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Related Concept Videos

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...
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...
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...
Overview of DNA Repair02:25

Overview of DNA Repair

In order to be passed through generations, genomic DNA must be undamaged and error-free. However, every day, DNA in a cell undergoes several thousand to a million damaging events by natural causes and external factors. Ionizing radiation such as UV rays, free radicals produced during cellular respiration, and hydrolytic damage from metabolic reactions can alter the structure of DNA. Damages caused include single-base alteration, base dimerization, chain breaks, and cross-linkage.
Chemically...
Principles of Drug Action01:24

Principles of Drug Action

Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
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...

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Related Experiment Video

Updated: May 23, 2026

Genome-wide Mapping of Drug-DNA Interactions in Cells with COSMIC (Crosslinking of Small Molecules to Isolate Chromatin)
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Genome-wide Mapping of Drug-DNA Interactions in Cells with COSMIC (Crosslinking of Small Molecules to Isolate Chromatin)

Published on: January 20, 2016

Small molecule drugs - optimizing DNA damaging agent-based therapeutics.

John A Hartley1, Daniel Hochhauser

  • 1Cancer Research UK Drug-DNA Interactions Research Group, UCL Cancer Institute, London WC1E 6BT, UK. john.hartley@ucl.ac.uk

Current Opinion in Pharmacology
|April 17, 2012
PubMed
Summary

Novel DNA-targeted chemotherapy combinations show promise against resistant tumors. Understanding drug interactions is key to developing effective cancer treatments with fewer side effects.

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Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • DNA-targeted chemotherapies are crucial for treating solid tumors and hematologic malignancies.
  • Conventional chemotherapy faces resistance, driving the need for novel agents and combinations.
  • Developing selective DNA-damaging drugs with reduced side effects is an ongoing challenge.

Purpose of the Study:

  • To review current DNA-targeted agents and their combinations in clinical evaluation.
  • To explore the mechanistic basis of interactions between novel targeted agents and DNA-interactive drugs.
  • To inform the design of optimal combination therapies for improved clinical outcomes.

Main Methods:

  • Review of recent studies on novel DNA-targeted agents and combination therapies.
  • Analysis of clinical evaluations of agents like trabectedin, bendamustine, and SG2000.
  • Examination of interactions between DNA damaging drugs and novel agents (e.g., kinase inhibitors, antibodies).

Main Results:

  • Novel combinations of cytotoxic chemotherapy demonstrate activity in drug-resistant tumors.
  • Trabectedin, bendamustine, and SG2000 represent diverse classes of DNA-targeted agents in clinical trials.
  • Combination of DNA damaging drugs with novel targeted agents is an emerging strategy.

Conclusions:

  • Understanding drug interactions is critical for optimizing combination chemotherapy.
  • Novel targeted agents combined with DNA-damaging drugs hold potential for enhanced cancer treatment.
  • Further research into these combinations will maximize clinical benefit and patient outcomes.