Beloranib

Beloranib has been used in trials studying the treatment of Obesity, Over-weight, Type 2 Diabetes, Craniopharyngioma, and Hypothalamic Injury, among others.|Beloranib is a fumagillin analogue and inhibitor of methionine aminopeptidase 2 (METAP2), with potential antiangiogenic and anti-obesity activity. As an irreversible inhibitor, beloranib blocks METAP2's functions, which include both protecting eukaryotic initiation factor 2 from inhibitory phosphorylation during translation, and by removing the amino-terminal methionine residue from nascent protein permitting the conversion of an inactive or non-functional protein to an active one. As a result, this agent prevents endothelial cell growth and inhibits tumor angiogenesis. In addition, METAP2 inhibition also down-regulates ERK1/2 signaling pathway, which is usually overactive in the fat tissues of obese people. Therefore, at a much lower dose, beloranib can induce liver fat utilization and reduce cholesterol and fatty acid synthesis. METAP2, a member of the dimetallohydrolase family, plays an important role during angiogenesis and is over-expressed in various cancers.

Molecular Weight:499.6
XLogP3:4.4
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:12
Exact Mass:499.29338803
Monoisotopic Mass:499.29338803
Topological Polar Surface Area:73.1
Heavy Atom Count:36
Complexity:815
Defined Atom Stereocenter Count:6
Defined Bond Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes