Page last updated: 2024-10-24

macromolecule depalmitoylation

Definition

Target type: biologicalprocess

The removal of palymitoyl groups from a macromolecule. [GOC:dos]

Depalmitoylation is a crucial biological process that involves the removal of palmitic acid, a saturated fatty acid, from a target protein or lipid. Palmitoylation, the attachment of palmitic acid, is a common post-translational modification that plays a vital role in regulating protein function, localization, and stability. Depalmitoylation serves as a counteracting mechanism, reversing the effects of palmitoylation and influencing cellular processes.

The enzymatic removal of palmitate is primarily carried out by a family of cysteine palmitoyl acyltransferases (CPTs), also known as depalmitoylases. These enzymes recognize and cleave the thioester bond between the palmitic acid and the cysteine residue on the target molecule.

The process of depalmitoylation is highly regulated and involves a complex interplay of factors, including:

1. **Specificity of CPTs:** Different CPTs exhibit varying substrate specificities, targeting particular proteins or lipids based on their sequence and structural features.

2. **Cellular Localization:** CPTs are often localized to specific cellular compartments, such as the plasma membrane, endoplasmic reticulum, or Golgi apparatus, where they can access their target substrates.

3. **Regulatory Signals:** Depalmitoylation can be triggered by various stimuli, including changes in cellular signaling pathways, environmental cues, or stress responses.

4. **Reversible Modification:** Depalmitoylation is a reversible process, and the balance between palmitoylation and depalmitoylation dynamically regulates protein function and cellular processes.

The biological significance of depalmitoylation is widespread, affecting a variety of cellular functions, including:

1. **Protein Trafficking:** Depalmitoylation can alter protein localization by detaching them from membranes, facilitating their transport to different cellular compartments.

2. **Signal Transduction:** Depalmitoylation can modulate the activity of signaling proteins, influencing their interactions with downstream targets and cellular responses.

3. **Membrane Dynamics:** Depalmitoylation can regulate the composition and fluidity of cellular membranes by removing palmitate from membrane-associated proteins and lipids.

4. **Cellular Processes:** Depalmitoylation plays crucial roles in diverse cellular processes, such as cell growth, differentiation, apoptosis, and neurotransmission.

Understanding the intricate mechanisms of depalmitoylation is essential for gaining insights into the regulation of various cellular functions and for developing therapeutic strategies targeting aberrant palmitoylation in disease states.'
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Proteins (1)

ProteinDefinitionTaxonomy
Lysophosphatidylserine lipase ABHD12A lysophosphatidylserine lipase ABHD12 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8N2K0]Homo sapiens (human)

Compounds (3)

CompoundDefinitionClassesRoles
1,6-bis(cyclohexyloximinocarbonyl)hexane1,6-bis(cyclohexyloximinocarbonyl)hexane: selective inhibitor of canine platelet diglyceride lipasecarbamate ester;
organonitrogen compound
dronabinolDelta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy.

Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.
benzochromene;
diterpenoid;
phytocannabinoid;
polyketide
cannabinoid receptor agonist;
epitope;
hallucinogen;
metabolite;
non-narcotic analgesic
orlistatorlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug.

Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.
beta-lactone;
carboxylic ester;
formamides;
L-leucine derivative
anti-obesity agent;
bacterial metabolite;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor