taspase 1

Target id: 2419

Nomenclature: taspase 1

Family: T2: Glycosylasparaginase precursor

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 taspase 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 420 20p12 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
Database Links
Specialist databases
MEROPS T02.004 (Hs)
Other databases
BRENDA
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: 3.4.25.-

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
Ligand Sp. Action Affinity Units Reference
yzm18 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. Cell115 (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 19/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2419.