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来普霉素A

来普霉素A用途

Leptomycin A 是链霉菌的代谢物,是 CRM1 的抑制剂,阻断CRM1和核出口信号相互作用,阻止多种蛋白质的核出口。Leptomycin A 抑制 HIV-1的复制。活性略低于 Leptomycin B。

来普霉素A名称

[ CAS 号 ]:
87081-36-5

[ 中文名 ]:
来普霉素A

[ 英文名 ]:
Leptomycin A

[英文别名 ]:

C32H46O6
Leptomycin A
Jildamycin

来普霉素A生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 抗感染 >> HIV

研究领域 >> 感染

信号通路 >> 跨膜转运 >> CRM1

[ 靶点 ]

CRM1[1][2].

[参考文献]

[1]. Kudo, N., et al. Leptomycin B inhibition of signal-mediated nuclear export by direct binding to CRM1. Exp. Cell Res. 242(2), 540-547 (1998).

[2]. Wolff B, et al. Leptomycin B is an inhibitor of nuclear export: inhibition of nucleo-cytoplasmic translocation of the human immunodeficiency virus type 1 (HIV-1) Rev protein and Rev-dependent mRNA. Chem Biol. 1997 Feb;4(2):139-47.

来普霉素A物理化学性质

[ 密度 ]:
1.079g/cm3

[ 沸点 ]:
717.7ºC at 760 mmHg

[ 分子式 ]:
C₃₂H₄₆O₆

[ 分子量 ]:
526.70400

[ 闪点 ]:
224.2ºC

[ 精确质量 ]:
526.32900

[ PSA ]:
100.90000

[ LogP ]:
6.39460

[ 折射率 ]:
1.544

[ 储存条件 ]:
?20°C

来普霉素A毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RA5391000

CHEMICAL NAME :: 2,10,12,16,18-Nonadecapentaenoic acid, 19-(3,6-dihydro-3-methyl-6-oxo-2H-pyran-2-yl)- 3,5,7,9,11,15,17-heptamethyl-6-hydroxy-8-oxo-

CAS REGISTRY NUMBER :: 87081-36-5

LAST UPDATED :: 199401

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C32-H46-O6

MOLECULAR WEIGHT :: 526.78

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

MUTATION DATA

TYPE OF TEST :: Mutation test systems - not otherwise specified

TEST SYSTEM :: Yeast - Schizosaccharomyces pombe

DOSE/DURATION :: 10 ug/L

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 38,1573,1985

来普霉素A安全信息

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P260-P280-P301 + P310-P311

[ 危害码 (欧洲) ]:
F,T

[ 风险声明 (欧洲) ]:
11-23/24/25-39/23/24/25

[ 安全声明 (欧洲) ]:
16-36/37-45

[ 危险品运输编码 ]:
UN 1230 3/PG 2

来普霉素A文献

Serine residue 115 of MAPK-activated protein kinase MK5 is crucial for its PKA-regulated nuclear export and biological function.

Cell. Mol. Life Sci. 68 , 847-62, (2011)

The mitogen-activated protein kinase-activated protein kinase-5 (MK5) resides predominantly in the nucleus of resting cells, but p38(MAPK), extracellular signal-regulated kinases-3 and -4 (ERK3 and ER...

Leptomycins A and B, new antifungal antibiotics. I. Taxonomy of the producing strain and their fermentation, purification and characterization.

J. Antibiot. 36(6) , 639-45, (1983)

A strain of Streptomyces was found to produce new antifungal antibiotics. The active compounds were purified and separated into two substances named leptomycin A and B by high performance liquid chrom...

Leptomycins A and B, new antifungal antibiotics. II. Structure elucidation.

J. Antibiot. 36(6) , 646-50, (1983)

The structures of new antifungal antibiotics, leptomycins A and B produced by Streptomyces sp. ATS1287 were determined as described below (Fig. 1) on the basis of their spectral and chemical character...

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