G protein-coupled receptors: structure- and function-based drug discovery

By Dehua Yang, Qingtong Zhou, Viktorija Labroska, Shanshan Qin, Sanaz Darbalaei, Yiran Wu, Elita Yuliantie, Linshan Xie, Houchao Tao, Jianjun Cheng and 5 more. 2021

500 citations recorded by the source corpus.

As one of the most successful therapeutic target families, G protein-coupled receptors (GPCRs) have experienced a transformation from random ligand screening to knowledge-driven drug design. We are eye-witnessing tremendous progresses made recently in the understanding of their structure–function relationships that facilitated drug development at an unprecedented pace. This article intends to provide a comprehensive overview of this important field to a broader readership that shares some common interests in drug discovery.

Subfields: Cellular and Molecular Neuroscience, Molecular Biology, Radiology, Nuclear Medicine and Imaging

How researchers see this paper

The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.

In Cellular and Molecular Neuroscience

1. Michael Feig
2. Lim Heo

In Molecular Biology

1. Lim Heo
2. Michael Feig
3. Collin F Arbour
4. Yang Zhang
5. Robin Pearce
6. Justin A. Lemkul
7. David Baker

In Radiology, Nuclear Medicine and Imaging

1. Michael Feig
2. Lim Heo

Citations in the corpus

• Multi-State Modeling of G-protein Coupled Receptors at Experimental Accuracy (2021, background): “G-protein coupled receptors (GPCRs) comprise one of the largest protein families in the human genome.9 They are involved in various biological roles such as behavior regulation and regulation of immune system activity.1,2,10,11 They are subdivided into several classes according to sequence homology ”
• AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors (2022, background): “However, the predicted models present different assemblies of ECD and TMD, compared with those of experimental structures.”