3.1.-.- Ester bond enzymes

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3.1.-.- Ester bond enzymes

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Enzymes

3199

galactosamine (N-acetyl)-6-sulfatase Show summary »« Hide summary More detailed page go icon to follow link

palmitoyl-protein thioesterase 1 Show summary »« Hide summary

Target Id

3199

Nomenclature

palmitoyl-protein thioesterase 1

Genes

PPT1 (Hs), Ppt1 (Mm), Ppt1 (Rn)

Ensembl ID

ENSG00000131238 (Hs), ENSMUSG00000028657 (Mm), ENSRNOG00000012616 (Rn)

UniProtKB AC

P50897 (Hs), O88531 (Mm), A0JN20 (Rn)

EC number

3.1.2.22
Removes thioester-linked fatty acyl groups (e.g. palmitate) from modified cysteine residues in proteins/peptides during lysosomal degradation. Prefers acyl chain lengths of 14-18 carbons H₂O + S-hexadecanoyl-L-cysteinyl-[protein] = H⁺ + hexadecanoate + L-cysteinyl-[protein] [3]

Inhibitors

ezurpimtrostat [2]

Comment

Involved in the catabolism of lipid-modified proteins during lysosomal degradation and autophagy. Inhibitors of PPT1 enzyme activity disrupt lysosomal function and autophagy, and are being examined for antitumour potential [2] and antiviral activity against SARS-CoV-2 [1].

References

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1. Bestion E, Zandi K, Belouzard S, Andreani J, Lepidi H, Novello M, Rouquairol C, Baudoin JP, Rachid M, La Scola B et al.. (2022) GNS561 Exhibits Potent Antiviral Activity against SARS-CoV-2 through Autophagy Inhibition. Viruses, 14 (1). DOI: 10.3390/v14010132 [PMID:35062337]

2. Brun S, Bestion E, Raymond E, Bassissi F, Jilkova ZM, Mezouar S, Rachid M, Novello M, Tracz J, Hamaï A et al.. (2022) GNS561, a clinical-stage PPT1 inhibitor, is efficient against hepatocellular carcinoma via modulation of lysosomal functions. Autophagy, 18 (3): 678-694. [PMID:34740311]

3. Lu JY, Verkruyse LA, Hofmann SL. (1996) Lipid thioesters derived from acylated proteins accumulate in infantile neuronal ceroid lipofuscinosis: correction of the defect in lymphoblasts by recombinant palmitoyl-protein thioesterase. Proc Natl Acad Sci U S A, 93 (19): 10046-50. [PMID:8816748]

How to cite this family page

Database page citation:

3.1.-.- Ester bond enzymes. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=880.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.