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Related Concept Videos

Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

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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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Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

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Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
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Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu01:29

Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu

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Genetic variations significantly influence drug response through pharmacokinetics, receptor interactions, and biologic milieu modifications. Pharmacokinetic alterations impact drug metabolism and clearance, affecting efficacy and toxicity. Variants in drug-metabolizing enzymes, such as CYP2C9 and CYP2C19, alter drug activation and elimination. For example, CYP2C9 loss-of-function variants require lower warfarin doses to prevent excessive bleeding, while CYP2C19 variants reduce clopidogrel...
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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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Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters01:16

Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters

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The pharmacogenetics of drug transporters is increasingly recognized as a critical factor influencing interindividual variability in drug absorption, distribution, and elimination. These membrane-bound proteins regulate drugs' movement across cellular barriers by actively pumping them out (efflux) or facilitating their uptake (influx). Among the major transporter families, ATP-binding cassette (ABC) and solute carrier (SLC) transporters play particularly prominent roles. Genetic polymorphisms...
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Principles of Pharmacogenetics: Types of Genetic Variants01:27

Principles of Pharmacogenetics: Types of Genetic Variants

143
The human genome is over 99.9% identical between individuals, yet genetic differences exist at millions of bases. The human genome contains approximately 3 million variant positions per individual, many of which are heterozygous, contributing to genetic diversity and individual traits. Genetic variations include single-nucleotide polymorphisms (SNPs), insertions, deletions, and copy number variations (CNVs).SNPs, the most common variation, involve single-base changes in DNA. These can be...
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Related Experiment Video

Updated: May 5, 2026

Direct Intraventricular Delivery of Drugs to the Rodent Central Nervous System
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NAD as a genotype-specific drug target.

Szu-Chieh Mei1, Charles Brenner

  • 1Department of Biochemistry, Carver College of Medicine, University of Iowa, Iowa City, IA 52242, USA.

Chemistry & Biology
|November 26, 2013
PubMed
Summary

Researchers found STF-118804, a nicotinamide phosphoribosyltransferase inhibitor, selectively targets mixed-lineage leukemia with MLL rearrangements. This highlights the potential of targeting NAD for specific cancer therapies.

Area of Science:

  • Biochemistry
  • Oncology
  • Genetics

Background:

  • Mixed-lineage leukemia (MLL) with chromosomal rearrangements is a challenging cancer subtype.
  • Targeting specific metabolic pathways offers a promising strategy for cancer therapy.

Purpose of the Study:

  • To identify novel therapeutic agents for MLL-rearranged leukemias.
  • To explore the role of nicotinamide phosphoribosyltransferase (NAMPT) in cancer cell survival.

Main Methods:

  • High-throughput chemical and genetic screening.
  • Cell type-specific drug screening.
  • Biochemical assays to assess enzyme inhibition.

Main Results:

  • STF-118804 was identified as a potent inhibitor of NAMPT.

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  • STF-118804 demonstrated cell type-specific inhibition of MLL-rearranged leukemia cells.
  • The study suggests NAMPT is crucial for the survival of these specific cancer cells.

    • Conclusions:

    • STF-118804 is a promising candidate for targeted therapy in MLL-rearranged leukemias.
    • Nicotinamide adenine dinucleotide (NAD) metabolism represents a viable target for specific cancer treatments.