Target type: biologicalprocess
The covalent attachment of lipid groups to an amino acid in a protein. [GOC:jl]
Protein lipidation is a crucial post-translational modification process that involves the covalent attachment of lipid molecules to proteins. This modification plays a critical role in regulating various cellular processes, including protein trafficking, membrane association, signal transduction, and protein-protein interactions.
There are several types of lipidation, each with unique mechanisms and functional consequences:
**1. Myristoylation:** Involves the attachment of myristate, a 14-carbon saturated fatty acid, to the N-terminal glycine residue of a protein. This modification typically occurs co-translationally and is often involved in protein targeting to membranes and protein-protein interactions.
**2. Palmitoylation:** This reversible modification involves the attachment of palmitic acid, a 16-carbon saturated fatty acid, to cysteine residues within a protein. Palmitoylation can occur at the plasma membrane and is often involved in membrane association, protein trafficking, and signal transduction.
**3. Prenylation:** This process involves the attachment of isoprenoid lipids, such as farnesyl or geranylgeranyl, to cysteine residues near the C-terminus of a protein. Prenylation is often involved in protein-protein interactions, membrane association, and signal transduction.
**4. Glycosylphosphatidylinositol (GPI) anchoring:** This modification involves the attachment of a GPI anchor, a complex glycolipid, to the C-terminus of a protein. GPI anchoring is typically involved in targeting proteins to the outer leaflet of the plasma membrane, where they can interact with other membrane-associated proteins.
**5. Fatty acylation:** This term encompasses a range of lipid modifications, including myristoylation and palmitoylation, that involve the attachment of fatty acids to proteins. Fatty acylation is often involved in protein membrane association and protein-protein interactions.
The specific type of lipidation and the location of lipid attachment within a protein determine the functional consequences of the modification. For instance, myristoylation and palmitoylation can target proteins to specific membrane compartments, while prenylation can modulate protein-protein interactions.
Overall, protein lipidation is a highly regulated process that plays a vital role in maintaining cellular function and homeostasis. Understanding the molecular mechanisms and functional consequences of lipidation is crucial for gaining insights into various cellular processes and for developing therapeutic strategies targeting these modifications.'
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Protein | Definition | Taxonomy |
---|---|---|
Protein-serine O-palmitoleoyltransferase porcupine | A protein-serine O-palmitoleoyltransferase porcupine that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9H237] | Homo sapiens (human) |
Phosphatidylinositol 3-kinase catalytic subunit type 3 | A phosphatidylinositol 3-kinase catalytic subunit type 3 that is encoded in the genome of human. [PRO:DNx] | Homo sapiens (human) |
Ceramide glucosyltransferase | A ceramide glucosyltransferase that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16739] | Homo sapiens (human) |
Ubiquitin-like modifier-activating enzyme ATG7 | A ubiquitin-like modifier-activating enzyme ATG7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O95352] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
---|---|---|---|
1-deoxynojirimycin | 1-deoxy-nojirimycin: structure in first source duvoglustat : An optically active form of 2-(hydroxymethyl)piperidine-3,4,5-triol having 2R,3R,4R,5S-configuration. | 2-(hydroxymethyl)piperidine-3,4,5-triol; piperidine alkaloid | anti-HIV agent; anti-obesity agent; bacterial metabolite; EC 3.2.1.20 (alpha-glucosidase) inhibitor; hepatoprotective agent; hypoglycemic agent; plant metabolite |
miglustat | miglustat : A hydroxypiperidine that is deoxynojirimycin in which the amino hydrogen is replaced by a butyl group. miglustat: a glucosylceramide synthase inhibitor | piperidines; tertiary amino compound | anti-HIV agent; EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor |
migalastat | migalastat: a potent inhibitor of glycolipid biosynthesis | piperidines | |
miglitol | piperidines | ||
N-(6-methyl-1,3-benzothiazol-2-yl)-2-[(4-oxo-3-phenyl-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)thio]acetamide | organic heterobicyclic compound; organonitrogen heterocyclic compound; organosulfur heterocyclic compound | ||
ML162 | ML162 : A monochlorobenzene that is benzene substituted by (chloroacetyl){2-oxo-2-[(2-phenylethyl)amino]-1-(thiophen-2-yl)ethyl}amino, chloro and methoxy groups at positions 1, 3 and 4, respectively. It is a covalent inhibitor of glutathione peroxidase 4 (GPX4) that induces ferroptosis in cells. | monochlorobenzenes; monomethoxybenzene; organochlorine compound; secondary carboxamide; tertiary carboxamide; thiophenes | EC 1.11.1.9 (glutathione peroxidase) inhibitor; ferroptosis inducer |
