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taspase 1

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Target not currently curated in GtoImmuPdb

Target id: 2419

Nomenclature: taspase 1

Family: T2: Glycosylasparaginase precursor

Contents:

Gene and Protein Information Click here for help
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 Click here for help
taspase, threonine aspartase, 1 | taspase
Database Links Click here for help
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 Click here for help
EC Number: 3.4.25.-

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
yzm18 Small molecule or natural product Hs Inhibition 4.5 pIC50 3
⤷ pIC50 4.5 (IC50 2.94x10-5 M) [3]
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].

References

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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]

How to cite this page

T2: Glycosylasparaginase precursor: taspase 1. Last modified on 29/01/2016. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2419.