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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...
Pharmacodynamic Models: Overview01:27

Pharmacodynamic Models: Overview

Pharmacodynamic (PD) responses describe the interaction between a drug and its biological target, culminating in a physiological effect. These responses can be classified into different types: continuous variables, such as blood glucose levels; categorical outcomes, like survival rates; and time-to-event metrics, such as disease progression. Understanding and modeling PD responses are critical for optimizing drug efficacy and safety.PD models describe the relationship between drug concentration...
Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
Patch Clamp01:18

Patch Clamp

Many fundamental cell functions such as muscle contraction and nerve transmission rely on the electrical signals produced by the movement of positively and negatively charged ions across the cell membrane. One competent method to record current flowing across the whole cell or single ion channel is the patch-clamp technique.
In this method, a glass micropipette containing electrolyte solution is tightly sealed against a small portion of the cell membrane. As a result, a patch of the cell...

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An overview of recent developments in GPCR modelling: methods and validation.

Adriano Martinelli1, Tiziano Tuccinardi

  • 1Università di Pisa, Dipartimento di Scienze Farmaceutiche, via Bonanno 6, 56126 Pisa, Italy. marti@farm.unipi.it.

Expert Opinion on Drug Discovery
|March 19, 2013
PubMed
Summary

Homology modeling (HM) aids in understanding G-protein-coupled receptors (GPCRs) by predicting their 3D structures. This computational approach is crucial for drug design, overcoming challenges in GPCR structural characterization.

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Pharmacophore Modeling for Targets with Extensive Ligand Libraries: A Case Study on SARS-CoV-2 Mpro

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Area of Science:

  • Biochemistry
  • Structural Biology
  • Computational Biology

Background:

  • G-protein-coupled receptors (GPCRs) are crucial membrane proteins involved in cellular signaling.
  • Understanding GPCR three-dimensional structure is vital for elucidating function and designing targeted ligands.
  • High-resolution structural determination of GPCRs remains challenging due to their membrane-bound nature.

Purpose of the Study:

  • To review common homology modeling (HM) computational steps for GPCRs.
  • To discuss recent alternative approaches and validation methods in GPCR modeling.
  • To present future targets and expected improvements in GPCR homology modeling.

Main Methods:

  • Homology modeling (HM) utilizing templates like bovine rhodopsin.
  • Integration of experimental data such as site-directed mutagenesis and cysteine accessibility studies.
  • Discussion of computational steps, alternative modeling approaches, and validation techniques.

Main Results:

  • Homology modeling is a key computational strategy for GPCR structural studies.
  • Experimental data integration enhances the accuracy and reliability of GPCR models.
  • Review of current HM techniques and their application to GPCRs.

Conclusions:

  • Homology modeling is indispensable for advancing GPCR research and drug discovery.
  • Continued development of computational methods will improve GPCR structural predictions.
  • Future applications of HM will expand our understanding of diverse GPCR targets.