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Prebys Center

Apelin Receptor Research Program

One of the pathological hallmarks of diabetic retinopathy (DR)— the most common diabetic eye disease and a leading cause of blindness in the US—is the development of immature, fragile blood vessels on the retina. This process, called angiogenesis, isstimulated by pro-angiogenic molecules such as vascular endothelial growth factorand apelin.  Apelin is a newly discovered protein shown to play a critical role in thedevelopment of blood vessels.  Several lines of evidence suggest that blocking apelinin the eye would be a successful treatment for DR, which is what we are investigating in this research program.

 

Patents

PCT WO 2015184011 “Agonists of the apelin receptor and methods of use thereof” Pinkerton, A. B.; Smith, L. H.

US 20140005181 “Small molecule antagonists of the apelin receptor for the treatment of disease” Smith, L. H.; Pinkerton, A. B.

Grant

HTS to Identify a Chemical Probes of the Apelin Receptor Signaling Pathway, Layton Smith

A Chemical Biology Strategy to Validate the Apelin Receptor as a Therapeutic Target for Diabetic Reintopathy, Layton Smith

Publications

Maloney PR, Khan P, Hedrick M, Gosalia P, Milewski M, Li L, Roth GP, Sergienko E, Suyama E, Sugarman E, Nguyen K, Mehta A, Vasile S, Su Y, Stonich D, Nguyen H, Zeng FY, Novo AM, Vicchiarelli M, Diwan J, Chung TDY, Pinkerton AB, Smith LH
2010;
Khan P, Maloney PR, Hedrick M, Gosalia P, Milewski M, Li L, Roth GP, Sergienko E, Suyama E, Sugarman E, Nguyen K, Mehta A, Vasile S, Su Y, Shi S, Stonich D, Nguyen H, Zeng FY, Novo AM, Vicchiarelli M, Diwan J, Chung TDY, Pinkerton AB, Smith LH
2010;
Maloney PR, Khan P, Hedrick M, Gosalia P, Milewski M, Li L, Roth GP, Sergienko E, Suyama E, Sugarman E, Nguyen K, Mehta A, Vasile S, Su Y, Stonich D, Nguyen H, Zeng FY, Novo AM, Vicchiarelli M, Diwan J, Chung TD, Smith LH, Pinkerton AB
Bioorg Med Chem Lett 2012 Nov 1;22(21):6656-60