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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...
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...
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:
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...
Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

Site-Targeted Drug Delivery Systems: Polymeric Carriers

Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
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...

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Related Experiment Video

Updated: Jun 5, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
05:28

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Published on: August 27, 2019

Do PAKs make good drug targets?

Zhuo-Shen Zhao, Ed Manser

    F1000 Biology Reports
    |December 22, 2010
    PubMed
    Summary
    This summary is machine-generated.

    p21-activated kinases (PAKs) are crucial in cancer. A new inhibitor, PF-3758309, shows promise by targeting PAKs to control tumor cell proliferation and survival, particularly in NF2-deficient cancers.

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    Published on: December 1, 2020

    Area of Science:

    • Oncology
    • Molecular Biology
    • Biochemistry

    Background:

    • p21-activated kinases (PAKs) are key signaling proteins downstream of Rho-family GTPases.
    • PAKs play critical roles in both the initiation and progression of various cancers.
    • The six mammalian PAK isoforms are categorized into two groups, both presenting therapeutic opportunities.

    Purpose of the Study:

    • To introduce and evaluate PF-3758309, a novel PAK inhibitor with high selectivity and potency.
    • To confirm the therapeutic potential of PAK inhibition in combating specific tumor types.
    • To explore the utility of NF2-deficient models for PAK inhibitor studies.

    Main Methods:

    • Development and characterization of the PAK inhibitor PF-3758309.
    • Experimental validation of PF-3758309's efficacy in preclinical cancer models.
    • Investigation of the molecular mechanisms underlying PAK inhibition's effects on cancer cells.

    Main Results:

    • PF-3758309 demonstrates significant selectivity and potency against PAKs.
    • Inhibition of PAKs using PF-3758309 effectively combats certain tumors.
    • The anti-tumor activity is associated with the modulation of cancer cell proliferation and survival pathways.
    • The Ras-Rac-PAK pathway, often dysregulated in NF2 loss, is a relevant target system.

    Conclusions:

    • PF-3758309 represents a promising therapeutic agent for PAK-targeted cancer therapy.
    • PAK inhibition is a validated strategy for controlling tumor growth and enhancing survival.
    • NF2-deficient cancers present a suitable context for evaluating the clinical efficacy of PAK inhibitors like PF-3758309.