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Related Concept Videos

Targets for Drug Action: Overview01:26

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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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Drug Discovery: Overview01:26

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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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Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
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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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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Developing drugs for the 'undruggable'.

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Scientists are exploring how to target

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Area of Science:

  • Biochemistry and Molecular Biology
  • Drug Discovery and Development
  • Genomics and Proteomics

Background:

  • The human interactome contains approximately 650,000 protein-protein interactions (PPIs).
  • Many of these PPIs are currently considered 'undruggable' due to their complex nature.
  • Identifying novel therapeutic targets within these PPIs is a significant challenge in medicine.

Discussion:

  • This research investigates strategies to overcome the 'undruggable' nature of specific protein-protein interactions.
  • Exploring novel chemical modalities and computational approaches to modulate PPIs.
  • Understanding the structural and dynamic features that dictate PPI druggability.

Key Insights:

  • Emerging techniques are enabling the targeting of previously intractable PPIs.
  • Modulating PPIs offers a new frontier for treating diseases with unmet medical needs.
  • The transition from 'undruggable' to 'druggable' involves innovative drug design and screening.

Outlook:

  • Developing a new class of therapeutics that target PPIs.
  • Expanding the scope of druggable targets in the human interactome.
  • Potential for personalized medicine by targeting disease-specific PPIs.