Page last updated: 2024-10-24

peptidase activator activity involved in apoptotic process

Definition

Target type: molecularfunction

Binds to and increases the activity of a peptidase that is involved in the apoptotic process. [GOC:BHF, GOC:mah, GOC:mtg_apoptosis, GOC:rl]

Peptidase activator activity involved in apoptotic process describes the role of proteins in initiating or regulating the activity of proteases, also known as peptidases, during the process of programmed cell death, or apoptosis. These activators often act by promoting the assembly of the death-inducing complex, a multi-protein structure that triggers the activation of specific caspases, a family of proteases crucial for apoptosis. This activation can occur through various mechanisms, including:

1. **Direct binding:** Some activators directly interact with the inactive pro-caspase molecule, inducing conformational changes that expose the active site and trigger auto-activation.

2. **Scaffolding:** Other activators act as scaffolding proteins, bringing together multiple components of the death-inducing complex, including pro-caspases, adaptor proteins, and other regulatory molecules. This assembly facilitates the activation of caspases through proximity-induced dimerization or by promoting conformational changes.

3. **Release of inhibitors:** Some activators function by displacing or removing inhibitory proteins that block caspase activation.

4. **Regulation of upstream signaling pathways:** Some activators participate in upstream signaling pathways that regulate the assembly and activation of the death-inducing complex. This includes proteins involved in sensing cellular stress, DNA damage, or other apoptotic stimuli.

The precise molecular mechanisms of action vary depending on the specific peptidase activator and the apoptotic pathway involved. However, the ultimate effect is the activation of caspases, leading to the execution of the apoptotic program, characterized by the breakdown of cellular components and the dismantling of the cell. This process plays a crucial role in maintaining tissue homeostasis, eliminating damaged or unwanted cells, and preventing uncontrolled cell growth.'
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Proteins (1)

ProteinDefinitionTaxonomy
Dipeptidyl peptidase 1A dipeptidyl peptidase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P53634]Homo sapiens (human)

Compounds (11)

CompoundDefinitionClassesRoles
Pyrrolidine-1-carbonitrilepyrrolidines
e 64E 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
canertinibmonochlorobenzenes;
morpholines;
organofluorine compound;
quinazolines
antineoplastic agent;
tyrosine kinase inhibitor
odanacatibodanacatib: a selective inhibitor of cathepsin K for the treatment of post-menopausal osteoporosis; structure in first source
bibw 2992aromatic ether;
enamide;
furans;
monochlorobenzenes;
organofluorine compound;
quinazolines;
secondary carboxamide;
tertiary amino compound
antineoplastic agent;
tyrosine kinase inhibitor
6-(3,5-difluoroanilino)-9-ethyl-2-purinecarbonitrile6-aminopurines
6-(3,5-difluoroanilino)-9-(2,2-difluoroethyl)-2-purinecarbonitrile6-aminopurines
9-(3,5-difluorophenyl)-6-(ethylamino)-2-purinecarbonitrileimidazoles
grassystatin agrassystatin A: isolated from a cyanobacterium, identified as Lyngbya cf.; structure in first source
thiopental sodiumorganochlorine compound;
piperazines;
pyrimidines
antineoplastic agent;
tyrosine kinase inhibitor
osimertinibosimertinib : A member of the class of aminopyrimidines that is 4-(1-methylindol-3-yl)pyrimidin-2-amine in which one of the amino hydrogens is replaced by a 2-methoxy-4-[2-(dimethylamino)ethyl](methyl)amino-5-acrylamidophenyl group. Used (as the mesylate salt) for treatment of EGFR T790M mutation positive non-small cell lung cancer.

osimertinib: an EGFR tyrosine kinase inhibitor
acrylamides;
aminopyrimidine;
biaryl;
indoles;
monomethoxybenzene;
secondary amino compound;
secondary carboxamide;
substituted aniline;
tertiary amino compound
antineoplastic agent;
epidermal growth factor receptor antagonist