Page last updated: 2024-10-24
peptidase inhibitor complex
Definition
Target type: cellularcomponent
A protein complex which is capable of peptidase inhibitor activity. [GO_REF:0000088, GOC:bhm, GOC:TermGenie, PMID:20860624]
A peptidase inhibitor complex is a molecular assembly comprised of one or more peptidase inhibitor proteins bound to their target peptidase(s). These complexes play a crucial role in regulating cellular processes by controlling the activity of peptidases, enzymes responsible for breaking down proteins. The cellular component of a peptidase inhibitor complex can vary depending on the specific inhibitors and peptidases involved, but generally includes:
* **The peptidase itself**: This is the enzyme that the inhibitor binds to and prevents from functioning. Peptidases are found in various cellular compartments, including the cytoplasm, nucleus, lysosomes, and extracellular matrix.
* **The inhibitor protein(s)**: These proteins are responsible for binding to the peptidase and blocking its activity. Inhibitor proteins can be located in the cytoplasm, nucleus, or secreted outside the cell.
* **Other associated proteins**: In some cases, other proteins may be associated with the peptidase inhibitor complex, acting as scaffolding or regulatory components. These proteins can be found in various cellular compartments depending on their specific functions.
The location and composition of the peptidase inhibitor complex within the cell are crucial for its function. For instance, inhibitors located in the cytoplasm can regulate the activity of intracellular peptidases, while inhibitors secreted outside the cell can control the activity of extracellular peptidases. The precise cellular location and composition of the peptidase inhibitor complex are determined by the specific peptidase and inhibitor involved, as well as the cellular context in which they interact.'
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Proteins (2)
| Protein | Definition | Taxonomy |
|---|---|---|
| Cathepsin B | A cathepsin B that is encoded in the genome of human. [PRO:DNx, UniProtKB:P07858] | Homo sapiens (human) |
| Plasminogen activator inhibitor 1 | A plasminogen activator inhibitor 1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P05121] | Homo sapiens (human) |
Compounds (54)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| gallic acid | gallate : A trihydroxybenzoate that is the conjugate base of gallic acid. | trihydroxybenzoic acid | antineoplastic agent; antioxidant; apoptosis inducer; astringent; cyclooxygenase 2 inhibitor; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; geroprotector; human xenobiotic metabolite; plant metabolite |
| diminazene | diminazene : A triazene derivative that is triazene in which each of the terminal nitrogens is substituted by a 4-carbamimidoylphenyl group. Diminazene: An effective trypanocidal agent. | carboxamidine; triazene derivative | antiparasitic agent; trypanocidal drug |
| dibutyl phthalate | dibutyl phthalate : A phthalate ester that is the diester obtained by the formal condensation of the carboxy groups of phthalic acid with two molecules of butan-1-ol. Although used extensively as a plasticiser, it is a ubiquitous environmental contaminant that poses a risk to humans. Dibutyl Phthalate: A plasticizer used in most plastics and found in water, air, soil, plants and animals. It may have some adverse effects with long-term exposure. | diester; phthalate ester | EC 3.2.1.20 (alpha-glucosidase) inhibitor; environmental contaminant; metabolite; plasticiser; teratogenic agent |
| benzophenone | benzophenone : The simplest member of the class of benzophenones, being formaldehyde in which both hydrogens are replaced by phenyl groups. | benzophenones | photosensitizing agent; plant metabolite |
| hexachlorophene | hexachlorophene : An organochlorine compound that is diphenylmethane in which each of the phenyl groups is substituted by chlorines at positions 2, 3, and 5, and by a hydroxy group at position 6. An antiseptic that is effective against Gram-positive organisms, it is used in soaps and creams for the treatment of various skin disorders. It is also used in agriculture as an acaricide and fungicide, but is not approved for such use within the European Union. Hexachlorophene: A chlorinated bisphenol antiseptic with a bacteriostatic action against Gram-positive organisms, but much less effective against Gram-negative organisms. It is mainly used in soaps and creams and is an ingredient of various preparations used for skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p797) | bridged diphenyl fungicide; polyphenol; trichlorobenzene | acaricide; antibacterial agent; antifungal agrochemical; antiseptic drug |
