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Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

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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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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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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.
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The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a...
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Related Experiment Video

Updated: Dec 23, 2025

Using Human Differentially Expressed Gene Lists to Perform Downstream Pathway Enrichment Analysis and Target Prioritization
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Molecular Targets Beyond the Big 3.

Karen L Reckamp1

  • 1Cedars-Sinai Medical Center, 8700 Beverly Boulevard, Los Angeles, CA 90048, USA.

Thoracic Surgery Clinics
|April 25, 2020
PubMed
Summary

Lung cancer is a complex genomic disease. Exploring genetic alterations beyond EGFR, ALK, and ROS1 is crucial for developing new precision therapies to improve patient survival.

Area of Science:

  • Oncology
  • Genomics
  • Molecular Biology

Background:

  • Lung cancer is a heterogeneous genomic disease, with smoking as the primary cause.
  • Genetic susceptibility and environmental factors contribute to 10-15% of lung cancer cases.
  • Current targeted therapies are effective for tumors with specific oncogenic drivers, improving patient survival.

Purpose of the Study:

  • To expand the understanding of genetic alterations in non-small cell lung cancer (NSCLC) beyond commonly targeted genes.
  • To identify novel therapeutic targets and agents for NSCLC.
  • To discuss the challenges and future directions in precision therapy for lung cancer.

Main Methods:

  • Review of current literature on genetic alterations in NSCLC.
  • Analysis of emerging targeted therapies for NSCLC.
Keywords:
BRAFGene mutationsHER2KRASMETNTRKRETTargeted therapy

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  • Discussion of the complexity of lung cancer genomics.

    • Main Results:

    • Genetic alterations beyond EGFR, ALK, and ROS1 are common in NSCLC.
    • These additional alterations represent potential targets for novel therapeutic agents.
    • Precision therapy requires continued investment to address lung cancer's complexity.

    Conclusions:

    • Understanding genetic diversity in lung cancer is key to developing more effective treatments.
    • Targeting genetic alterations beyond EGFR, ALK, and ROS1 offers opportunities to improve outcomes for a broader patient population.
    • Continued research and investment in precision oncology are essential for advancing lung cancer care.