Top ▲
Gene and Protein Information  |
||||||
| 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 |
| peptidase M 2 | initiation factor 2 associated 67 kDa protein | metAP 2 | methionine aminopeptidase 2 | eIF-2-associated p67 | MAP2 | MNPEP |
| Database Links |
|
| Specialist databases | |
| MEROPS | M24.002 (Hs) |
| Other databases | |
| Alphafold | P50579 (Hs), O08663 (Mm), P38062 (Rn) |
| BRENDA | 3.4.11.18 |
| ChEMBL Target | CHEMBL3922 (Hs), CHEMBL1075272 (Mm) |
| DrugBank Target | P50579 (Hs) |
| Ensembl Gene | ENSG00000111142 (Hs), ENSMUSG00000036112 (Mm), ENSRNOG00000021881 (Rn) |
| Entrez Gene | 10988 (Hs), 56307 (Mm), 64370 (Rn) |
| Human Protein Atlas | ENSG00000111142 (Hs) |
| KEGG Enzyme | 3.4.11.18 |
| KEGG Gene | hsa:10988 (Hs), mmu:56307 (Mm), rno:64370 (Rn) |
| OMIM | 601870 (Hs) |
| Pharos | P50579 (Hs) |
| RefSeq Nucleotide | NM_006838 (Hs), NM_019648 (Mm), NM_022539 (Rn) |
| RefSeq Protein | NP_006829 (Hs), NP_062622 (Mm), NP_071984 (Rn) |
| UniProtKB | P50579 (Hs), O08663 (Mm), P38062 (Rn) |
| Wikipedia | METAP2 (Hs) |
| Enzyme Reaction |
||||
|
||||
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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 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 [5]. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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. Heinrich T, Seenisamy J, Becker F, Blume B, Bomke J, Dietz M, Eckert U, Friese-Hamim M, Gunera J, Hansen K et al.. (2019) Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor M8891: A Clinical Compound for the Treatment of Cancer. J Med Chem, 62 (24): 11119-11134. [PMID:31725285]
4. 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]
5. 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]
M24: Methionyl aminopeptidase: Methionyl aminopeptidase 2. Last modified on 06/06/2023. Accessed on 18/03/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1573.
