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Target not currently curated in GtoImmuPdb
Target id: 2381
Nomenclature: membrane bound transcription factor peptidase, site 1
Family: S8: Subtilisin
Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 1 | 1052 | 16q23.3-q24.1 | MBTPS1 | membrane bound transcription factor peptidase, site 1 | |
| Mouse | 1 | 1052 | 8 E1 | Mbtps1 | membrane-bound transcription factor peptidase, site 1 | |
| Rat | 1 | 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 |
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| Specialist databases | |
| MEROPS | S08.063 (Hs) |
| Other databases | |
| Alphafold | Q14703 (Hs), Q9WTZ2 (Mm), Q9WTZ3 (Rn) |
| BRENDA | 3.4.21.112 |
| CATH/Gene3D | 3.40.50.200, 3.40.50.880 |
| ChEMBL Target | CHEMBL5916 (Hs) |
| Ensembl Gene | ENSG00000140943 (Hs), ENSMUSG00000031835 (Mm), ENSRNOG00000015173 (Rn) |
| Entrez Gene | 8720 (Hs), 56453 (Mm), 89842 (Rn) |
| Human Protein Atlas | ENSG00000140943 (Hs) |
| KEGG Enzyme | 3.4.21.112 |
| KEGG Gene | hsa:8720 (Hs), mmu:56453 (Mm), rno:89842 (Rn) |
| OMIM | 603355 (Hs) |
| Pharos | Q14703 (Hs) |
| RefSeq Nucleotide | NM_003791 (Hs), NM_001167910 (Mm), NM_019709 (Mm), NM_053569 (Rn) |
| RefSeq Protein | NP_003782 (Hs), NP_062683 (Mm), NP_001161382 (Mm), NP_446021 (Rn) |
| UniProtKB | Q14703 (Hs), Q9WTZ2 (Mm), Q9WTZ3 (Rn) |
| Wikipedia | MBTPS1 (Hs) |
| Enzyme Reaction |
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Download all structure-activity data for this target as a CSV file 
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||
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| 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]. |
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]
S8: Subtilisin: membrane bound transcription factor peptidase, site 1. Last modified on 29/01/2016. Accessed on 08/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2381.
