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Methionyl aminopeptidase 2

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Target not currently curated in GtoImmuPdb

Target id: 1573

Nomenclature: Methionyl aminopeptidase 2

Family: M24: Methionyl aminopeptidase

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 478 12q22 METAP2 methionyl aminopeptidase 2
Mouse - 478 10 C2 Metap2 methionine aminopeptidase 2
Rat - 478 7q13 Metap2 methionyl aminopeptidase 2
Previous and Unofficial Names Click here for help
initiation factor 2 associated 67 kDa protein | metAP 2 | methionine aminopeptidase 2 | peptidase M 2 | eIF-2-associated p67 | MAP2 | MNPEP
Database Links Click here for help
Specialist databases
MEROPS M24.002 (Hs)
Other databases
Alphafold
BRENDA
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 3.4.11.18

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
XMT-1191 Small molecule or natural product Hs Inhibition 8.0 pIC50 1
pIC50 8.0 (IC50 9x10-9 M) [1]
beloranib Small molecule or natural product Primary target of this compound Hs Inhibition - - 3
[3]
Inhibitor Comments
Aclimostat (ZGN-1061; PubChem CID 126573394) is another MetAP2 inhibitor that was developed by Zafgen as an anti-obesity drug [2]. It suffered from the same unacceptable safety issues as belaronib, and its development was halted at Phase 2 [4].

References

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1. Akullian LC, Stevenson CA, Yurkovetskiy AV, Benson JD, Fram RJ, Lowinger TB. (2009) Anti-angiogenic and Anti-tumor Activity of XMT-1107, a Fumagillol-derived Polymer Conjugate, and its in vivo Release Product XMT-1191. Proc Am Assoc Cancer Res,: 670.

2. Burkey BF, Hoglen NC, Inskeep P, Wyman M, Hughes TE, Vath JE. (2018) Preclinical Efficacy and Safety of the Novel Antidiabetic, Antiobesity MetAP2 Inhibitor ZGN-1061. J Pharmacol Exp Ther, 365 (2): 301-313. [PMID:29491038]

3. Kim YM, An JJ, Jin YJ, Rhee Y, Cha BS, Lee HC, Lim SK. (2007) Assessment of the anti-obesity effects of the TNP-470 analog, CKD-732. J Mol Endocrinol, 38 (4): 455-65. [PMID:17446235]

4. Wentworth JM, Colman PG, Zafgen Study Group. (2020) The methionine aminopeptidase 2 inhibitor ZGN-1061 improves glucose control and weight in overweight and obese individuals with type 2 diabetes: A randomized, placebo-controlled trial. Diabetes Obes Metab, 22 (7): 1215-1219. [PMID:32077231]

How to cite this page

M24: Methionyl aminopeptidase: Methionyl aminopeptidase 2. Last modified on 10/08/2020. Accessed on 02/12/2022. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1573.