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Abstract: This paper reports on a systemic screen for potent and selective dipeptidyl peptidase (DPP) II inhibitors. The boronic acid derivative boroNorvaline (boroNva) was designated as the P1 position amino acid and a library of amino acids, both natural and synthetic, were coupled with boroNva to form dipeptide inhibitors. The inhibitors were tested against the members of the DPPIV activity and... read more/or structure homolog (DASH) enzymes and the 20S proteasome. It was found that the boroNva based compounds had strong potency for DPPII, especially Methionine (Met)-boroNva (6) and Leucine (Leu)-boroNva (10), but suffered from poor selectivity. The selectivity for DPPII was improved when α, α carbon di-substituted amino acids were coupled with boroNva. These small molecules can help provide a new route for increased selectivity of boronic acid derivatives, and ultimately facilitate our understanding of DPPII's role in biological systems.
Thesis (M.S.)--Tufts University, 2016.
Submitted to the Dept. of Pharmacology & Experimental Therapeutics.
Advisor: William Bachovchin.
Committee: David Greenblatt.
Keywords: Biochemistry, and Organic chemistry.read less
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