LymphedemaV1, Main, Exploration, bibRecord, 000993

The shifting landscape of KATP channelopathies and the need for ‘sharper’ therapeutics

Identifieur interne : 000993 ( Main/Exploration ); précédent : 000992; suivant : 000994

The shifting landscape of KATP channelopathies and the need for ‘sharper’ therapeutics

Auteurs : Sujay V. Kharade [États-Unis] ; Colin Nichols [États-Unis] ; Jerod S. Denton [États-Unis]

Source :

Future Medicinal Chemistry [ 1756-8919 ] ; 2016.

RBID : PMC:4976861

Abstract

ATP-sensitive potassium (K_ATP) channels play fundamental roles in the regulation of endocrine, neural and cardiovascular function. Small-molecule inhibitors (e.g., sulfonylurea drugs) or activators (e.g., diazoxide) acting on SUR1 or SUR2 have been used clinically for decades to manage the inappropriate secretion of insulin in patients with Type 2 diabetes, hyperinsulinism and intractable hypertension. More recently, the discovery of rare disease-causing mutations in K_ATP channel-encoding genes has highlighted the need for new therapeutics for the treatment of certain forms of neonatal diabetes mellitus, congenital hyperinsulinism and Cantu syndrome. Here, we provide a high-level overview of the pathophysiology of these diseases and discuss the development of a flexible high-throughput screening platform to enable the development of new classes of K_ATP channel modulators.

Url:

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4976861

DOI: 10.4155/fmc-2016-0005
PubMed: 27161588
PubMed Central: 4976861

Affiliations:

Le document en format XML

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<front><div type="abstract" xml:lang="en"><p>ATP-sensitive potassium (K<sub>ATP</sub>
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 channel-encoding genes has highlighted the need for new therapeutics for the treatment of certain forms of neonatal diabetes mellitus, congenital hyperinsulinism and Cantu syndrome. Here, we provide a high-level overview of the pathophysiology of these diseases and discuss the development of a flexible high-throughput screening platform to enable the development of new classes of K<sub>ATP</sub>
 channel modulators.</p>
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The shifting landscape of KATP channelopathies and the need for ‘sharper’ therapeutics

The shifting landscape of KATP channelopathies and the need for ‘sharper’ therapeutics

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Abstract

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