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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:
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
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Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
Structure-Activity Relationships and Drug Design01:28

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Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
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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.
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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...

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Related Experiment Video

Updated: May 11, 2026

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
07:42

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Published on: September 19, 2018

Tankyrases as drug targets.

Lari Lehtiö1, Nai-Wen Chi, Stefan Krauss

  • 1Biocenter Oulu and Department of Biochemistry, University of Oulu, Oulu, Finland. lari.lehtio@oulu.fi

The FEBS Journal
|May 8, 2013
PubMed
Summary

Tankyrase 1 and 2 are enzymes involved in crucial cell functions and disease processes. Inhibitors targeting tankyrases show promise as cancer therapeutics by modulating enzyme activity.

Keywords:
Wnt signallingcancerdiphtheria toxin-like ADP-ribosyltransferase (ARTD)drug discoverymitosispoly(ADP-ribose) polymerase (PARP)tankyrasetelomerevesicle trafficking

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Published on: August 27, 2019

Area of Science:

  • Biochemistry and Molecular Biology
  • Enzymology
  • Drug Discovery

Background:

  • Tankyrases (TNKS1/2) are poly(ADP-ribosyl)ases with unique structural domains.
  • They play roles in cellular processes like telomere maintenance, cell division, and signaling pathways.
  • Dysregulation of tankyrase activity is linked to various diseases, making them potential drug targets.

Purpose of the Study:

  • To review the structural features and cellular functions of tankyrases.
  • To discuss the development and mechanisms of tankyrase inhibitors.
  • To highlight the therapeutic potential of tankyrase inhibitors, particularly in oncology.

Main Methods:

  • Structural analysis of tankyrase catalytic domains.
  • Biochemical assays to characterize enzyme activity and inhibitor binding.
  • Review of existing literature on tankyrase inhibitors and their applications.

Main Results:

  • Tankyrase inhibitors exhibit selectivity based on binding to distinct subsites within the NAD+ groove.
  • Inhibitors targeting the nicotinamide or adenosine subsites, or both, have been developed.
  • These inhibitors demonstrate potential as chemical probes and lead compounds for cancer therapy.

Conclusions:

  • Tankyrase inhibitors offer a promising avenue for therapeutic intervention in cancers.
  • Understanding inhibitor binding modes is key to developing potent and selective drugs.
  • Further research into tankyrase inhibitors could lead to novel cancer treatments.