| 1,2,5,8-tetrahydroxy anthraquinone | 1,2,5,8-tetrahydroxy anthraquinone: structure in first source quinalizarin : A tetrahydroxyanthraquinone having the four hydroxy groups at the 1-, 2-, 5- and 8-positions. | tetrahydroxyanthraquinone | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor |
| suramin | suramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years. Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties. | naphthalenesulfonic acid; phenylureas; secondary carboxamide | angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug |
| nitroxoline | nitroxoline : A monohydroxyquinoline in which the hydroxy group is positioned at C-8 with a nitro group trans to it at C-5. nitroxoline: structure in Merck Index, 9th ed, #6475; RN given refers to parent cpd | C-nitro compound; monohydroxyquinoline | antifungal agent; antiinfective agent; antimicrobial agent; renal agent |
| allicin | botanical anti-fungal agent; sulfoxide | antibacterial agent | |
| epigallocatechin gallate | (-)-epigallocatechin 3-gallate : A gallate ester obtained by the formal condensation of gallic acid with the (3R)-hydroxy group of (-)-epigallocatechin. epigallocatechin gallate: a steroid 5alpha-reductase inhibitor and antimutagen in green tea (Camellia sinensis) | flavans; gallate ester; polyphenol | antineoplastic agent; antioxidant; apoptosis inducer; geroprotector; Hsp90 inhibitor; neuroprotective agent; plant metabolite |
| aloxistatin | aloxistatin : An L-leucine derivative that is the amide obtained by formal condensation of the carboxy group of (2S,3S)-3-(ethoxycarbonyl)oxirane-2-carboxylic acid with the amino group of N-(3-methylbutyl)-L-leucinamide. aloxistatin: a membrane-permeable cysteine protease inhibitor | epoxide; ethyl ester; L-leucine derivative; monocarboxylic acid amide | anticoronaviral agent; cathepsin B inhibitor |
| 5,5'-methylenedisalicylic acid | 5,5'-methylenedisalicylic acid: inhibits attachment of ribosomes to microsomal membranes; RN given refers to parent cpd; structure in first source & Merck Index, 9th ed, #5934 | ||
| leupeptin | aldehyde; tripeptide | bacterial metabolite; calpain inhibitor; cathepsin B inhibitor; EC 3.4.21.4 (trypsin) inhibitor; serine protease inhibitor | |
| carbobenzoxyvalylphenylalanine aldehyde | Z-Val-Phe-H : A dipeptide resulting from the formal condensation of the carboxy group of N-benzyloxycarbonyl-L-valine with the amino group of L-phenylalanine aldehyde. It is a potent cell-permeable inhibitor of calpain I and II, and is also a gamma-secretase inhibitor. | aldehyde; carbamate ester; dipeptide | antileishmanial agent; apoptosis inhibitor; EC 3.4.22.52 (calpain-1) inhibitor; EC 3.4.22.53 (calpain-2) inhibitor; EC 3.4.23.46 (memapsin 2) inhibitor |
| sennoside A | sennoside A : A member of the class of sennosides that is rel-(9R,9'R)-9,9',10,10'-tetrahydro-9,9'-bianthracene-2,2'-dicarboxylic acid which is substituted by hydroxy groups at positions 4 and 4', by beta-D-glucopyranosyloxy groups at positions 5 and 5', and by oxo groups at positions 10 and 10'. The exact stereochemisty at positions 9 and 9' is not known - it may be R,R (as shown) or S,S. | oxo dicarboxylic acid; sennosides | |
| calpeptin | amino acid amide | ||
| Pyrrolidine-1-carbonitrile | pyrrolidines | ||
| n-(n-(3-carboxyoxirane-2-carbonyl)leucyl)isoamylamine | N-(N-(3-carboxyoxirane-2-carbonyl)leucyl)isoamylamine: inhibits calcium-activated neutral protease; see also record for E-64; RN given refers to (2-S-(2alpha,3beta)(R*)-isomer) | leucine derivative | |
| 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 |
| n-(3-ethoxycarbonyloxirane-2-carbonyl)-isoleucyl-proline | |||
| ak 295 | AK 295: a dipeptide alpha-ketoamide calpain inhibitor | ||
| bortezomib | amino acid amide; L-phenylalanine derivative; pyrazines | antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor | |
| acetylleucyl-leucyl-norleucinal | acetylleucyl-leucyl-norleucinal : A tripeptide composed of N-acetylleucyl, leucyl and norleucinal residues joined in sequence. acetylleucyl-leucyl-norleucinal: a proteasome inhibitor | aldehyde; tripeptide | cysteine protease inhibitor |
