A potential therapeutic role for P2X7 receptor (P2X7R) antagonists in the treatment of inflammatory diseases

被引：234

作者：

Arulkumaran, Nishkantha ^{[1
]}

Unwin, Robert J. ^{[2
,3
]}

Tam, Frederick W. K. ^{[1
]}

机构：

[1] Univ London Imperial Coll Sci Technol & Med, Hammersmith Hosp, Renal Sect, Dept Med, London W12 0HS, England

[2] UCL, Ctr Nephrol, London NW3 2PF, England

[3] UCL, London Epithelial Grp, London NW3 2PF, England

来源：

EXPERT OPINION ON INVESTIGATIONAL DRUGS | 2011年 / 20卷 / 07期

基金：

英国惠康基金;

关键词：

apoptosis; inflammasome; inflammation; interleukin-1; P2X7; RHEUMATOID-ARTHRITIS PATIENTS; SENSITIVE P2X(7) RECEPTOR; ACUTE-RENAL-FAILURE; LUNG INFLAMMATION; PEPTIDE LL-37; DANGER SIGNAL; SEVERE SEPSIS; EXPRESSION; ATP; APOPTOSIS;

D O I：

10.1517/13543784.2011.578068

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Areas covered: We have reviewed the current literature on the role of the P2X7R in inflammatory diseases, focusing on potential therapeutic applications of selective P2X7R antagonists as anti-inflammatory agents. Particular emphasis has been placed on the potential role of P2X7R in common inflammatory diseases. The latest developments in Phase I and II clinical trials of P2X7R antagonists are covered. Expert opinion: Recent studies using gene knockout mice and selective P2X7R antagonists suggest that P2X7R is a viable therapeutic target for inflammatory diseases. However, efficacious P2X7R antagonists for use in clinical studies are still at an early stage of development. Future challenges include: identifying potential toxicity and side effects of treatment, timing of treatment initiation and its duration in chronic inflammatory conditions, optimum dosage and development of a functional assay for P2X7R that would help to guide treatment.

引用

页码：897 / 915

页数：19

共 117 条

[1] Basal activation of the P2X7 ATP receptor elevates mitochondrial calcium and potential, increases cellular ATP levels, and promotes serum-independent growth [J].