L337H mutant of rat neuronal nitric oxide synthase resembles human neuronal nitric oxide synthase toward inhibitors.

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Fang J, Ji H, Lawton GR, Xue F, Roman LJ, Silverman RB

L337H mutant of rat neuronal nitric oxide synthase resembles human neuronal nitric oxide synthase toward inhibitors.

J Med Chem. 2009 Jul 23;52(14):4533-7. doi: 10.1021/jm900380j.

PubMed ID

19537690 [ View in PubMed

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Abstract

A common dichotomy exists in inhibitor design: should the compounds be designed to block the enzymes of animals in the preclinical studies or to inhibit the human enzyme? We report that a single mutation of Leu-337 in rat neuronal nitric oxide synthase (nNOS) to His makes the enzyme resemble human nNOS more than rat nNOS. We expect that the approach used in this study can unite the dichotomy and speed up the process of inhibitor design and development.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Nitroarginine	Nitric oxide synthase, brain	IC 50 (nM)	4400	N/A	N/A	Details