European Centre for Living Technology, University of Venice, 30123 Venice, Italy.
Int J Mol Sci. 2024 Jan 28;25(3):1621. doi: 10.3390/ijms25031621.
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human genome and constitute about 30% of all drug targets. In this article, intended for a non-mathematical audience, both experimental observations and new theoretical results are compared in the context of information transmission across the cell membrane. The amount of information actually currently used or projected to be used in clinical settings is a small fraction of the information transmission capacity of the GPCR. This indicates that the number of yet undiscovered drug targets within GPCRs is much larger than what is currently known. Theoretical studies with some experimental validation indicate that localized heat deposition and dissipation are key to the identification of sites and mechanisms for drug action.
G 蛋白偶联受体(GPCRs)是人类基因组中最大的受体家族,约占所有药物靶点的 30%。本文面向非数学读者,在跨细胞膜信息传递的背景下,比较了实验观察结果和新的理论结果。实际上,在临床环境中使用或预计使用的信息量只是 GPCR 信息传递能力的一小部分。这表明 GPCR 中尚未发现的药物靶点数量远远超过目前已知的数量。一些具有实验验证的理论研究表明,局部热沉积和耗散是确定药物作用部位和机制的关键。