Page last updated: 2024-11-08

leptomycin b

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID435143
MeSH IDM0116474

Synonyms (7)

Synonym
leptomycin b ,
87081-35-4
FT-0627793
ci 940;lmb
elactocin; mantuamycin; antibiotic ci 940
DTXSID60861093
17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-19-(3-methyl-6-oxo-3,6-dihydro-2h-pyran-2-yl)-8-oxononadeca-2,10,12,16,18-pentaenoic acid

Research Excerpts

Overview

Leptomycin B (LMB) is an antibiotic originally isolated from Streptomyces. It inhibits the export of proteins containing a nuclear export signal from the nucleus to the cytoplasm. The drug has significant in vitro potency but limited in vivo efficacy due to toxicity.

ExcerptReferenceRelevance
"Leptomycin B (LMB) is a highly specific inhibitor of CRM1, a cellular karyopherin-β that transports nuclear export signal-containing proteins from the nucleus to the cytoplasm. "( Role of immediate early protein ICP27 in the differential sensitivity of herpes simplex viruses 1 and 2 to leptomycin B.
Lengyel, J; Park, D; Rice, SA, 2013
)
2.05
"Leptomycin B (LMB) is an antibiotic originally isolated from Streptomyces that has the ability to inhibit the export of proteins containing a nuclear export signal from the nucleus to the cytoplasm."( Combined effects of p53 gene therapy and leptomycin B in human esophageal squamous cell carcinoma.
Akutsu, Y; Brooks, R; Hoshino, I; Komatsu, A; Matsubara, H; Matsushita, K; Miyazawa, Y; Murakami, K; Nishimori, T; Ochiai, T; Sakata, H; Yoneyama, Y; Yoshida, M, 2008
)
1.33
"Leptomycin B (LMB) is a highly specific inhibitor of CRM1 with significant in vitro potency but limited in vivo efficacy due to toxicity."( Identification of nuclear export inhibitors with potent anticancer activity in vivo.
Craig, DA; Dong, SD; Murli, S; Mutka, SC; Timmermans, PB; Ward, SL; Yang, WQ, 2009
)
1.07
"Leptomycin B (LMB) is a Streptomyces metabolite that causes specific inhibition of the cell cycle of fission yeast and mammalian cells."( Nucleo-cytoplasmic transport of proteins as a target for therapeutic drugs.
Yashiroda, Y; Yoshida, M, 2003
)
1.04
"Leptomycin B (LMB) is a Streptomyces metabolite that inhibits the chromosomal region maintenance (CRM)1-dependent nuclear export of proteins. "( Involvement of nuclear accumulation of heat shock protein 27 in leptomycin B-induced apoptosis in HeLa cells.
Imoto, M; Tashiro, E; Tsuchiya, A; Yoshida, M, 2005
)
2.01
"Leptomycin B (LMB) is a Streptomyces metabolite that causes the specific inhibition of the nuclear export of proteins containing a nuclear export signal (NES). "( Involvement of protein phosphatase 2A nuclear accumulation and subsequent inactivation of activator protein-1 in leptomycin B-inhibited cyclin D1 expression.
Imoto, M; Tashiro, E; Tsuchiya, A; Yoshida, M, 2007
)
1.99
"Leptomycin B (LMB) is a Streptomyces metabolite that inhibits nuclear export of the human immunodeficiency virus type 1 regulatory protein Rev at low nanomolar concentrations. "( Leptomycin B inhibition of signal-mediated nuclear export by direct binding to CRM1.
Horinouchi, S; Kudo, N; Schreiner, EP; Sekimoto, T; Wolff, B; Yanagida, M; Yoneda, Y; Yoshida, M, 1998
)
3.19
"Leptomycin B is a cytotoxin which directly interacts with and inhibits the action of CRM1, an essential mediator of the nuclear exit of proteins containing nuclear export signals (NES) of the HIV1 REV type. "( An inhibitor of nuclear export activates the p53 response and induces the localization of HDM2 and p53 to U1A-positive nuclear bodies associated with the PODs.
Laín, S; Lane, DP; Lane, EB; Midgley, C; Sparks, A, 1999
)
1.75
"Leptomycin B (LMB) is a specific inhibitor of Crm1-dependent nuclear export of proteins. "( A single amino acid substitution in the ICP27 protein of herpes simplex virus type 1 is responsible for its resistance to leptomycin B.
Goshima, F; Koshizuka, T; Murata, T; Nishiyama, Y; Takakuwa, H, 2001
)
1.96

