Fleig Andrea, Penner Reinhold
Laboratory of Cell and Molecular Signaling, Center for Biomedical Research, The Queen's Medical Center and Department of Cell and Molecular Biology, John A. Burns School of Medicine, The University of Hawaii, Honolulu, HI 96813, USA.
Trends Pharmacol Sci. 2004 Dec;25(12):633-9. doi: 10.1016/j.tips.2004.10.004.
Significant progress in the molecular and functional characterization of a subfamily of genes that encode melastatin-related transient receptor potential (TRPM) cation channels has been made during the past few years. This subgroup of the TRP superfamily of ion channels contains eight mammalian members and has isoforms in most eukaryotic organisms. The individual members of the TRPM subfamily have specific expression patterns and ion selectivity, and their specific gating and regulatory mechanisms are tailored to integrate multiple signaling pathways. The diverse functional properties of these channels have a profound effect on the regulation of ion homoeostasis by mediating direct influx of Ca2+, controlling Mg2+ entry, and determining the potential of the cell membrane. TRPM channels are involved in several physiological and pathological conditions in electrically excitable and non-excitable cells, which make them exciting targets for drug discovery.
在过去几年中,编码与褪黑素相关的瞬时受体电位(TRPM)阳离子通道的基因亚家族在分子和功能表征方面取得了重大进展。这个离子通道TRP超家族的亚组包含八个哺乳动物成员,并且在大多数真核生物中都有亚型。TRPM亚家族的各个成员具有特定的表达模式和离子选择性,它们特定的门控和调节机制经过调整以整合多种信号通路。这些通道多样的功能特性通过介导Ca2+的直接内流、控制Mg2+的进入以及决定细胞膜电位,对离子稳态的调节产生深远影响。TRPM通道参与了可兴奋细胞和非可兴奋细胞中的多种生理和病理状况,这使得它们成为药物研发中令人兴奋的靶点。