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Related Concept Videos

Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates these...
Drugs Affecting Neurotransmitter Release or Uptake01:21

Drugs Affecting Neurotransmitter Release or Uptake

Certain drugs can affect how neurotransmitters called catecholamines, are released or taken back up in the adrenergic neuron. They can have different effects on the body's sympathetic transmission. Reserpine, a natural compound found in the Rauwolfia shrub, blocks a transporter called vesicular monoamine transporter (VMAT), which leads to a buildup of catecholamines in the cell and reduces sympathetic transmission. Another drug called guanethidine works in multiple ways, including blocking...
Drug Toxicity: Overview01:00

Drug Toxicity: Overview

Drug toxicity quantifies the harm a compound causes to an organism, varying by dose and potentially impacting whole systems or specific organs like the liver. Toxic reactions may arise from venomous insect or spider bites, with effects ranging from mild symptoms to severe outcomes such as brain damage or death. Common forms of acute poisoning include ethanol intoxication and overdose of pain or fever medications, with substances like GHB and heroin being particularly lethal at doses close to...
Cholinergic Receptors: Muscarinic01:25

Cholinergic Receptors: Muscarinic

The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine. 
The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+. Activation...
Non-gated Ion Channels01:24

Non-gated Ion Channels

Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.

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Related Experiment Video

Updated: Jul 3, 2026

Development and Standardization of an Ex Vivo Micromethod for Intracellular Quantification of Vincristine in Primary ALL Cells by LC-MS/MS
08:24

Development and Standardization of an Ex Vivo Micromethod for Intracellular Quantification of Vincristine in Primary ALL Cells by LC-MS/MS

Published on: January 23, 2026

[Vinca alkaloid and MDR1].

Nagio Takigawa1, Mitsune Tanimoto

  • 1Dept. of Respiratory Medicine, Okayama University Hospital, Okayama, Japan.

Gan to Kagaku Ryoho. Cancer & Chemotherapy
|July 18, 2008
PubMed
Summary
This summary is machine-generated.

Vinca alkaloids, like vincristine, target tubulin. Genetic variations in the MDR1 gene, which encodes P-glycoprotein (P-gp), may influence chemotherapy efficacy and toxicity.

Related Experiment Videos

Last Updated: Jul 3, 2026

Development and Standardization of an Ex Vivo Micromethod for Intracellular Quantification of Vincristine in Primary ALL Cells by LC-MS/MS
08:24

Development and Standardization of an Ex Vivo Micromethod for Intracellular Quantification of Vincristine in Primary ALL Cells by LC-MS/MS

Published on: January 23, 2026

Area of Science:

  • Pharmacogenomics
  • Molecular Biology
  • Oncology

Context:

  • Vinca alkaloids are crucial chemotherapy agents that inhibit microtubule formation by binding to tubulin.
  • P-glycoprotein (P-gp), encoded by the MDR1 gene, is an efflux transporter implicated in multidrug resistance and found in normal tissues.
  • Single nucleotide polymorphisms (SNPs) in the MDR1 gene, specifically at exons 12, 21, and 26, are well-documented and can lead to amino acid substitutions.

Purpose:

  • To explore the relationship between MDR1 gene polymorphisms and haplotypes and the pharmacodynamics of vinca alkaloid chemotherapy.
  • To investigate how these genetic variations influence drug efficacy and toxicity.
  • To understand the impact of P-gp expression levels on vincristine pharmacokinetics and patient outcomes.

Summary:

  • This research examines the impact of specific single nucleotide polymorphisms (SNPs) and haplotypes within the MDR1 gene on the effectiveness and side effects of vinca alkaloid chemotherapy.
  • Studies have identified key MDR1 SNPs (e.g., C1236T, G2677T/A, C3435T) and their association with altered amino acid sequences, potentially affecting P-gp function.
  • The correlation between MDR1 haplotypes and vincristine elimination half-life has been reported, suggesting a genetic basis for variable drug response.

Impact:

  • Understanding MDR1 genetic variations can lead to personalized chemotherapy regimens, optimizing treatment efficacy and minimizing toxicity for cancer patients.
  • This research contributes to the field of pharmacogenomics, providing insights into drug metabolism and transport mechanisms.
  • The findings may facilitate the development of predictive biomarkers for patient response to vinca alkaloid-based therapies, improving clinical decision-making.