Literature DB >> 26556675

Validation of ion channel targets.

Aaron C Gerlach1, Brett M Antonio1.   

Abstract

A prerequisite for a successful target-based drug discovery program is a robust data set that increases confidence in the validation of the molecular target and the therapeutic approach. Given the significant time and resource investment required to carry a drug to market, early selection of targets that can be modulated safely and effectively forms the basis for a strong portfolio and pipeline. In this article we present some of the more useful scientific approaches that can be applied toward the validation of ion channel targets, a molecular family with a history of clinical success in therapeutic areas such as cardiovascular, respiratory, pain and neuroscience.

Entities:  

Keywords:  drug discovery; ion channel; modulator; proof of mechanism; validation

Mesh:

Substances:

Year:  2015        PMID: 26556675      PMCID: PMC4850043          DOI: 10.1080/19336950.2015.1081725

Source DB:  PubMed          Journal:  Channels (Austin)        ISSN: 1933-6950            Impact factor:   2.581


  20 in total

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Review 2.  Genotype-phenotype relationships in cystic fibrosis.

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3.  Respiration and parturition affected by conditional overexpression of the Ca2+-activated K+ channel subunit, SK3.

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Journal:  Science       Date:  2000-09-15       Impact factor: 47.728

4.  Quantitative single-cell RNA-seq with unique molecular identifiers.

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5.  Retigabine as adjunctive therapy in adults with partial-onset seizures: integrated analysis of three pivotal controlled trials.

Authors:  Roger J Porter; David E Burdette; Antonio Gil-Nagel; Susan T Hall; Robin White; Soraya Shaikh; Sarah E DeRossett
Journal:  Epilepsy Res       Date:  2012-04-16       Impact factor: 3.045

6.  Peptidergic CGRPα primary sensory neurons encode heat and itch and tonically suppress sensitivity to cold.

Authors:  Eric S McCoy; Bonnie Taylor-Blake; Sarah E Street; Alaine L Pribisko; Jihong Zheng; Mark J Zylka
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Review 7.  Impact of genetics on the clinical management of channelopathies.

Authors:  Peter J Schwartz; Michael J Ackerman; Alfred L George; Arthur A M Wilde
Journal:  J Am Coll Cardiol       Date:  2013-05-15       Impact factor: 24.094

Review 8.  Genetically humanized mouse models of drug metabolizing enzymes and transporters and their applications.

Authors:  Nico Scheer; C Roland Wolf
Journal:  Xenobiotica       Date:  2013-07-11       Impact factor: 1.908

9.  Temporal control of gene deletion in sensory ganglia using a tamoxifen-inducible Advillin-Cre-ERT2 recombinase mouse.

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Journal:  Mol Pain       Date:  2011-12-21       Impact factor: 3.395

10.  CGRPα-expressing sensory neurons respond to stimuli that evoke sensations of pain and itch.

Authors:  Eric S McCoy; Bonnie Taylor-Blake; Mark J Zylka
Journal:  PLoS One       Date:  2012-05-01       Impact factor: 3.240

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  1 in total

Review 1.  Potassium channels in the sinoatrial node and their role in heart rate control.

Authors:  Qadeer Aziz; Yiwen Li; Andrew Tinker
Journal:  Channels (Austin)       Date:  2018       Impact factor: 2.581

  1 in total

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