Effects

ExcerptReferenceRelevance
"Leptomycin B (LMB) has recently been found to increase the protein level and transcriptional activity of p53 by interfering with nucleocytoplasmic export and subsequent degradation by the proteasome."( Leptomycin B stabilizes and activates p53 in primary prostatic epithelial cells and induces apoptosis in the LNCaP cell line.
Kiviharju, TM; Lecane, PS; Peehl, DM; Sellers, RG, 2003
)
2.48

Actions

ExcerptReferenceRelevance
"Leptomycin B did not increase the speed of entry of the fusion protein, suggesting that the relatively slow entry of the fusion protein is not due to the CRM1-dependent nuclear export of the protein."( An N-terminal segment of the active component of the bacterial genotoxin cytolethal distending toxin B (CDTB) directs CDTB into the nucleus.
Ikura, M; Komatsuzawa, H; Kurihara, H; Nishikubo, S; Ohara, M; Oswald, E; Sugai, M; Ueno, Y, 2003
)
1.04

Treatment

Leptomycin B (LMB) treatment demonstrated that VP1 export from nucleus to cytoplasm occurred through a chromosome region maintenance 1 (CRM1)-dependent pathway. Treatment with LMB significantly reduced the rate of nuclear export 4 -10-fold, thereby increasing parathyroid hormone-related protein concentration in the nucleus/nucleolus.