| benzyloxycarbonylleucyl-leucyl-leucine aldehyde | benzyloxycarbonylleucyl-leucyl-leucine aldehyde: proteasome inhibitor N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal : A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative. | amino aldehyde; carbamate ester; tripeptide | proteasome inhibitor |
| Epigallocatechin 3,5-Digallate | catechin | ||
| mg 262 | MG 262: a proteasome inhibitor | ||
| telaprevir | cyclopentapyrrole; cyclopropanes; oligopeptide; pyrazines | antiviral drug; hepatitis C protease inhibitor; peptidomimetic | |
| benzyloxycarbonyl-phe-ala-fluormethylketone | cathepsin B inhibitor : A cysteine protease inhibitor which inhibits cathepsin B (EC 3.4.22.1). | ||
| guttiferone a | guttiferone A: antibacterial from Clusiaceae family; structure in first source | ||
| pepstatin | pepstatin: inhibits the aspartic protease endothiapepsin | pentapeptide; secondary carboxamide | bacterial metabolite; EC 3.4.23.* (aspartic endopeptidase) inhibitor |
| pai 039 | tiplaxtinin: inhibitor of plasminogen activator inhibitor-1 | indole-3-acetic acids | |
| ca 074 methyl ester | |||
| relacatib | relacatib: a cathepsin K inhibitor; structure in first source | ||
| xr 334 | XR 334: a low molecular weight modulator of human plasminogen activator inhibitor-1 activity; structure given in first source; RN given refers to (Z,Z)-isomer | ||
| ca 074 | |||
| k11002 | |||
| a-705253 | A-705253: structure in first source | ||
| l 006235 | |||
| l-873724 | L-873724: a selective inhibitor of cathepsin K; structure in first source | ||
| odanacatib | odanacatib: a selective inhibitor of cathepsin K for the treatment of post-menopausal osteoporosis; structure in first source | ||
| balicatib | balicatib: cathepsin K inhibitor | ||
| s-benzyl phenylmethanethiosulfinate | S-benzyl phenylmethanethiosulfinate: an antioxidant; structure in first source | ||
| n-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide | boceprevir : A synthetic tripeptide consisting of N-(tert-butylcarbamoyl)-3-methyl-L-valyl, a cyclopropyl-fused prolyl and 3-amino-4-cyclobutyl-2-oxobutanamide residues joined in sequence. Used for treatment of chronic hepatitis C virus genotype 1 infection. | tripeptide; ureas | antiviral drug; hepatitis C protease inhibitor; peptidomimetic |
| sideroxylonal c | sideroxylonal C: formylated phloroglucinol from flowers of Eucalyptus albens; structure in first source | ||
| calpain inhibitor iii | calpain inhibitor III: potential anticataract drug | ||
| epoxomicin | morpholines; tripeptide | proteasome inhibitor | |
| carfilzomib | epoxide; morpholines; tetrapeptide | antineoplastic agent; proteasome inhibitor | |
| PF-00835231 | PF-00835231 : A primary alcohol resulting from the cleavage of the phosphate group of the prodrug PF-07304814. It is an inhibitor of SARS-CoV-1 and -2 main protease (3CLpro) and exhibits potent in vitro antiviral activity. | aromatic ether; indolecarboxamide; L-leucine derivative; primary alcohol; pyrrolidin-2-ones; secondary carboxamide | anticoronaviral agent; drug metabolite; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor |
| mk-7009 | vaniprevir : An azamacrocyclic compound that is a hepatitis C virus (HCV) NS3/4A protease inhibitor which is approved for the treatment of hepatitis C virus infections in Japan. vaniprevir: inhibits hepatitis C virus NS3/4a protease | azamacrocycle; carbamate ester; cyclopropanes; N-sulfonylcarboxamide; pyrrolidinecarboxamide | antiviral drug; hepatitis C protease inhibitor |
| gallinamide a | gallinamide A: antimalarial peptide from marine cyanobacteria | ||
| bi 201335 | faldaprevir: inhibits hepatitis C virus NS3 protease | ||
| 6-(3,5-difluoroanilino)-9-ethyl-2-purinecarbonitrile | 6-aminopurines | ||
| grassystatin a | grassystatin A: isolated from a cyanobacterium, identified as Lyngbya cf.; structure in first source | ||
| N-[(2S)-3-cyclohexyl-1-oxo-1-({(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}amino)propan-2-yl]-1H-indole-2-carboxamide | N-[(2S)-3-cyclohexyl-1-oxo-1-({(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}amino)propan-2-yl]-1H-indole-2-carboxamide : A secondary carboxamide resulting from the formal condensation of the carboxy group of 1H-indole-2-carboxylic acid with the primary amino group of 3-cyclohexyl-N-{(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}-L-alaninamide. It is an inhibitor of SARS coronavirus main proteinase and inhibits SARS-CoV-2 replication in cell culture (EC50 = 0.53 muM). | aldehyde; indolecarboxamide; oligopeptide; pyrrolidin-2-ones; secondary carboxamide | anticoronaviral agent; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor |