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Pharmaceutical Research, 1987
Since the early 1980s, an intensive effort has been focused on the development of orally effective and long-acting inhibitors of renin. During this time, in vitro potency has increased greatly, with several transition-state inhibitor designs yielding inhibitors with subnanomolar IC50 values.
E, Haber +3 more
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Since the early 1980s, an intensive effort has been focused on the development of orally effective and long-acting inhibitors of renin. During this time, in vitro potency has increased greatly, with several transition-state inhibitor designs yielding inhibitors with subnanomolar IC50 values.
E, Haber +3 more
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[From the renin gene to renin inhibitors].
Annales d'endocrinologie, 1986The only known action of renin is the hydrolysis of angiotensinogen into angiotensin I. Renin is synthesized as an inactive precursor, preprorenin. The processing of prorenin into active renin occurs after the clivage of a profragment, just after a dibasic pair of amino-acids.
P, Corvol, J, Ménard
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Is Angiotensinogen a Renin Inhibitor and Not the Substrate for Renin?
Journal of Hypertension, 1986The cleavage of the angiotensinogen molecule by renin is slow. The rate constant for cleavage of the enzyme-substrate complex, Kcat (turnover number) is lower than usual for enzymes (0.6/s for the homologous human renin reactions and 0.15/s for the homologous mouse renin reaction).
K, Poulsen, J, Jacobsen
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Clinical Science, 1973
1. To examine the substrate specificity of renin a series of analogues of a noctapeptide previously shown to be an effective substrate (Skeggs, Lentz, Kahn & Hochstrasser, 1968) were synthesized. 2. These peptides were studied both with respect to their actions as competitive inhibitors and as substrates. 3.
K, Poulsen, J A, Burton, E, Haber
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1. To examine the substrate specificity of renin a series of analogues of a noctapeptide previously shown to be an effective substrate (Skeggs, Lentz, Kahn & Hochstrasser, 1968) were synthesized. 2. These peptides were studied both with respect to their actions as competitive inhibitors and as substrates. 3.
K, Poulsen, J A, Burton, E, Haber
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Nihon rinsho. Japanese journal of clinical medicine, 1985
Infusion of H.261, the inhibitor of human renin in the baboon, lowered blood angiotensin I, plasma angiotensin II, and arterial pressure suggesting that in the sodium-depleted state angiotensin II contributes to the maintenance of arterial pressure. In a second experiment dose-response infusions of angiotensin II were given in conscious sodium-depleted
T, Ogihara, Y, Kumahara
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Infusion of H.261, the inhibitor of human renin in the baboon, lowered blood angiotensin I, plasma angiotensin II, and arterial pressure suggesting that in the sodium-depleted state angiotensin II contributes to the maintenance of arterial pressure. In a second experiment dose-response infusions of angiotensin II were given in conscious sodium-depleted
T, Ogihara, Y, Kumahara
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Competitive inhibitors of renin
Biochemistry, 1973K, Poulsen, J, Burton, E, Haber
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