ExcerptReferenceRelevance
"Leptomycin B (LMB) treatment demonstrated that VP1 export from nucleus to cytoplasm occurred through a chromosome region maintenance 1 (CRM1)-dependent pathway."( Identification of nuclear localization signal and nuclear export signal of VP1 from the chicken anemia virus and effects on VP2 shuttling in cells.
Cheng, JH; Chuang, PC; Hsu, SL; Lai, GH; Lee, MS; Lien, YY; Sun, FC, 2019
)
1.24
"Leptomycin B treatment accumulated XRCC4(N326L) in the nucleus but only partially rescued radiosensitivity of M10-XRCC4(N326L)."( Asparagine 326 in the extremely C-terminal region of XRCC4 is essential for the cell survival after irradiation.
Fukuchi, M; Imamichi, S; Matsumoto, Y; Sharma, MK; Wanotayan, R, 2015
)
1.14
"In leptomycin B (LMB)-treated cells, endogenous ZBP1 efficiently accumulated in nuclear foci, which overlapped PML oncogenic domains (PODs) or nuclear bodies (NBs)."( Intracellular localization of human ZBP1: Differential regulation by the Z-DNA binding domain, Zalpha, in splice variants.
Ahn, JH; Kim, KK; Kim, YG; Park, MY; Pham, HT, 2006
)
0.85
"Leptomycin B treatment significantly reduced the rate of nuclear export 4 -10-fold, thereby increasing parathyroid hormone-related protein concentration in the nucleus/nucleolus about 2-fold."( Dynamics of leptomycin B-sensitive nucleocytoplasmic flux of parathyroid hormone-related protein.
Gillespie, MT; Henderson, B; Jans, DA; Lam, MH, 2001
)
1.41
"Treatment with leptomycin B resulted in the nuclear retention of HECTD1, which was associated with the loss of SNAIL expression."( HECTD1 regulates the expression of SNAIL: Implications for epithelial‑mesenchymal transition.
De Geyter, C; Jia, Z; Peng, Y; Wang, X; Zhang, H, 2020
)
0.9
"Treatment with leptomycin B (LMB), a specific inhibitor of nuclear export mediated by leucine-rich nuclear export signal (NES), also causes nuclear accumulation of wild-type L-periaxin."( Nuclear export of L-periaxin, mediated by its nuclear export signal in the PDZ domain.
Shi, Y; Yang, T; Zhang, L, 2014
)
0.74
"Treatment with leptomycin B, a nuclear export inhibitor, increased the amount of nuclear Cas9 and enabled mutation induction in GV oocytes."( Efficient mutagenesis by CRISPR/Cas system during meiotic maturation of porcine oocytes.
Fujii, W; Naito, K; Onuma, A; Sugiura, K, 2017
)
0.79
"Treatment with leptomycin B induced nuclear accumulation of both endogenous and overexpressed Dpr1."( Dapper1 is a nucleocytoplasmic shuttling protein that negatively modulates Wnt signaling in the nucleus.
Chen, YG; Gao, X; Li, X; Meng, A; Ning, Y; Wen, J; Zhang, L, 2008
)
0.69
"Treatment with leptomycin B, a potent and specific inhibitor of the exportin CRM1, induced its accumulation into the nucleus, suggesting that CRM1 mediates the nuclear export of Ngn3."( Neurogenin 3 cellular and subcellular localization in the developing and adult hippocampus.
Arevalo, MA; Garcia-Fernandez, C; Garcia-Segura, LM; Membrive, G; Simon-Areces, J, 2010
)
0.7
"Treatment with leptomycin B, an inhibitor of CRM-1 receptor-mediated export, inhibited export of unliganded GFP-VDR but did not influence export of liganded GFP-VDR or YFP-RXR."( Retinoid X receptor dominates the nuclear import and export of the unliganded vitamin D receptor.
Barsony, J; Prüfer, K, 2002
)
0.65
"Treatment with leptomycin B, a potent inhibitor of CRM1/exportin1, disrupted the cytoplasmic localization of both Flag-tagged CDC25B and NES-fused GFP."( Nuclear export signal in CDC25B.
Hirata, M; Ishizaka, Y; Matsunaga, T; Nakagama, H; Ohtsubo, M; Shimura, M; Uchida, S; Yamashita, K; Yoshida, M, 2004
)
0.66
"Upon treatment with leptomycin B, a specific inhibitor of the nuclear export receptor CRM1, a marked nuclear accumulation of TIS11 was observed, indicating that TIS11 shuttles between the nucleus and the cytoplasm."( Identification of nuclear import and export signals within the structure of the zinc finger protein TIS11.
Kaneda, N; Morita, N; Murata, T; Yoshino, Y, 2002
)
0.63

Bioavailability

ExcerptReferenceRelevance
" We propose that nucleo-mitochondrial translocation of proteins is more widespread than previously anticipated providing additional means to control protein bioavailability as well as cellular communication between both compartments."( NOA1, a novel ClpXP substrate, takes an unexpected nuclear detour prior to mitochondrial import.
Al-Furoukh, N; Baker, TA; Braun, T; Kardon, JR; Krüger, M; Szibor, M, 2014
)
0.4

Dosage Studied

ExcerptRelevanceReference
" Binding to XPO1 was quantitated from SINE compound treated adherent and suspension cells in vitro, dosed ex vivo human peripheral blood mononuclear cells (PBMCs), and PBMCs from mice dosed orally with drug in vivo."( A method for quantification of exportin-1 (XPO1) occupancy by Selective Inhibitor of Nuclear Export (SINE) compounds.
Baloglu, E; Crochiere, ML; Del Alamo, D; Donovan, S; Kauffman, M; Klebanov, B; Landesman, Y; Lee, M; Shacham, S, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (568)

TimeframeStudies, This Drug (%)All Drugs %
pre-19909 (1.58)18.7374
1990's45 (7.92)18.2507
2000's368 (64.79)29.6817
2010's137 (24.12)24.3611
2020's9 (1.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 38.21

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index38.21 (24.57)
Research Supply Index6.35 (2.92)
Research Growth Index5.53 (4.65)
Search Engine Demand Index55.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (38.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.18%)5.53%
Reviews15 (2.63%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other554 (97.19%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]