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Related Concept Videos

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...
Lipids as Anchors01:32

Lipids as Anchors

In the plasma membrane, the lipids forming the bilayer can also act as an anchor to tether proteins to the membrane. The three main types of lipid anchors found in eukaryotes are – prenyl groups, fatty acyl groups, and glycosylphosphatidylinositol or GPI groups. Prenyl and fatty acyl groups act as anchors on the cytosolic surface of the membrane, whereas GPI anchors proteins on the extracellular side.
The carboxy-terminal of most of the prenylated proteins, such as Ras proteins, contains the...
Overview of Lipid Metabolism01:24

Overview of Lipid Metabolism

Lipid metabolism is a crucial process in the human body that involves the synthesis and degradation of lipids. This process is essential for energy production, cell membrane formation, and hormone production, among other functions.
Lipolysis: The Breakdown of Lipids:
Lipolysis is the process of breaking down lipids, particularly triglycerides, into glycerol and fatty acids. This process typically occurs in the adipose tissue and is triggered by various hormones, including glucagon and...
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:
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

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 rapamycin-insensitive companion...
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

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

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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Updated: May 24, 2026

Lipidomics and Transcriptomics in Neurological Diseases
09:58

Lipidomics and Transcriptomics in Neurological Diseases

Published on: March 18, 2022

Targeting protein lipidation in disease.

Marilyn D Resh1

  • 1Cell Biology Program, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, Box 143, New York, NY 10065, USA. m-resh@ski.mskcc.org

Trends in Molecular Medicine
|February 21, 2012
PubMed
Summary

Lipid modifications like myristoylation and prenylation regulate proteins. Inhibitors targeting these processes show potential for treating infectious diseases, cancer, and rare aging syndromes.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • Lipid modifications (fatty acids, isoprenoids) are crucial for protein function.
  • These modifications regulate protein structure, localization, and activity.
  • Dysregulation of protein lipidation is implicated in various human diseases.

Purpose of the Study:

  • To review recent advancements in identifying protein lipidation inhibitors.
  • To explore the therapeutic potential of these inhibitors in human diseases.
  • To highlight novel agents targeting specific lipid modification pathways.

Main Methods:

  • Literature review of recent research on protein lipidation inhibitors.
  • Analysis of studies investigating the effects of inhibitors on disease models.

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Optimized Incorporation of Alkynyl Fatty Acid Analogs for the Detection of Fatty Acylated Proteins using Click Chemistry
07:27

Optimized Incorporation of Alkynyl Fatty Acid Analogs for the Detection of Fatty Acylated Proteins using Click Chemistry

Published on: April 9, 2021

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Last Updated: May 24, 2026

Lipidomics and Transcriptomics in Neurological Diseases
09:58

Lipidomics and Transcriptomics in Neurological Diseases

Published on: March 18, 2022

Optimized Incorporation of Alkynyl Fatty Acid Analogs for the Detection of Fatty Acylated Proteins using Click Chemistry
07:27

Optimized Incorporation of Alkynyl Fatty Acid Analogs for the Detection of Fatty Acylated Proteins using Click Chemistry

Published on: April 9, 2021

  • Identification of key protein lipidation pathways and their targeted inhibitors.
  • Main Results:

    • Myristoylation inhibitors demonstrate efficacy against human pathogens.
    • Prenylation inhibitors show limited success in cancer but potential for progeria.
    • New agents targeting palmitoylation of Ras, Wnt, and Hh proteins have emerged.

    Conclusions:

    • Inhibitors of protein lipidation represent a promising therapeutic strategy.
    • Targeting myristoylation, prenylation, and palmitoylation offers diverse treatment possibilities.
    • Further development of these agents could lead to next-generation chemotherapeutics.