An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs

Lundstrom, Kenneth

doi:10.1007/978-1-60327-317-6_4

Cited by 137Receptor Mechanisms and SignalingComputational Drug Discovery MethodsProtein Structure and Dynamics

An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs

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Lundstrom, Kenneth·2009·Methods in Molecular Biology

DOI 10.1007/978-1-60327-317-6_4PMC PMC7122359

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Abstract

The drug discovery process has passed through dramatic changes during the past 20 years. The requirements for drug manufacturing and especially the safety aspects related to the final medicine have become immense. This development has made the drug discovery and development processes both time-consuming and labor intensive. Not surprisingly, development of drugs has become extremely expensive. In addition, the success rate of bringing new successful drugs to the market has been worryingly low. One approach to speed up drug discovery and also to reduce the adverse effects of developed drugs has been to apply structure-based drug design. There are a number of examples of success. For instance, structural information has played an important role in lead optimization in drug screening programs ( 1 ) . Furthermore, high-resolution structures of HIV proteinase ( 2 ) and influenza virus neuraminidase ( 3 ) have contributed directly to the development of AIDS (Agenerase® and Viracept®) and flu (Relenza®) drugs, respectively. In total, more than 10 drugs can today be considered as designed based on known high-resolution structures of target molecules.

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GPCRs have long been known as among the most druggable of targets, and their druggability is currently advancing rapidly due to advances in GPCR structural biology and molecular dynamic simulations.
“Moreover, while GPCRs have long been known as among the most ‘druggable’ of targets (Gurrath, 2001; Lundstrom, 2009), the ‘druggability’ of GPCRs is currently advancing very rapidly due to advances in GPCR structural biology and molecular dynamic simulations (Hilger et al., 2018; Koehl et al., 2018; Weis and Kobilka, 2018).”
From Single-cell transcriptomic evidence for dense intracortical neuropeptide networks (2019) · cites this paper as Lundstrom, 2009

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Authors: Lundstrom, K.
Corresponding author: Lundstrom, Kenneth
ORCID: Lundstrom, Kenneth
Venue: Methods in Molecular Biology
Publisher: Humana Press
Published: 2009
Volume: 552
Pages: 51-66
ISSN: 1064-3745 (ISSN-L)
1940-6029
DOI: 10.1007/978-1-60327-317-6_4
PMC: PMC7122359
OpenAlex: W35537551
Cited by: 137
References: 100
Citations by year: 2026: 2 · 2025: 5 · 2024: 11 · 2023: 8 · 2022: 4 · 2021: 9 · 2020: 8 · 2019: 7 · 2018: 6 · 2017: 8 · 2016: 9 · 2015: 18 · 2014: 8 · 2013: 12 · 2012: 8
FWCI: 8.67
Type: book chapter
Language: en
Open access: bronze
doi.org
Licence: www.springer.com/tdm (tdm)
Locations: Methods in molecular biology (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Structure and Dynamics
Keywords: G protein-coupled receptors, structure-based drug design, structural biology, drug discovery, lead optimization, drug screening, HIV protease inhibitors, influenza neuraminidase inhibitors, high-resolution protein structures
MeSH terms: Animals, Humans, Drug Design, Combinatorial Chemistry Techniques, Receptors, G-Protein-Coupled, Drug Discovery

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An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs

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