taspase 1 | T2: Glycosylasparaginase precursor | IUPHAR/BPS Guide to PHARMACOLOGY

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taspase 1

Target not currently curated in GtoImmuPdb

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

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 | taspase
Database Links
Specialist databases
MEROPS T02.004 (Hs)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number: 3.4.25.-

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter 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].


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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 21/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2419.