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Related Concept Videos

Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Integrins01:10

Integrins

Animal and protozoan cells do not have cell walls to help maintain shape and provide structural stability. Instead, these eukaryotic cells secrete a sticky mass of carbohydrates and proteins into the spaces between adjacent cells. This network of proteins and molecules is called an extracellular matrix or ECM.
Some ECM proteins assemble into a basement membrane to which the remaining components adhere. Proteoglycans typically form the bulk of the ECM while fibrous proteins, like collagen,...
Activation of Integrins01:15

Activation of Integrins

Integrins bind ligands and transmit information from outside the cell to inside or vice-versa through an "outside-in signaling" or "inside-out signaling."
In "outside-in signaling," external factors in the extracellular space bind to exposed ligand binding sites on integrins. This causes the inactive protein to undergo a conformational change to become active. Integrins are often clustered on the cell membrane. Repetitive and regularly spaced ligand binding events provide an effective stimulus.
Intracellular Signaling Affects Focal Adhesions01:17

Intracellular Signaling Affects Focal Adhesions

Integrins act both as extracellular input receivers and as intracellular processing activators. As their name suggests, integrins are entirely integrated into the membrane structure. Their hydrophobic membrane-spanning regions interact with the phospholipid bilayer's hydrophobic region. These membrane receptors provide extracellular attachment sites for effectors like hormones and growth factors. They activate intracellular response cascades when their effectors are bound and active.
Some...
Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...

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Related Experiment Video

Updated: May 22, 2026

A Flow Cytometry-Based High-Throughput Technique for Screening Integrin-Inhibitory Drugs
04:15

A Flow Cytometry-Based High-Throughput Technique for Screening Integrin-Inhibitory Drugs

Published on: February 2, 2024

Integrins as therapeutic targets.

Simon L Goodman1, Martin Picard

  • 1Department of Cellular Pharmacology - Oncology Platform, Merck KGaA, Frankfurterstrasse 250, 64271 Darmstadt, Germany. Simon.L.Goodman@merckgroup.com

Trends in Pharmacological Sciences
|May 29, 2012
PubMed
Summary
This summary is machine-generated.

Integrins regulate cell adhesion in development and disease. Numerous anti-integrin drugs are in clinical trials, highlighting their importance as cancer drug targets.

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Dynamic Adhesion Assay for the Functional Analysis of Anti-adhesion Therapies in Inflammatory Bowel Disease
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Dynamic Adhesion Assay for the Functional Analysis of Anti-adhesion Therapies in Inflammatory Bowel Disease

Published on: September 20, 2018

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A Flow Cytometry-Based High-Throughput Technique for Screening Integrin-Inhibitory Drugs
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Dynamic Adhesion Assay for the Functional Analysis of Anti-adhesion Therapies in Inflammatory Bowel Disease
08:27

Dynamic Adhesion Assay for the Functional Analysis of Anti-adhesion Therapies in Inflammatory Bowel Disease

Published on: September 20, 2018

Area of Science:

  • Molecular Biology
  • Cell Biology
  • Pharmacology

Background:

  • Integrins are key regulators of cell-cell and cell-extracellular matrix (ECM) interactions.
  • Dysfunctional integrin adhesion is implicated in various pathologies, including cancer, inflammation, and thrombotic diseases.
  • Integrins are accessible cell surface targets for pharmacological intervention.

Purpose of the Study:

  • To provide an overview of integrins as drug targets.
  • To focus on the role of integrins in cancer therapeutics.
  • To assess the scale of clinical development for anti-integrin drugs.

Main Methods:

  • Literature review of integrin function and therapeutic relevance.
  • Analysis of data from three major drug-trial databases.
  • Examination of approved integrin-targeting drugs and their market performance.

Main Results:

  • Integrin-targeting drugs have achieved significant clinical success, with five approved therapies generating over $1.5 billion in sales in 2010.
  • Approximately 260 anti-integrin drugs have entered clinical trials, indicating substantial research and development efforts.
  • Integrins represent a promising class of targets, particularly in the field of oncology.

Conclusions:

  • Integrins are crucial for normal biological processes and disease pathogenesis.
  • The extensive clinical pipeline underscores the therapeutic potential of targeting integrins.
  • Further development of integrin-targeting drugs, especially for cancer, is warranted.