n-(5-adamantane-1-yl-methoxy-pentyl)deoxynojirimycin | |||
PI3-Kinase alpha Inhibitor 2 | organic heterobicyclic compound; organonitrogen heterocyclic compound; organosulfur heterocyclic compound | ||
l-altro-1-deoxynojirimycin | L-altro-1-deoxynojirimycin: structure in first source | ||
idelalisib | idelalisib : A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indolent non-Hodgkin's lymphoma and relapsed chronic lymphocytic leukemia. idelalisib: an antineoplastic agent and p110delta inhibitor; structure in first source | aromatic amine; organofluorine compound; purines; quinazolines; secondary amino compound | antineoplastic agent; apoptosis inducer; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
zstk474 | ZSTK-474 : A triamino-1,3,5-triazine that is 1,3,5-triazine in which two of the hydrogens have been replaced by morpholin-4-yl groups while the third hydrogen has been replaced by a 2-(difluoromethyl)benzimidazol-1-yl group. It is an inhibitor of phosphatidylinositol 3-kinase. | benzimidazoles; morpholines; organofluorine compound; triamino-1,3,5-triazine | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
dactolisib | dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment. dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR | imidazoquinoline; nitrile; quinolines; ring assembly; ureas | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor |
ku 60019 | |||
buparlisib | NVP-BKM120: a pan class I PI3 kinase inhibitor with antineoplastic activity; structure in first source | aminopyridine; aminopyrimidine; morpholines; organofluorine compound | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
pevonedistat | pevonedistat : A pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidine which is substituted by a (1S)-2,3-dihydro-1H-inden-1-ylnitrilo group at position 4 and by a (1S,3S,4S)-3-hydroxy-4-[(sulfamoyloxy)methyl]cyclopentyl group at position 7. It is a potent and selective NEDD8-activating enzyme inhibitor with an IC50 of 4.7 nM, and currently under clinical investigation for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndromes. pevonedistat: a potent and selective inhibitor of NAE (NEDD8-activating enzyme) | cyclopentanols; indanes; pyrrolopyrimidine; secondary amino compound; sulfamidate | antineoplastic agent; apoptosis inducer |
gdc 0941 | pictrelisib : A sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring. | indazoles; morpholines; piperazines; sulfonamide; thienopyrimidine | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
gdc 0980 | |||
azd2014 | vistusertib: potent and selective dual mTORC1 and mTORC2 inhibitor; structure in first source | ||
pki 587 | gedatolisib: inhibits both phosphatidylinositol 3-kinase and mTOR; structure in first source | ||
5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine | sapanisertib: an mTOR inhibitor | benzoxazole | |
lgk974 | LGK974 : A carboxamide, the structure of which is that of acetamide substituted on carbon by a 2',3-dimethyl-2,4'-bipyridin-5-yl group and on nitrogen by a 5-(pyrazin-2-yl)pyridin-2-yl group. It is a highly potent, selective and orally bioavailable Porcupine inhibitor (a Wnt signalling inhibitor). LGK974: a potent and specific small-molecule inhibitor of Porcupine (PORCN) acyltransferase | bipyridines; pyrazines; pyridines; secondary carboxamide | Wnt signalling inhibitor |
ch 5132799 | CH 5132799: structure in first source | ||
torin 1 | torin 1 : A member of the class of pyridoquinolines that is 9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2-one bearing an additional 4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl substituent at position 1. It is a potent inhibitor of mTOR and exhibits anti-cancer properties. | N-acylpiperazine; N-arylpiperazine; organofluorine compound; pyridoquinoline; quinolines | antineoplastic agent; mTOR inhibitor |
gdc-0032 | |||
spautin-1 | |||
torin 2 | torin 2 : A member of the class of pyridoquinolines that is benzo[h][1,6]naphthyridin-2-one carrying additional 3-(trifluoromethyl)phenyl and 6-aminopyridin-3-yl substituents at positions 1 and 9 respectively. It is a potent inhibitor of mTOR and exhibits anti-cancer properties. | aminopyridine; organofluorine compound; primary amino compound; pyridoquinoline | antineoplastic agent; mTOR inhibitor |
cudc-907 | |||
sar245408 | |||
byl719 | proline derivative | ||
amg 511 | AMG 511: structure in first source | ||
wnt-c59 | 2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide: a PORCN acyltransferase inhibitor; structure in first source | ||
cc-223 | |||
sar405 | SAR405: a Vps34 inhibitor with antineoplastic activity; structure in first source |