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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/09/17 16:56:47」(JST)

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Ubenimex (INN), also known by the brand name Bestatin, is a competitive protease inhibitor. It is an inhibitor of aminopeptidase B,^[2] leukotriene A4 hydrolase,^[3] and aminopeptidase N.^[4] It is being studied for use in the treatment of acute myelocytic leukemia.^[5] It is derived from Streptomyces olivoreticuli.^[6]

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

References

^ 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.
^ Bauvois, B; Dauzonne, D (January 2006). "Aminopeptidase-N/CD13 (EC 3.4.11.2) inhibitors: Chemistry, biological evaluations, and therapeutic prospects". Medicinal Research Reviews 26 (1): 88–130. doi:10.1002/med.20044. PMID 16216010.

External links

The MEROPS online database for peptidases and their inhibitors: Bestatin

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UpToDate Contents

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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

Induction of leucine aminopeptidase (LAP) like activity with wounding and methyl jasmonate in pigeonpea (Cajanas cajan) suggests the role of these enzymes in plant defense in leguminosae.

Lomate PR, Hivrale VK.SourceDepartment of Biochemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431004, Maharashtra, India.
Plant physiology and biochemistry : PPB / Societe francaise de physiologie vegetale.2011 Jun;49(6):609-16. Epub 2011 Mar 3.
Aminopeptidases are ubiquitous in nature and their activities have been identified in several plant species. Leucine aminopeptidases (LAPs) are predominantly studied in solanaceous plants and are induced in response to wounding, herbivory and methyl jasmonate (MeJA). The functions of plant aminopept
PMID 21420308

Aminopeptidase-N/CD13 is a potential proapoptotic target in human myeloid tumor cells.

Piedfer M, Dauzonne D, Tang R, N'guyen J, Billard C, Bauvois B.Source*Centre de Recherche des Cordeliers, Institut National de la Sante et de la Recherche Medicale (INSERM) U872, Paris, France;
The FASEB journal : official publication of the Federation of American Societies for Experimental Biology.2011 May 12. [Epub ahead of print]
The transmembrane metalloprotease aminopeptidase-N (APN)/CD13 is overexpressed in various solid and hematological malignancies in humans, including acute myeloid leukemia (AML) and is thought to influence tumor progression. Here, we investigated the contribution of APN/CD13 to the regulation of grow
PMID 21566207

Japanese Journal

高齢者急性骨髄性白血病に対する寛解導入療法の投与方法に関するランダム化比較試験(JALSG GML200研究) (特集血液腫瘍に対する重要な臨床試験と国内外の診療に及ぼすインパクト)

脇田充史
血液内科 66(4), 481-489, 2013-04
NAID 40019688416

Randomized comparison of fixed-schedule versus response-oriented individualized induction therapy and use of ubenimex during and after consolidation therapy for elderly patients with acute myeloid leukemia : the JALSG GML200 Study

WAKITA Atsushi,OHTAKE Shigeki,TAKADA Satoru,YAGASAKI Fumiharu,KOMATSU Hirokazu,MIYAZAKI Yasushi,KUBO Kohmei,KIMURA Yukihiko,TAKESHITA Akihiro,ADACHI Yoko,KIYOI Hitoshi,YAMAGUCHI Takuhiro,YOSHIDA Minoru,OHNISHI Kazunori,MIYAWAKI Shuichi,NAOE Tomoki,UEDA Ryuzo,OHNO Ryuzo
International journal of hematology 96(1), 84-93, 2012-07-01
NAID 10030954605

IB-IIIA期非小細胞癌完全切除の補助化学療法は行うべきであるか<EBMに基づく肺癌診療のPros and Cons>

國頭英夫
肺癌 42(7), 771-774, 2002-12-20
NAID 110003141868

Related Pictures

★リンクテーブル★

リンク元	「ウベニメクス」「Bestatin」

「ウベニメクス」

Ubenimex^[1]
Names
	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 Registry Number	58970-76-6; 65391-42-6 (HCl)
ChEMBL	ChEMBL29292
ChemSpider	65145
	InChI InChI=1S/C16H24N2O4/c1-10(2)8-13(16(21)22)18-15(20)14(19)12(17)9-11-6-4-3-5-7-11/h3-7,10,12-14,19H,8-9,17H2,1-2H3,(H,18,20)(H,21,22)/t12-,13+,14+/m1/s1; Key: VGGGPCQERPFHOB-RDBSUJKOSA-N ; InChI=1/C16H24N2O4/c1-10(2)8-13(16(21)22)18-15(20)14(19)12(17)9-11-6-4-3-5-7-11/h3-7,10,12-14,19H,8-9,17H2,1-2H3,(H,18,20)(H,21,22)/t12-,13+,14+/m1/s1; Key: VGGGPCQERPFHOB-RDBSUJKOBZ ;
Jmol-3D images	Image
PubChem	72172
	SMILES CC(C)C[C@@H](C(=O)O)NC(=O)[C@H]([C@@H](CC1=CC=CC=C1)N)O ;
UNII	I0J33N5627
Properties
Chemical formula	C16H24N2O4
Molar mass	308.38 g·mol−1
Melting point	245 °C (473 °F; 518 K) (decomposes)
Hazards
S-phrases	S22 S24/25
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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	Infobox references