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3.4.24.85: S2P endopeptidase

This is an abbreviated version!
For detailed information about S2P endopeptidase, go to the full flat file.

Word Map on EC 3.4.24.85

Reaction

Cleaves several transcription factors that are type-2 transmembrane proteins within membrane-spanning domains. Known substrates include sterol regulatory element-binding protein (SREBP) -1, SREBP-2 and forms of the transcriptional activator ATF6. SREBP-2 is cleaved at the site DRSR_ILL_483-/-CVLTFLCLSFNPLTSLLQWGGA, in which the membrane-spanning segment is underlined. The residues NP (bold), 11 residues distal to the site of cleavage in the membrane-spanning domain, are important for cleavage by S2P endopeptidase. Replacement of either of these residues does not prevent cleavage, but there is no cleavage if both of these residues are replaced. =

Synonyms

EcfE, Eep, HurP, I-CLiP, intramembrane-cleaving protease, MEROPS:M50, MmpA, MucP, proteinase, sterol regulatory element-binding protein, RasP, RseP, Rv2869c, S2P, S2P protease, site-1 protease, site-2 metalloprotease, site-2 protease, site-2-protease, sll0528, Slr0643, Slr1821, SPOIVFB, Sre2, SREBP cleavage activity, SREBP cysteine proteinase, SREBP proteinase, SREBP-1 proteinase, SREBP-2 proteinase, sterol regulatory element binding protein, sterol regulatory element binding protein-2 proteinase, sterol regulatory element-binding proteinase, sterol-regulated protease, Stp1, YaeL, YluC

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.24 Metalloendopeptidases
                3.4.24.85 S2P endopeptidase

Application

Application on EC 3.4.24.85 - S2P endopeptidase

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APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
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
synthesis
in absence of cholesterol, SREBP double cleavage leads to activation of transcription of genes encoding multiple enzymes of the cholesterol biosynthetic pathway