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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.
There are several types of targeted therapies against specific...
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...
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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Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
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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...
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...

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Updated: May 31, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
06:26

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

Published on: May 16, 2021

Targeting cancer using fragment based drug discovery.

Andrew P Turnbull1, Susan M Boyd

  • 1CRT Discovery Laboratories, Department of Crystallography, Birkbeck College, University of London, Malet Street, London, WC1E 7HX. aturnbull@cancertechnology.com

Anti-Cancer Agents in Medicinal Chemistry
|June 29, 2011
PubMed
Summary

Fragment-based drug discovery is a popular method for identifying drug leads. This approach uses small compounds to find starting points for drug design, with several programs now in clinical trials.

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Last Updated: May 31, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
06:26

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Published on: May 16, 2021

NMR-Based Fragment Screening in a Minimum Sample but Maximum Automation Mode
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Published on: June 4, 2021

Workflow and Tools for Crystallographic Fragment Screening at the Helmholtz-Zentrum Berlin
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Workflow and Tools for Crystallographic Fragment Screening at the Helmholtz-Zentrum Berlin

Published on: March 3, 2021

Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Biochemistry

Background:

  • Fragment-based drug discovery (FBDD) has emerged as a significant approach in pharmaceutical research.
  • It offers an alternative and complementary strategy to traditional high-throughput screening (HTS).
  • FBDD utilizes small molecule fragments to identify initial hits for drug design.

Purpose of the Study:

  • To highlight the advancements and growing popularity of FBDD.
  • To discuss the capabilities of FBDD in identifying starting points for structure-based drug design.
  • To address the challenges and strategies within the FBDD methodology.

Main Methods:

  • Utilizes small libraries of low molecular weight compounds.
  • Employs sensitive detection methods for weak fragment-protein interactions.
  • Focuses on strategies for fragment-to-lead optimization.

Main Results:

  • FBDD enables rapid identification of starting points for drug design.
  • Sensitive detection of weak interactions is crucial for fragment screening.
  • Development of strategies to grow fragments into drug candidates is key.
  • Several FBDD programs have advanced compounds into clinical trials, validating the approach.

Conclusions:

  • Fragment-based drug discovery is a validated and increasingly popular method in the pharmaceutical industry.
  • The approach effectively identifies starting points for structure-based drug design.
  • Overcoming challenges in fragment detection and optimization is critical for success.