Use of kv1.3 blockers for inflammatory skin conditions

W. Nguyen, B. L. Howard, D. S. Neale, P. E. Thompson, P. J. White, Heike Wulff, D. T. Manallack

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

Recent results using animal models of inflammatory skin conditions have shown that blockers of the voltage-gated potassium channel, Kv1.3 hold great promise for clinical utility. Kv1.3 blockers act as immunosuppressants by modulating the various subsets of inflammatory T and B cells involved in autoimmune disorders. While peptidic inhibitors based on naturally occurring venoms demonstrate potent and selective Kv1.3 blockade, these require parenteral administration and may face potential immunogenicity problems. Small molecule blockers show considerable diversity, however selectivity over other Kv1-family channels has been difficult to achieve. More recent advances have added to the evidence that Kv1.3 channels are a suitable therapeutic target and that the development of novel and selective agents will herald new drugs for inflammatory skin disorders.

Original languageEnglish (US)
Pages (from-to)2882-2896
Number of pages15
JournalCurrent Medicinal Chemistry
Volume17
Issue number26
DOIs
StatePublished - 2010

Fingerprint

Skin
B-Lymphocyte Subsets
Voltage-Gated Potassium Channels
Venoms
T-Lymphocyte Subsets
Immunosuppressive Agents
Animals
Animal Models
Cells
Molecules
Pharmaceutical Preparations
Therapeutics

Keywords

  • Autoimmune disorder
  • Drug design
  • Inflammation
  • Kv1.3 channel
  • Psoriasis

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

Cite this

Nguyen, W., Howard, B. L., Neale, D. S., Thompson, P. E., White, P. J., Wulff, H., & Manallack, D. T. (2010). Use of kv1.3 blockers for inflammatory skin conditions. Current Medicinal Chemistry, 17(26), 2882-2896. https://doi.org/10.2174/092986710792065072

Use of kv1.3 blockers for inflammatory skin conditions. / Nguyen, W.; Howard, B. L.; Neale, D. S.; Thompson, P. E.; White, P. J.; Wulff, Heike; Manallack, D. T.

In: Current Medicinal Chemistry, Vol. 17, No. 26, 2010, p. 2882-2896.

Research output: Contribution to journalArticle

Nguyen, W, Howard, BL, Neale, DS, Thompson, PE, White, PJ, Wulff, H & Manallack, DT 2010, 'Use of kv1.3 blockers for inflammatory skin conditions', Current Medicinal Chemistry, vol. 17, no. 26, pp. 2882-2896. https://doi.org/10.2174/092986710792065072
Nguyen, W. ; Howard, B. L. ; Neale, D. S. ; Thompson, P. E. ; White, P. J. ; Wulff, Heike ; Manallack, D. T. / Use of kv1.3 blockers for inflammatory skin conditions. In: Current Medicinal Chemistry. 2010 ; Vol. 17, No. 26. pp. 2882-2896.
@article{62b44a1ac10a409682cba1c500c44570,
title = "Use of kv1.3 blockers for inflammatory skin conditions",
abstract = "Recent results using animal models of inflammatory skin conditions have shown that blockers of the voltage-gated potassium channel, Kv1.3 hold great promise for clinical utility. Kv1.3 blockers act as immunosuppressants by modulating the various subsets of inflammatory T and B cells involved in autoimmune disorders. While peptidic inhibitors based on naturally occurring venoms demonstrate potent and selective Kv1.3 blockade, these require parenteral administration and may face potential immunogenicity problems. Small molecule blockers show considerable diversity, however selectivity over other Kv1-family channels has been difficult to achieve. More recent advances have added to the evidence that Kv1.3 channels are a suitable therapeutic target and that the development of novel and selective agents will herald new drugs for inflammatory skin disorders.",
keywords = "Autoimmune disorder, Drug design, Inflammation, Kv1.3 channel, Psoriasis",
author = "W. Nguyen and Howard, {B. L.} and Neale, {D. S.} and Thompson, {P. E.} and White, {P. J.} and Heike Wulff and Manallack, {D. T.}",
year = "2010",
doi = "10.2174/092986710792065072",
language = "English (US)",
volume = "17",
pages = "2882--2896",
journal = "Current Medicinal Chemistry",
issn = "0929-8673",
publisher = "Bentham Science Publishers B.V.",
number = "26",

}

TY - JOUR

T1 - Use of kv1.3 blockers for inflammatory skin conditions

AU - Nguyen, W.

AU - Howard, B. L.

AU - Neale, D. S.

AU - Thompson, P. E.

AU - White, P. J.

AU - Wulff, Heike

AU - Manallack, D. T.

PY - 2010

Y1 - 2010

N2 - Recent results using animal models of inflammatory skin conditions have shown that blockers of the voltage-gated potassium channel, Kv1.3 hold great promise for clinical utility. Kv1.3 blockers act as immunosuppressants by modulating the various subsets of inflammatory T and B cells involved in autoimmune disorders. While peptidic inhibitors based on naturally occurring venoms demonstrate potent and selective Kv1.3 blockade, these require parenteral administration and may face potential immunogenicity problems. Small molecule blockers show considerable diversity, however selectivity over other Kv1-family channels has been difficult to achieve. More recent advances have added to the evidence that Kv1.3 channels are a suitable therapeutic target and that the development of novel and selective agents will herald new drugs for inflammatory skin disorders.

AB - Recent results using animal models of inflammatory skin conditions have shown that blockers of the voltage-gated potassium channel, Kv1.3 hold great promise for clinical utility. Kv1.3 blockers act as immunosuppressants by modulating the various subsets of inflammatory T and B cells involved in autoimmune disorders. While peptidic inhibitors based on naturally occurring venoms demonstrate potent and selective Kv1.3 blockade, these require parenteral administration and may face potential immunogenicity problems. Small molecule blockers show considerable diversity, however selectivity over other Kv1-family channels has been difficult to achieve. More recent advances have added to the evidence that Kv1.3 channels are a suitable therapeutic target and that the development of novel and selective agents will herald new drugs for inflammatory skin disorders.

KW - Autoimmune disorder

KW - Drug design

KW - Inflammation

KW - Kv1.3 channel

KW - Psoriasis

UR - http://www.scopus.com/inward/record.url?scp=77955617273&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=77955617273&partnerID=8YFLogxK

U2 - 10.2174/092986710792065072

DO - 10.2174/092986710792065072

M3 - Article

C2 - 20858170

AN - SCOPUS:77955617273

VL - 17

SP - 2882

EP - 2896

JO - Current Medicinal Chemistry

JF - Current Medicinal Chemistry

SN - 0929-8673

IS - 26

ER -