Target type: molecularfunction
Catalysis of the hydrolysis of a single C-terminal amino acid residue from the C-terminus of a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [https://www.ebi.ac.uk/merops/about/glossary.shtml#CARBOXYPEPTIDASE]
Serine-type carboxypeptidases are a class of enzymes that catalyze the hydrolysis of peptide bonds at the C-terminal end of proteins and peptides. They are characterized by the presence of a catalytic triad consisting of a serine residue, a histidine residue, and an aspartic acid residue. The mechanism of action involves the following steps:
1. **Substrate Binding:** The peptide substrate binds to the active site of the enzyme, with the C-terminal amino acid positioned near the catalytic triad.
2. **Nucleophilic Attack:** The serine hydroxyl group acts as a nucleophile and attacks the carbonyl carbon of the peptide bond, forming a covalent intermediate.
3. **Proton Transfer:** The histidine residue acts as a general base, abstracting a proton from the serine hydroxyl group, facilitating the nucleophilic attack.
4. **Tetrahedral Intermediate:** The formation of the covalent intermediate results in a tetrahedral intermediate, which is stabilized by the interactions of the catalytic triad.
5. **Hydrolysis:** Water molecules enter the active site and attack the carbonyl carbon of the intermediate, leading to the hydrolysis of the peptide bond.
6. **Product Release:** The C-terminal amino acid is released from the enzyme, and the enzyme is ready to catalyze another reaction.
The serine-type carboxypeptidases are involved in a wide range of biological processes, including protein degradation, peptide hormone processing, and the regulation of blood pressure. They are also important targets for drug development, as their inhibition can be used to treat diseases such as cancer and hypertension.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Lysosomal Pro-X carboxypeptidase | A lysosomal Pro-X carboxypeptidase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P42785] | Homo sapiens (human) |
| Lysosomal protective protein | A lysosomal protective protein that is encoded in the genome of human. [PRO:DNx, UniProtKB:P10619] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| 3,4-dichloroisocoumarin | 3,4-dichloroisocoumarin : A member of the class of isocoumarins that is isocoumarin substituted by chloro groups at positions 3 and 4. It is a serine protease inhibitor. | isocoumarins; organochlorine compound | geroprotector; serine protease inhibitor |
| isoflurophate | Isoflurophate: A di-isopropyl-fluorophosphate which is an irreversible cholinesterase inhibitor used to investigate the NERVOUS SYSTEM. | dialkyl phosphate | |
| phencyclidine | phencyclidine : A member of the class of piperidines that is piperidine in which the nitrogen is substituted with a 1-phenylcyclohexyl group. Formerly used as an anaesthetic agent, it exhibits both hallucinogenic and neurotoxic effects. Phencyclidine: A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust. | benzenes; piperidines | anaesthetic; neurotoxin; NMDA receptor antagonist; psychotropic drug |
| 2-methyl-1,2,3,4-tetrahydroisoquinoline | |||
| tenocyclidine | tenocyclidine : A tertiary amino compound that consists of cyclohexane having piperidin-1-yl and thiophen-2-yl groups attached at position 1. A dissociative anaesthetic drug with halluccinogenic and stimulant effects. Its effects are similar to those of phencyclidine (PCP, an analogue with the thienyl group replaced by phenyl), but it is rather more potent. | piperidines; tertiary amino compound; thiophenes | central nervous system stimulant; hallucinogen; neuroprotective agent; NMDA receptor antagonist |
| 1,2,3,4-tetrahydro-1-(phenylmethyl)isoquinoline | 1,2,3,4-tetrahydro-1-(phenylmethyl)isoquinoline: structure given in first source | benzyltetrahydroisoquinoline | |
| 1,2,3,4-tetrahydro-1-phenylisoquinoline | 1,2,3,4-tetrahydro-1-phenylisoquinoline: structure in first source | ||
| metaphit | metaphit: site-directed acylating agent of phencyclidine receptors in rat brain; structure given in first source | ||
| 1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine | 1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine: structure given in first source 1-[1-(1-benzothiophen-2-yl)cyclohexyl]piperidine : A tertiary amino compound that consists of cyclohexane having piperidin-1-yl and benzothiophen-2-yl groups attached at position 1. A potent dopamine re-uptake inhibitor with a behavioral profile different from that of phencyclidine (PCP) and similar to that of cocaine. | 1-benzothiophenes; piperidines; tertiary amino compound | dopamine uptake inhibitor |
| e 64 | E 64: cysteine protease inhibitor of microbial origin, which inhibits cathepsin B (EC 3.4.22.1) and cathepsin L (EC 3.4.22.-) | dicarboxylic acid monoamide; epoxy monocarboxylic acid; guanidines; L-leucine derivative; zwitterion | antimalarial; antiparasitic agent; protease inhibitor |
| jtp 4819 | JTP 4819: a prolyl endopeptidase inhibitor; structure given in first source | ||
| dizocilpine | secondary amino compound; tetracyclic antidepressant | anaesthetic; anticonvulsant; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist | |
| bortezomib | amino acid amide; L-phenylalanine derivative; pyrazines | antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor | |
| cocaine | cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca. Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. | benzoate ester; methyl ester; tertiary amino compound; tropane alkaloid | adrenergic uptake inhibitor; central nervous system stimulant; dopamine uptake inhibitor; environmental contaminant; local anaesthetic; mouse metabolite; plant metabolite; serotonin uptake inhibitor; sodium channel blocker; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| 4-phenyl-1,2,3,4-tetrahydroisoquinoline | 4-phenyl-1,2,3,4-tetrahydroisoquinoline: RN given is for (R)-isomer; inhibits spinal reflex-enhancing effects of methamphetamine, phenylethylamine, and nomifensine | isoquinolines | |
| gs-7340 | tenofovir alafenamide : An L-alanine derivative that is isopropyl L-alaninate in which one of the amino hydrogens is replaced by an (S)-({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)(phenoxy)phosphoryl group. A prodrug for tenofovir, it is used (as the fumarate salt) in combination therapy for the treatment of HIV-1 infection. tenofovir alafenamide: component of Biktarvy | 6-aminopurines; ether; isopropyl ester; L-alanine derivative; phosphoramidate ester | antiviral drug; HIV-1 reverse transcriptase inhibitor; prodrug |
| carfilzomib | epoxide; morpholines; tetrapeptide | antineoplastic agent; proteasome inhibitor | |
| rpx7009 | RPX7009: a beta-lactamase inhibitor; structure in first source |