関: ubenimex

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/06/24 15:32:55」(JST)

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Ubenimex (INN), also known as bestatin, is a competitive protease inhibitor. It is an inhibitor of aminopeptidase B,^[2] leukotriene A4 hydrolase,^[3] aminopeptidase N.^[4] It is being studied for use in the treatment of acute myelocytic leukemia.^[5]

Crystal structure of bestatin in the binding pocket of leukotriene A4 hydrolase. Rendered from PDB 1HS6.

References[edit]

^ N-((2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl)-L-leucine at Sigma-Aldrich
^ Umezawa,H., Aoyagi,T., Suda,H., Hamada,M. & Takeuchi,T. (1976). Bestatin, an inhibitor of aminopeptidase B, produced by actinomycetes. (29). pp. 97–99.
^ Muskardin,D.T., Voelkel,N.F. & Fitzpatrick,F.A. (1994). Modulation of pulmonary leukotriene formation and perfusion pressure by bestatin, an inhibitor of leukotriene A4 hydrolase. (48). pp. 131–137.
^ K Sekine, H Fujii and F Abe (1999). Induction of apoptosis by bestatin (ubenimex) in human leukemic cell lines 13 (5). pp. 729–734.
^ Hirayama, Y; Sakamaki, S; Takayanagi, N; Tsuji, Y; Sagawa, T; Chiba, H; Matsunaga, T; Niitsu, Y (2003). "Chemotherapy with ubenimex corresponding to patient age and organ disorder for 18 cases of acute myelogeneous leukemia in elderly patients--effects, complications and long-term survival". Gan to kagaku ryoho. Cancer & chemotherapy 30 (8): 1113–8. PMID 12938265.

External links[edit]

The MEROPS online database for peptidases and their inhibitors: Bestatin

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1. 切除可能非小細胞肺癌における全身補助化学療法 adjuvant systemic therapy in resectable non small cell lung cancer

English Journal

The effects of bestatin on humoral response to sheep erythrocytes in non-treated and cyclophosphamide-immunocompromised mice.

Lis M, Szczypka M, Suszko A, Obmińska-Mrukowicz B.SourceDepartment of Biochemistry, Pharmacology and Toxicology, Faculty of Veterinary Medicine, Wrocław University of Environmental and Life Sciences , Wrocław , Poland.
Immunopharmacology and immunotoxicology.Immunopharmacol Immunotoxicol.2013 Feb;35(1):133-8. doi: 10.3109/08923973.2012.719524. Epub 2012 Sep 7.
The effects of bestatin on humoral immune response to sheep erythrocytes (SRBC) and restoration of the response impaired by a single cyclophosphamide dose (350 mg/kg) were tested on mice. Bestatin (at doses of 10, 1, and 0.1 mg/kg) was administered intraperitoneally (i.p.) 5 or 10 times. The pha
PMID 22957713

Aminopeptidase activity profile in cultured human osteoblasts.

Lucena G, Reyes-Botella C, García-Martínez O, Díaz-Rodríguez L, Alba F, Ruiz C.Source1Institute of Neurosciences, University of Granada, Granada, Spain.
Biological research for nursing.Biol Res Nurs.2013 Jan;15(1):56-61. doi: 10.1177/1099800411414870. Epub 2011 Jul 15.
Aminopeptidases (APs) are enzymes involved in a wide variety of biological processes and present in a variety of different cell populations. The authors studied these enzymes in primary cultured human osteoblasts in order to establish an activity profile and thereby contribute to knowledge of bone t
PMID 21765118

Japanese Journal

Purification and Characterization of Porcine Skeletal Muscle Aminopeptidase T, a Novel Metallopeptidase Homologous to Leukotriene A_4 Hydrolase

Sarker Mohammed Alamgir,Matsuda Shinji,Mizutani Osamu [他],RAO Shengbin,MIGITA Koshiro,GOTO YAMAMOTO Nami,IEFUJI Haruyuki,NISHIMURA Toshihide
Bioscience, biotechnology, and biochemistry 75(6), 1154-1159, 2011-06-23
… The enzyme activity was strongly inhibited by bestatin and was negatively affected by ethylenediaminetetraacetic acid (EDTA). …
NAID 10029328354

The Effect of Different Species Aminopeptidase N Structure on the Activity Screening of Aminopeptidase N Inhibitor

Wang Xuejian,Zhang Lei,Yang Kanghui [他],Zhang Cai,Zhang Jian,Fang Hao,Xu Wenfang
Biological and Pharmaceutical Bulletin 33(10), 1658-1665, 2010
… In the present study, we got a novel compound 16l which markedly inhibited the enzyme activity of porcine APN, and the inhibition constant, Ki, of 16l are similar to the positive medicine Bestatin determined using porcine APN. …
NAID 130000402358

Structure of aminopeptidase N from Escherichia coli complexed with the transition-state analogue aminophosphinic inhibitor PL250.

Fournié-Zaluski Marie Claude,Poras Hervé,Roques Bernard P,Nakajima Yoshitaka,Ito Kiyoshi,Yoshimoto Tadashi
Acta crystallographica. Section D, Biological crystallography 65(8), 814-822, 2009-08
… The strength of the phosphinic zinc binding and the occupancy of the S'(2) subsite account for the 100-fold increase in affinity of PL250 compared with the dipeptide-derived inhibitor bestatin (K(i) = 4.1 x 10(-6) M). …
NAID 120001664851

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リンク元

「ウベニメクス」

Ubenimex
	IUPAC name (2S)-2-[[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]amino]-4-methylpentanoic acid
	Other names Bestatin; N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine
Identifiers
CAS number	58970-76-6, ; 65391-42-6 (HCl)
PubChem	72172
ChEMBL	CHEMBL29292
Jmol-3D images	Image 1
	SMILES CC(C)C[C@@H](C(=O)O)NC(=O)[C@H]([C@@H](CC1=CC=CC=C1)N)O ;
Properties
Molecular formula	C16H24N2O4
Molar mass	308.37 g mol−1
Melting point	245 °C (dec.)
Hazards
S-phrases	S22 S24/25
	(verify) (what is: /?); Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
	Infobox references

　　[★]

英: ubenimex
商: ベスタチン Bestatin
関: その他の腫瘍用薬

[1] N-((2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl)-L-leucine at Sigma-Aldrich

[2] Umezawa,H., Aoyagi,T., Suda,H., Hamada,M. & Takeuchi,T. (1976). Bestatin, an inhibitor of aminopeptidase B, produced by actinomycetes. (29). pp. 97–99.

[3] Muskardin,D.T., Voelkel,N.F. & Fitzpatrick,F.A. (1994). Modulation of pulmonary leukotriene formation and perfusion pressure by bestatin, an inhibitor of leukotriene A4 hydrolase. (48). pp. 131–137.

[4] K Sekine, H Fujii and F Abe (1999). Induction of apoptosis by bestatin (ubenimex) in human leukemic cell lines 13 (5). pp. 729–734.

[5] Hirayama, Y; Sakamaki, S; Takayanagi, N; Tsuji, Y; Sagawa, T; Chiba, H; Matsunaga, T; Niitsu, Y (2003). "Chemotherapy with ubenimex corresponding to patient age and organ disorder for 18 cases of acute myelogeneous leukemia in elderly patients--effects, complications and long-term survival". Gan to kagaku ryoho. Cancer & chemotherapy 30 (8): 1113–8. PMID 12938265.

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Bestatin