Evolving cryo-EM structural approaches for GPCR drug discovery.
Sign Up to like & getrecommendations! Published in 2021 at "Structure"
DOI: 10.1016/j.str.2021.04.008
Abstract: G protein-coupled receptors (GPCRs) are the largest class of cell surface drug targets. Advances in stabilization of GPCR:transducer complexes, together with improvements in cryoelectron microscopy (cryo-EM) have recently been applied to structure-assisted drug design for… read more here.
Keywords: cryo structural; evolving cryo; gpcr drug; drug ... See more keywords
GPCRomics: An Approach to Discover GPCR Drug Targets.
Sign Up to like & getrecommendations! Published in 2019 at "Trends in pharmacological sciences"
DOI: 10.1016/j.tips.2019.04.001
Abstract: G protein-coupled receptors (GPCRs) are targets for ∼35% of approved drugs but only ∼15% of the ∼800 human GPCRs are currently such targets. GPCRomics, the use of unbiased, hypothesis-generating methods [e.g., RNA-sequencing (RNA-seq)], with tissues… read more here.
Keywords: drug targets; targets gpcromics; gpcr drug; discover gpcr ... See more keywords
The application of artificial intelligence to accelerate GPCR drug discovery.
Sign Up to like & getrecommendations! Published in 2023 at "British journal of pharmacology"
DOI: 10.1111/bph.16140
Abstract: The application of artificial intelligence approaches to drug discovery for G protein-coupled receptors (GPCRs) is a rapidly expanding area. Artificial intelligence can be used at multiple stages during the drug discovery process, from aiding our… read more here.
Keywords: artificial intelligence; gpcr drug; drug discovery;
EDITORIAL; GPCR Drug Discovery: Emerging Targets, Novel Approaches and Future Trends.
Sign Up to like & getrecommendations! Published in 2019 at "Current topics in medicinal chemistry"
DOI: 10.2174/156802661916190828093500
Abstract: read more here.
Keywords: targets novel; gpcr drug; editorial gpcr; drug discovery ... See more keywords
BOW-GBDT: A GBDT Classifier Combining With Artificial Neural Network for Identifying GPCR–Drug Interaction Based on Wordbook Learning From Sequences
Sign Up to like & getrecommendations! Published in 2020 at "Frontiers in Cell and Developmental Biology"
DOI: 10.3389/fcell.2020.623858
Abstract: Background: As a class of membrane protein receptors, G protein-coupled receptors (GPCRs) are very important for cells to complete normal life function and have been proven to be a major drug target for widespread clinical… read more here.
Keywords: gpcr drug; drug pairs; bow gbdt; drug ... See more keywords
Accelerating GPCR Drug Discovery With Conformation-Stabilizing VHHs
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Molecular Biosciences"
DOI: 10.3389/fmolb.2022.863099
Abstract: The human genome encodes 850 G protein-coupled receptors (GPCRs), half of which are considered potential drug targets. GPCRs transduce extracellular stimuli into a plethora of vital physiological processes. Consequently, GPCRs are an attractive drug target… read more here.
Keywords: drug discovery; pharmacology; accelerating gpcr; gpcr drug ... See more keywords