Search Results - "Lala, Deepak S"
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The Medicinal Chemistry of Liver X Receptor (LXR) Modulators
Published in Journal of medicinal chemistry (11-09-2014)“…LXRs have been of interest as targets for the treatment of atherosclerosis for over a decade. In recent years, LXR modulators have also garnered interest for…”
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The Hypolipidemic Natural Product Guggulsterone Acts as an Antagonist of the Bile Acid Receptor
Published in Molecular endocrinology (Baltimore, Md.) (01-07-2002)“…Ayurveda, the ancient Indian system of health care and medicine, has a well-organized materia medica in which plants form a dominant part. A key illustration…”
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3
Activation of the Orphan Nuclear Receptor Steroidogenic Factor 1 by Oxysterols
Published in Proceedings of the National Academy of Sciences - PNAS (13-05-1997)“…Steroidogenic factor 1 (SF-1), an orphan member of the intracellular receptor superfamily, plays an essential role in the development and function of multiple…”
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Repression of p65 Transcriptional Activation by the Glucocorticoid Receptor in the Absence of Receptor-Coactivator Interactions
Published in Molecular endocrinology (Baltimore, Md.) (01-01-2004)“…Glucocorticoids are among the most potent antiinflammatory agents, acting through the glucocorticoid receptor (GR) to suppress gene expression of a variety of…”
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Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists
Published in Bioorganic & medicinal chemistry (15-03-2016)“…[Display omitted] Mineralocorticoid receptor (MR) antagonists continue to be a prevalent area of research in the pharmaceutical industry. Herein we report the…”
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Activation of specific RXR heterodimers by an antagonist of RXR homodimers
Published in Nature (London) (03-10-1996)“…Retinoid X receptor (RXR) plays a central role in the regulation of many intracellular receptor signalling pathways and can mediate ligand-dependent…”
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Pharmacological characterization of the selective 11β-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes
Published in European journal of pharmacology (05-01-2015)“…To combat the increased morbidity and mortality associated with the developing diabetes epidemic new therapeutic interventions are desirable. Inhibition of…”
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Regulation of sphingomyelin phosphodiesterase acid-like 3A gene (SMPDL3A) by liver X receptors
Published in Molecular pharmacology (01-10-2012)“…Liver X receptor (LXR) α and LXRβ function as physiological sensors of cholesterol metabolites (oxysterols), regulating key genes involved in cholesterol and…”
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Influence of sub-chronic selective 11β-hydroxysteroid dehydrogenase 1 inhibition on the hypothalamic-pituitary-adrenal axis in female cynomolgus monkeys
Published in European journal of pharmacology (15-10-2016)“…Inhibition of local cortisol regeneration from circulating cortisone by blocking 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) has been shown to ameliorate the…”
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The hypolipidemic natural product guggulsterone acts as an antagonist of the bile acid receptor
Published in Molecular endocrinology (Baltimore, Md.) (01-07-2002)“…Ayurveda, the ancient Indian system of health care and medicine, has a well-organized materia medica in which plants form a dominant part. A key illustration…”
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Effects of the bace1 inhibitor bi 1181181 and the anti-abeta antibody m266 on abeta in rat brain homogenate and CSF
Published in Alzheimer's & dementia (01-07-2015)Get full text
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Liver X Receptors Interact with Corepressors to Regulate Gene Expression
Published in Molecular endocrinology (Baltimore, Md.) (01-06-2003)“…Liver X receptors (LXRs) are members of the nuclear receptor superfamily that regulate gene expression in response to oxysterols and play a critical role in…”
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An Activin Receptor-Like Kinase 5 Inhibitor Reduces Collagen Deposition in a Rat Dermal Incision Wound Healing Model
Published in Plastic and reconstructive surgery (1963) (01-11-2011)“…Excessive dermal scarring is characterized by an overabundant deposition of extracellular matrix caused by fibrosis. The purpose of this study was to modify a…”
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Pharmacological characterization of the new bace1 inhibitor bi 1181181
Published in Alzheimer's & dementia (01-07-2015)Get full text
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15
Multiplexing nuclear receptors for agonist identification in a cell-based reporter gene high-throughput screen
Published in Journal of biomolecular screening (01-06-2003)“…High-throughput screening (HTS) has become an essential part of the drug discovery process. Due to the rising requirements for both data quality and quantity,…”
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The Ligand-Dependent Interaction of Mineralocorticoid Receptor with Coactivator and Corepressor Peptides Suggests Multiple Activation Mechanisms
Published in Molecular endocrinology (Baltimore, Md.) (01-06-2005)“…We investigated the coregulator (coactivator and corepressor) interactions with the mineralocorticoid receptor (MR) that lead to activation and inhibition of…”
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Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring
Published in Bioorganic & medicinal chemistry letters (15-05-2012)“…Application of PF-03671148 to rat wounds leads to a dose dependent inhibition of multiple fibrotic genes in vivo. A series of 2-(1H-pyrazol-1-yl)pyridines are…”
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Steroidogenic factor 1: an essential mediator of endocrine development
Published in Recent progress in hormone research (2002)“…The orphan nuclear receptor steroidogenic factor 1 (SF-1, also called Ad4BP and officially designated NR5A1) has emerged as an essential regulator of endocrine…”
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The liver X receptors
Published in Current opinion in investigational drugs (London, England : 2000) (01-09-2005)“…The liver X receptors (LXRs), members of the nuclear receptor superfamily, are potential targets for a variety of diseases. While there are many opportunities…”
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Molecular mechanisms of mineralocorticoid receptor antagonism by eplerenone
Published in Mini reviews in medicinal chemistry (01-08-2005)“…Mineralocorticoid receptor (MR) antagonism has proven to effectively attenuate the pathophysiological effects of aldosterone in clinical and experimental…”
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