Giannella Mario, Angeli Piero
School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, 62032 Camerino, Italy.
In Silico Pharmacol. 2013 Dec 20;1:21. doi: 10.1186/2193-9616-1-21. eCollection 2013.
The organizers of the Camerino Receptor Symposia survey the development of receptorology. They trace the course from the first Symposium in 1978, which laid the foundation for Pirenzepine, the first selective muscarinic antagonist, to the 2010 Symposium, which highlighted the utility of functional simple domain antibodies (nanobodies) as novel G Protein-Coupled Receptor (GPCR) modulators. This 30-year period sees the acceptance of terms such as G-protein, auto- and heteroreceptors, site-directed mutagenesis, chimeric receptors, constitutive activity, inverse agonism, and orphan receptors. GPCRs are finally a reality and Langley and Ehrlich, if they returned to their laboratories, would be proud of how their intuitions have been realized.
卡梅里诺受体研讨会的组织者们审视了受体学的发展历程。他们追溯了从1978年第一届研讨会开始的发展轨迹,那次研讨会为首个选择性毒蕈碱拮抗剂哌仑西平奠定了基础,一直到2010年的研讨会,该研讨会强调了功能性单域抗体(纳米抗体)作为新型G蛋白偶联受体(GPCR)调节剂的效用。在这30年期间,人们接受了诸如G蛋白、自身受体和异源受体、定点诱变、嵌合受体、组成性活性、反向激动作用和孤儿受体等术语。GPCR最终成为了现实,要是兰利和埃利希回到他们的实验室,他们会为自己的直觉如此得以实现而感到自豪。