Bestatin, Ubenimex: Bestatin, a small molecular weight dipeptide, is a potent inhibitor of various aminopeptidases, as well as, LTA4 hydrolase and Aminopeptidase N (APN/CD13). Bestatin is an immunomodifier. Bestatin also acts an immunorestorator and curative or preventive agent for spontaneous tumor.

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Bestatin alone or its combination with chemicals can prolongate the disease-free interval and survival period in adult acute or chronic leukemia. A pan-hematopoietic stimulator and restorator; Bestatin promotes granulocytopoiesis and thrombocyt

opoiesis in vitro. Additionally, Bestatin is an inhibitor of several natural opioid peptides1.

1) Neuropharmacology

Mei-Rong Jia, et al. The Analgesic Activity of Bestatin as a Potent APN Inhibitor. Frontiers in Neuroscience 2010-01-01 Learn more>>

2) Cytoskeletal

Vivian W. Tang and William M. Brieher ,a-Actinin-4/FSGS1 is required for Arp2/3-dependent actin assembly at the adherens junction. J. Cell Biol. Vol. 196 No. 1 115130 Learn more>>

3) Cell Growth, Cell Division, and Spore Cell Differentiation

Yekaterina Poloz, Andrew Catalano, and Danton H. ODay. Bestatin Inhibits Cell Growth, Cell Division, and Spore Cell Differentiation in Dictyostelium discoideum. Published Ahead of Print 17 February 2012.Eukaryotic Cell 2012, 11(4):545. DOI: 10.1128/EC.05311-11. Learn more>>

4) Biological Sciences - Biochemistry

Michael B. Harbut, et al. Bestatin-based chemical biology strategy reveals distinct roles for malaria M1- and M17-family aminopeptidases PNAS 2011 108 (34) E526-E534; published ahead of print August 15, 2011. Learn more>>

5) Enzyme Catalysis and Regulation

Masato Maruyama, et al Laeverin/Aminopeptidase Q, a Novel Bestatin-sensitive Leucine Aminopeptidase Belonging to the M1 Family of Aminopeptidases J. Biol. Chem. 2007 282: 20088-20096. First Published on May 24, 2007 Learn more>>

6) Lung Cancer

Yukito Ichinose, et al. Randomized Double-Blind Placebo-Controlled Trial of Bestatin in Patients With resected Stage I Squamous-Cell Lung Carcinoma. JNCI J Natl Cancer Inst (2003) 95(8): 605-610 doi:10.1093/jnci/95.8.605. Learn more>>

7) Development and Hormone Action

Wenguang Zheng et al  Bestatin, an Inhibitor of Aminopeptidases, Provides a Chemical Genetics Approach to Dissect Jasmonate Signaling in Arabidopsis Plant Physiol. August 2006 141: 1400-1413. First Published on June 23, 2006. Learn more>>

8) Esophageal Cancer

Xiaoxin Chen et al, Leukotriene A4 Hydrolase in Rat and Human Esophageal Adenocarcinomas and Inhibitory Effects of Bestatin JNCI J Natl Cancer Inst (2003) 95(14): 1053-1061 doi:10.1093/jnci/95.14.1053. Learn more>>

9) Lens/Opthamology 

Deepak Chandra et al. Inhibition of Fiber Cell Globulization and Hyperglycemia-Induced Lens Opacification by Aminopeptidase Inhibitor Bestatin IOVS July 2002 43:2285-2292 Learn more>>

10) Cardiac Fibroblasts

Paul Lijnen, et al, Effect of bestatin on angiotensin I-, II- and III-induced collagen gel contraction in cardiac fibroblasts Journal of Renin-Angiotensin-Aldosterone System December 2004 vol. 5 no. 4 183-188. Learn more>>

11) Angiogenesis & Cancer

JJ Gao et al, LYP, a bestatin dimethylaminoethyl ester, inhibited cancer angiogenesis both in vitro andin vivo. Microvasc Res, September 1, 2011; 82(2): 122-30. Learn more>>

12) Angiogenesis & Tumor Metastasis

Y Luan, et al, L, YP3, a new bestatin derivative for aminopeptidase N inhibition. Med Chem, January 1, 2011; 7(1): 32-36. Learn more>>

13) Immunology

Scornik O.A.; Botbol V., Bestatin as an Experimental Tool in Mammals Current Drug Metabolism, Volume 2, Number 1  pp. 67-85(19). Learn more>>

14) Drug Development

L. Chen, Y. Teng, W. Xu,  Progress in the Development of Bestatin Analogues as Aminopeptidases Inhibitors. Current Medicinal Chemistry Volume 18 Issue 7. pp.964-976 (13). Learn more>>


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  1. Bestatin (Ubenimex)
    Bestatin (Ubenimex)

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