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Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | - | 420 | 20p12.1 | TASP1 | taspase 1 | |
| Mouse | - | 420 | 2 F3 | Tasp1 | taspase, threonine aspartase 1 | |
| Rat | - | 420 | 3q36-q41 | Tasp1 | taspase 1 | |
| Previous and Unofficial Names |
| taspase, threonine aspartase, 1 | taspase |
| Database Links |
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| Specialist databases | |
| MEROPS | T02.004 (Hs) |
| Other databases | |
| Alphafold | Q9H6P5 (Hs), Q8R1G1 (Mm) |
| BRENDA | 3.4.25.- |
| ChEMBL Target | CHEMBL6153 (Hs) |
| Ensembl Gene | ENSG00000089123 (Hs), ENSMUSG00000039033 (Mm), ENSRNOG00000004493 (Rn) |
| Entrez Gene | 55617 (Hs), 75812 (Mm), 311468 (Rn) |
| Human Protein Atlas | ENSG00000089123 (Hs) |
| KEGG Enzyme | 3.4.25.- |
| KEGG Gene | hsa:55617 (Hs), mmu:75812 (Mm), rno:311468 (Rn) |
| OMIM | 608270 (Hs) |
| Pharos | Q9H6P5 (Hs) |
| RefSeq Nucleotide | NM_017714 (Hs), NM_175225 (Mm), NM_001159641 (Mm), NM_001159640 (Mm), NM_001044243 (Rn) |
| RefSeq Protein | NP_060184 (Hs), NP_780434 (Mm), NP_001153113 (Mm), NP_001153112 (Mm), NP_001037708 (Rn) |
| UniProtKB | Q9H6P5 (Hs), Q8R1G1 (Mm) |
| Wikipedia | TASP1 (Hs) |
| Enzyme Reaction |
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Download all structure-activity data for this target as a CSV file 
| Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||
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| General Comments |
| Taspase 1 regulates cell cycle gene expression by cleavage-mediated substrate activation. This activity is essential for cell proliferation [4]. Mammalian taspase 1 substrates include MLL (mixed-lineage leukemia = lysine (K)-specific methyltransferase 2A, KMT2A) [1-2], MLL2 (= lysine (K)-specific methyltransferase 2D, KTMD2) and transcription factor IIA [5]. |
1. Hsieh JJ, Cheng EH, Korsmeyer SJ. (2003) Taspase1: a threonine aspartase required for cleavage of MLL and proper HOX gene expression. Cell, 115 (3): 293-303. [PMID:14636557]
2. Hsieh JJ, Ernst P, Erdjument-Bromage H, Tempst P, Korsmeyer SJ. (2003) Proteolytic cleavage of MLL generates a complex of N- and C-terminal fragments that confers protein stability and subnuclear localization. Mol Cell Biol, 23 (1): 186-94. [PMID:12482972]
3. Lee JT, Chen DY, Yang Z, Ramos AD, Hsieh JJ, Bogyo M. (2009) Design, syntheses, and evaluation of Taspase1 inhibitors. Bioorg Med Chem Lett, 19 (17): 5086-90. [PMID:19631530]
4. Takeda S, Chen DY, Westergard TD, Fisher JK, Rubens JA, Sasagawa S, Kan JT, Korsmeyer SJ, Cheng EH, Hsieh JJ. (2006) Proteolysis of MLL family proteins is essential for taspase1-orchestrated cell cycle progression. Genes Dev, 20 (17): 2397-409. [PMID:16951254]
5. Zhou H, Spicuglia S, Hsieh JJ, Mitsiou DJ, Høiby T, Veenstra GJ, Korsmeyer SJ, Stunnenberg HG. (2006) Uncleaved TFIIA is a substrate for taspase 1 and active in transcription. Mol Cell Biol, 26 (7): 2728-35. [PMID:16537915]
T2: Glycosylasparaginase precursor: taspase 1. Last modified on 29/01/2016. Accessed on 13/01/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2419.
