skip to main content
DOE PAGES title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design—Part 1

Authors:
; ; ; ; ; ; ; ; ; ; ; ; ; ; ORCiD logo;
Publication Date:
Sponsoring Org.:
USDOE
OSTI Identifier:
1358851
Resource Type:
Publisher's Accepted Manuscript
Journal Name:
Bioorganic and Medicinal Chemistry Letters
Additional Journal Information:
Journal Name: Bioorganic and Medicinal Chemistry Letters Journal Volume: 26 Journal Issue: 12; Journal ID: ISSN 0960-894X
Publisher:
Elsevier
Country of Publication:
United Kingdom
Language:
English

Citation Formats

Cheruvallath, Zacharia, Tang, Mingnam, McBride, Christopher, Komandla, Mallareddy, Miura, Joanne, Ton-Nu, Thu, Erikson, Phil, Feng, Jun, Farrell, Pamela, Lawson, J. David, Vanderpool, Darin, Wu, Yiqin, Dougan, Douglas R., Plonowski, Artur, Holub, Corine, and Larson, Chris. Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design—Part 1. United Kingdom: N. p., 2016. Web. https://doi.org/10.1016/j.bmcl.2016.04.073.
Cheruvallath, Zacharia, Tang, Mingnam, McBride, Christopher, Komandla, Mallareddy, Miura, Joanne, Ton-Nu, Thu, Erikson, Phil, Feng, Jun, Farrell, Pamela, Lawson, J. David, Vanderpool, Darin, Wu, Yiqin, Dougan, Douglas R., Plonowski, Artur, Holub, Corine, & Larson, Chris. Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design—Part 1. United Kingdom. https://doi.org/10.1016/j.bmcl.2016.04.073
Cheruvallath, Zacharia, Tang, Mingnam, McBride, Christopher, Komandla, Mallareddy, Miura, Joanne, Ton-Nu, Thu, Erikson, Phil, Feng, Jun, Farrell, Pamela, Lawson, J. David, Vanderpool, Darin, Wu, Yiqin, Dougan, Douglas R., Plonowski, Artur, Holub, Corine, and Larson, Chris. Wed . "Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design—Part 1". United Kingdom. https://doi.org/10.1016/j.bmcl.2016.04.073.
@article{osti_1358851,
title = {Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design—Part 1},
author = {Cheruvallath, Zacharia and Tang, Mingnam and McBride, Christopher and Komandla, Mallareddy and Miura, Joanne and Ton-Nu, Thu and Erikson, Phil and Feng, Jun and Farrell, Pamela and Lawson, J. David and Vanderpool, Darin and Wu, Yiqin and Dougan, Douglas R. and Plonowski, Artur and Holub, Corine and Larson, Chris},
abstractNote = {},
doi = {10.1016/j.bmcl.2016.04.073},
journal = {Bioorganic and Medicinal Chemistry Letters},
number = 12,
volume = 26,
place = {United Kingdom},
year = {2016},
month = {6}
}

Journal Article:
Free Publicly Available Full Text
Publisher's Version of Record
https://doi.org/10.1016/j.bmcl.2016.04.073

Citation Metrics:
Cited by: 4 works
Citation information provided by
Web of Science

Save / Share:

Works referenced in this record:

Ligand efficiency: a useful metric for lead selection
journal, May 2004


The Development of MetAP-2 Inhibitors in Cancer Treatment
journal, March 2012


An Unusual Peptide Deformylase Features in the Human Mitochondrial N-terminal Methionine Excision Pathway
journal, December 2003

  • Serero, Alexandre; Giglione, Carmela; Sardini, Alessandro
  • Journal of Biological Chemistry, Vol. 278, Issue 52
  • DOI: 10.1074/jbc.M309770200

Adaptations for the Oxidation of Polycyclic Aromatic Hydrocarbons Exhibited by the Structure of Human P450 1A2
journal, February 2007

  • Sansen, Stefaan; Yano, Jason K.; Reynald, Rosamund L.
  • Journal of Biological Chemistry, Vol. 282, Issue 19
  • DOI: 10.1074/jbc.M611692200

Eukaryotic methionyl aminopeptidases: two classes of cobalt-dependent enzymes.
journal, August 1995

  • Arfin, S. M.; Kendall, R. L.; Hall, L.
  • Proceedings of the National Academy of Sciences, Vol. 92, Issue 17
  • DOI: 10.1073/pnas.92.17.7714

Methionine aminopeptidase (type 2) is the common target for angiogenesis inhibitors AGM-1470 and ovalicin
journal, June 1997


Adipose tissue mass can be regulated through the vasculature
journal, July 2002

  • Rupnick, M. A.; Panigrahy, D.; Zhang, C. -Y.
  • Proceedings of the National Academy of Sciences, Vol. 99, Issue 16
  • DOI: 10.1073/pnas.162349799

Amino-terminal protein processing in Saccharomyces cerevisiae is an essential function that requires two distinct methionine aminopeptidases.
journal, December 1995


The anti-angiogenic agent fumagillin covalently binds and inhibits the methionine aminopeptidase, MetAP-2
journal, June 1997

  • Sin, N.; Meng, L.; Wang, M. Q. W.
  • Proceedings of the National Academy of Sciences, Vol. 94, Issue 12
  • DOI: 10.1073/pnas.94.12.6099