Antidiabetic and antisteatotic effects of the selective fatty acid synthase (FAS) inhibitor platensimycin in mouse models of diabetes

…, CC Chung, G Salituro, BV Karanam… - Proceedings of the …, 2011 - National Acad Sciences
Platensimycin (PTM) is a recently discovered broad-spectrum antibiotic produced by
Streptomyces platensis. It acts by selectively inhibiting the elongation-condensing enzyme FabF of …

In vitro metabolism of FK-506 in rat, rabbit, and human liver microsomes: identification of a major metabolite and of cytochrome P450 3A as the major enzymes …

SH Vincent, BV Karanam, SK Painter… - Archives of biochemistry …, 1992 - Elsevier
The metabolism of the immunosuppressant FK-506 was shown to be catalyzed primarily by
cytochrome P450 isozymes of the P450 3A subfamily. Antibodies against rat P450 3A …

Discovery of MK-4409, a novel oxazole FAAH inhibitor for the treatment of inflammatory and neuropathic pain

…, EJ Martel, JF Leone, L Frey, B Karanam… - ACS Medicinal …, 2014 - ACS Publications
We report herein the identification of MK-4409, a potent and selective fatty acid amide
hydrolase (FAAH) inhibitor. Starting from a high throughput screening (HTS) hit, medicinal …

Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity

…, KA Lyons, AH Mao, JR Carlin, BV Karanam… - Bioorganic & medicinal …, 2001 - Elsevier
Stereospecific introduction of a methyl group to the indole-3-side chain enhanced activity in
our tryptamine-derived series of GnRH receptor antagonists. Further improvements were …

Benzazepinone Nav1. 7 blockers: potential treatments for neuropathic pain

…, ML Garcia, N Jochnowitz, BV Karanam… - Bioorganic & medicinal …, 2007 - Elsevier
Benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain - ScienceDirect
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Trace level quantification of deuterated 17β‐estradiol and estrone in ovariectomized mouse plasma and brain using liquid chromatography/tandem mass spectrometry …

…, S Patel, R Bakhtiar, B Karanam… - … in mass spectrometry, 2004 - Wiley Online Library
A sensitive liquid chromatography/tandem mass spectrometry (LC/MS/MS) method coupled
with dansylation was developed for the simultaneous quantification of exogenously …

Discovery of MK-3168: a PET tracer for imaging brain fatty acid amide hydrolase

…, N Jochnowitz, M Rosenbach, B Karanam… - ACS Medicinal …, 2013 - ACS Publications
We report herein the discovery of a fatty acid amide hydrolase (FAAH) positron emission
tomography (PET) tracer. Starting from a pyrazole lead, medicinal chemistry efforts directed …

Pharmacological inhibition of diacylglycerol acyltransferase 1 reduces body weight and modulates gut peptide release—Potential insight into mechanism of action

…, E Carballo‐Jane, S Craw, X Guan, B Karanam… - …, 2013 - Wiley Online Library
Objective Investigation was conducted to understand the mechanism of action of diacylglycerol
acyltransferase 1 (DGAT1) using small molecules DGAT1 inhibitors, compounds K and L. …

2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain

…, KA Lyons, AH Mao, JR Carlin, BV Karanam… - Bioorganic & medicinal …, 2002 - Elsevier
A series of 2-arylindoles containing novel heteroaromatic substituents on the tryptamine
tether, based on compound 1, was prepared and evaluated for their ability to act as …

Imidazopyridines: a novel class of hNav1. 7 channel blockers

…, WJ Martin, KA Lyons, X Li, BV Karanam… - Bioorganic & medicinal …, 2008 - Elsevier
A series of imidazopyridines were evaluated as potential sodium channel blockers for the
treatment of neuropathic pain. Several members were identified with good hNa v 1.7 potency …