Related Experiment Video

Updated: Sep 19, 2025

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

9.0K

Leveraging machine learning and molecular docking techniques to predict novel melanocortin-4 receptor agonists

Stavroula Giakoumopoulou1, Paris Christodoulou1, Minos-Timotheos Matsoukas1

  • 1University of West Attica, Egaleo, Greece.

Folia Medica
|June 17, 2025
PubMed
Abstract

Insights

Monogenic obesity linked to melanocortin-4 receptor (MC4R) gene mutations presents treatment challenges. Targeting MC4R offers a promising therapeutic strategy for obesity due to its role in energy balance.

Area of Science:

  • Endocrinology
  • Genetics
  • Pharmacology

Background:

  • Monogenic obesity due to melanocortin-4 receptor (MC4R) gene mutations is a significant health concern.
  • Despite research, effective treatments for MC4R-related obesity remain limited.
  • The MC4R plays a crucial role in regulating energy homeostasis and adipose tissue development.

Purpose of the Study:

  • To explore the therapeutic potential of targeting the MC4R for obesity treatment.
  • To investigate novel strategies for addressing monogenic obesity caused by MC4R dysfunction.

Main Methods:

  • Review of current research on MC4R genetics and function.
  • Analysis of drug development approaches targeting the MC4R pathway.
  • Evaluation of the role of MC4R in energy balance and adiposity.

Main Results:

  • MC4R is a key regulator of body weight and energy expenditure.
  • Mutations in MC4R lead to severe obesity.
  • Pharmacological targeting of MC4R shows promise for treating obesity.

Conclusions:

  • The MC4R is a validated and critical target for obesity pharmacotherapy.
  • Developing MC4R-targeting drugs could provide effective treatments for monogenic and potentially other forms of obesity.
Keywords:
cheminformatics computational techniques drug design virtual screening therapeutics machine learning

More Related Videos

A Robust Discovery Platform for the Identification of Novel Mediators of Melanoma Metastasis07:41

A Robust Discovery Platform for the Identification of Novel Mediators of Melanoma Metastasis

Published on: March 8, 2022

2.6K
A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 406:56

A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4

Published on: March 10, 2018

13.9K

Related Concept Videos

Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous...
2.9K
Drug-Receptor Interactions01:29

Drug-Receptor Interactions

Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue....
6.1K
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
8.8K
The Two-State Receptor Model01:29

The Two-State Receptor Model

The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
2.5K