The aspartic proteinase renin is an attractive target for the treatment of hypertension and
cardiovascular/renal disease such as chronic kidney disease and heart failure. We …

Renin is the rate-limiting enzyme in the renin–angiotensin–aldosterone system (RAAS)
which regulates blood pressure and renal function and hence is an attractive target for the …

Introduction of the 2, 2-dimethyl-4-phenylpiperazin-5-one scaffold into the P3–P1 portion of
the (2S, 4S, 5S)-5-amino-6-dialkylamino-4-hydroxy-2-isopropylhexanamide backbone …

Selective inhibition of the aspartyl protease renin has gained attraction as an interesting
approach to control hypertension and associated cardiovascular risk factors given its unique …

A novel orally bioavailable renin inhibitor, DS-8108b (5), showing potent renin inhibitory
activity and excellent in vivo efficacy is described. We report herein the synthesis and …

A small library of fragments comprising putative recognition motifs for the catalytic dyad of
aspartic proteases was generated by in silico similarity searches within the corporate …

Background: The aspartic proteinase renin plays an important physiological role in the
regulation of blood pressure. It catalyses the first step in the conversion of angiotensinogen …

The action of the aspartyl protease renin is the rate-limiting initial step of the renin-
angiotensin-aldosterone system. Therefore, renin is a particularly promising target for blood …

Structure guided optimization of a series of nonpeptidic alkyl amine renin inhibitors allowed
the rational incorporation of additional polar functionality. Replacement of the …

Background The aspartic proteinase renin catalyses the first and rate-limiting step in the
conversion of angiotensinogen to the hormone angiotensin II, and therefore plays an …