K 5/00
C07K 7/00
C07K 14/00
C07K 17/00
Applicants: UNIVERSITY OF HOUSTON SYSTEM
Inventors: SCHWARTZ, Robert, J.
ZHANG, Hua
CRAFT, John, W.
GILBERTSON, Scott
MACKENZIE, Kevin
ABBASGHOLIZADEH, Reza
BARK, Steven
BRIGGS, James, M.
FOX, Robert
Title: RHO ASSOCIATED KINASE (ROCK) INHIBITORS AND THEIR USE IN TREATING DISEASE
Abstract:
The present disclosure describes peptide inhibitors of Rho-associtated-kinase (ROCK) and their use in treating disorders including heart failure, the leading cause of combined morbidity and mortality in the United States. An inhibitory polypeptide blocks ROCK1 activity in the presence of 1 mM ATP. The binding epitope on ROCK1 was mapped using chemical cross-linking to the Activation Loop, a novel locus identifying a new class of inhibitory drugs. The peptides described will be useful against a number of important diseases such as heart disease, pulmonary hypertension, arterial hypertension, gluacoma management, insulin resistance, kidney disease, hemolytic anemia, stroke, ischemia reperfusion injury, or acute mycloid leukemia.