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.

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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	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
DU-145 cell	-	Homo sapiens	-
PC-3 cell	-	Homo sapiens	-

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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Release 2023.1 (January 2023)