Morris Katherine, Kuo Byron, Wilkinson Mark D, Davison Joseph S, Befus A Dean, Mathison Ronald D
Department of Medicine, Faculty of Medicine and Dentistry, University of Alberta, 550A Heritage Medical Research Centre, Edmonton, Alberta, Canada.
Recent Pat Inflamm Allergy Drug Discov. 2007 Jun;1(2):124-32. doi: 10.2174/187221307780979892.
The recently emerged Vcsa1 gene is one member of the variable coding sequence (VCS) multigene family of Rattus norvegicus. This gene encodes the precursor prohormone SMR1 (submandibular rat-1), which on enzymatic processing gives rise to several 5 to 11 amino acid peptides that modulate a variety of physiological functions. The analgesic pentapeptide sialorphin and anti-inflammatory heptapeptide submandibular gland peptide-T (TDIFEGG) are the most intensively studied. Although the Vcsa1 gene and its protein product are unique to rats, TDIFEGG or a derivative acts on all species examined to date, including human cells, in functions related to allergic reactions and inflammation. In this review, the patent and academic literature on SMR1 and its natural peptides and their derivatives are reviewed for consideration of biological targets and relevance to the development of novel therapeutic agents. The VCS gene family is discussed and we speculate on possible human homologs of these potent anti-inflammatory rat-derived peptides. The biologically active peptide products of SMR1 are considered and the mechanism of action and structure-activity relationships of the anti-inflammatory submandibular gland peptide-T and its derivatives are discussed.
最近出现的Vcsa1基因是褐家鼠可变编码序列(VCS)多基因家族的成员之一。该基因编码前体激素原SMR1(大鼠颌下腺-1),经酶加工后可产生几种由5至11个氨基酸组成的肽,这些肽可调节多种生理功能。镇痛五肽唾液吗啡肽和抗炎七肽颌下腺肽-T(TDIFEGG)是研究最为深入的。尽管Vcsa1基因及其蛋白质产物是大鼠特有的,但TDIFEGG或其衍生物在与过敏反应和炎症相关的功能中,对迄今为止所检测的所有物种(包括人类细胞)均有作用。在本综述中,我们回顾了关于SMR1及其天然肽和衍生物的专利及学术文献,以考虑其生物学靶点以及与新型治疗药物开发的相关性。我们讨论了VCS基因家族,并推测了这些强效抗炎大鼠源肽可能的人类同源物。我们还考虑了SMR1的生物活性肽产物,并讨论了抗炎颌下腺肽-T及其衍生物的作用机制和构效关系。