membrane bound transcription factor peptidase, site 1

Target id: 2381

Nomenclature: membrane bound transcription factor peptidase, site 1

Family: S8: Subtilisin

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for membrane bound transcription factor peptidase, site 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1052 16q24 MBTPS1 membrane bound transcription factor peptidase, site 1
Mouse - 1052 8 E1 Mbtps1 membrane-bound transcription factor peptidase, site 1
Rat - 1052 19q12 Mbtps1 membrane-bound transcription factor peptidase, site 1
Previous and Unofficial Names
endopeptidase S1P | PCSK8 | S1P endopeptidase | site-1 protease | Ski1 | sterol-regulated luminal protease | subtilisin/kexin isozyme 1 | membrane-bound transcription factor peptidase
Database Links
Specialist databases
MEROPS S08.063 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.21.112

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound 7b [PMID: 17583500] Hs Inhibition 8.1 pIC50 2
pIC50 8.1 (IC50 8x10-9 M) [2]
General Comments
MBTPS1 is an important posttranscriptional modulator of sterol regulatory element-binding proteins (SREBPs), which are proteins that transcriptionally regulate cholesterol, fatty acid, and glucose metabolism. Pharmacologic inhibition of MBTPS1 reduces lipogenic enzyme gene expression and lipid synthesis in vitro and in vivo [1].

References

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1. Hawkins JL, Robbins MD, Warren LC, Xia D, Petras SF, Valentine JJ, Varghese AH, Wang IK, Subashi TA, Shelly LD et al.. (2008) Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J. Pharmacol. Exp. Ther.326 (3): 801-8. [PMID:18577702]

2. Hay BA, Abrams B, Zumbrunn AY, Valentine JJ, Warren LC, Petras SF, Shelly LD, Xia A, Varghese AH, Hawkins JL et al.. (2007) Aminopyrrolidineamide inhibitors of site-1 protease. Bioorg. Med. Chem. Lett.17 (16): 4411-4. [PMID:17583500]

How to cite this page

S8: Subtilisin: membrane bound transcription factor peptidase, site 1. Last modified on 29/01/2016. Accessed on 21/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2381.