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Literature summary for 3.4.24.85 extracted from

  • Guan, M.; Fousek, K.; Chow, W.A.
    Nelfinavir inhibits regulated intramembrane proteolysis of sterol regulatory element binding protein-1 and activating transcription factor 6 in castration-resistant prostate cancer (2012), FEBS J., 279, 2399-2411.
    View publication on PubMed
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Application

Application Comment Organism
medicine nelfinavir and its analogs inhibit castration-resistant prostate cancer proliferation by blocking regulated intramembrane proteolysis through suppression of site-2 protease cleavage activity. This leads to accumulation of precursors of sterol regulatory element-binding protein SREBP-1 and activating transcription factor ATF6, and development of insufficient reserves of their transcriptionally-active forms Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
7,8-dimethoxy-1,2,3,11a-tetrahydro-5H,11H-pyrrolo[2,1-c][1,4]benzothiazepine-5,11-dione analog of nelfinavir, inhibits cleavage of artificial protein substrate CED-9 in an in vitro proteolysis assay. Inhibits castration-resistant prostate cancer proliferation by blocking regulated intramembrane proteolysis through suppression of site-2 protease cleavage activity Homo sapiens
nelfinavir nelfinavir and its analogs inhibit cleavage of artificial protein substrate CED-9 in an in vitro proteolysis assay. Nelfinavir and its analogs inhibit castration-resistant prostate cancer proliferation by blocking regulated intramembrane proteolysis through suppression of site-2 protease cleavage activity Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Source Tissue

Source Tissue Comment Organism Textmining
DU-145 cell
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 Homo sapiens
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PC-3 cell
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 Homo sapiens
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
CED-9 + H2O artificial protein substrate, Caenorhabditis elegans protein 9, homolog to human Bcl-2 Homo sapiens ?
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 ?