Page last updated: 2024-10-24

aspartic-type peptidase activity

Definition

Target type: molecularfunction

Catalysis of the hydrolysis of peptide bonds in a polypeptide chain by a mechanism in which a water molecule bound by the side chains of aspartic residues at the active center acts as a nucleophile. [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE]

Aspartic-type peptidase activity refers to the catalytic mechanism employed by a class of enzymes known as aspartic peptidases. These enzymes cleave peptide bonds within proteins, playing a crucial role in protein degradation and processing. Their catalytic mechanism relies on two aspartic acid residues located within the active site of the enzyme. These residues, often termed Asp1 and Asp2, act in concert to facilitate the hydrolysis of the peptide bond. The mechanism involves the following steps: 1) The substrate peptide binds to the active site of the enzyme, positioning the scissile bond (the peptide bond to be cleaved) between the two aspartic acid residues. 2) Asp1 acts as a general base, abstracting a proton from a water molecule. 3) The activated water molecule then attacks the carbonyl carbon of the scissile bond, forming a tetrahedral intermediate. 4) Asp2, acting as a general acid, donates a proton to the leaving group, the amino group of the peptide bond. 5) The tetrahedral intermediate collapses, breaking the peptide bond and releasing the two peptide fragments. The two aspartic acid residues within the active site work in tandem to facilitate the hydrolysis reaction. Asp1 activates the water molecule for nucleophilic attack, while Asp2 stabilizes the transition state and facilitates the departure of the leaving group. This concerted action of the two aspartic acid residues is essential for the catalytic activity of aspartic peptidases.'
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Proteins (1)

ProteinDefinitionTaxonomy
Cathepsin DA cathepsin D that is encoded in the genome of human. [PRO:DNx, UniProtKB:P07339]Homo sapiens (human)

Compounds (20)

CompoundDefinitionClassesRoles
nafamostatnafamostat: inhibitor of trypsin, plasmin, pancreatic kallikrein, plasma kallikrein & thrombin; strongly inhibits esterolytic activities of C1r & C1 esterase complement-mediated hemolysis; antineoplasticbenzoic acids;
guanidines
1,2-diphenylhydrazine
amprenavircarbamate ester;
sulfonamide;
tetrahydrofuryl ester
antiviral drug;
HIV protease inhibitor
bila 2157 bsBILA 2157 BS: renin inhibitor; RN given for (1S-(1R*(S*),2S*,3R*))-isomer; structure in first source
resveratroltrans-resveratrol : A resveratrol in which the double bond has E configuration.resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
om99-2OM99-2: eight-residue memapsin 2 inhibitor; structure in first source
pl 100PL 100: inhibits HIV-1 protease; structure in first source
benzyloxycarbonyl-phe-ala-fluormethylketonecathepsin B inhibitor : A cysteine protease inhibitor which inhibits cathepsin B (EC 3.4.22.1).
pepstatinpepstatin: inhibits the aspartic protease endothiapepsinpentapeptide;
secondary carboxamide
bacterial metabolite;
EC 3.4.23.* (aspartic endopeptidase) inhibitor
ca 074
kni 10006
balicatibbalicatib: cathepsin K inhibitor
tasiamide btasiamide B: 4-amino-3-hydroxy-5-phenylpentanoic acid containing peptide from the marine cyanobacterium Symploca sp.; structure in first source
calpain inhibitor iiicalpain inhibitor III: potential anticataract drug
PF-00835231PF-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
gsk188909GSK188909: a potent and selective non-peptidic BACE-1 inhibitor; structure in first source
ly2811376
grassystatin agrassystatin A: isolated from a cyanobacterium, identified as Lyngbya cf.; structure in first source
ly2886721
tipranavirtipranavir : A pyridine-2-sulfonamide substituted at C-5 by a trifluoromethyl group and at the sulfonamide nitrogen by a dihydropyrone-containing m-tolyl substituent. It is an HIV-1 protease inhibitor.

tipranavir: inhibits HIV-1 protease
sulfonamideantiviral drug;
HIV protease inhibitor