Kinesin spindle protein (KSP) inhibitors in combination with chemotherapeutic agents for cancer therapy.


:A diverse group of proteins, the activities of which are precisely orchestrated during mitosis, have emerged as targets for cancer therapeutics; these include the Aurora kinases (AKs), Polo-like kinases (PLKs), and the kinesin spindle protein (KSP). KSP is essential for the proper separation of spindle poles during mitosis. Agents that target KSP selectively act on cells undergoing cell division, which means that KSP inhibitors are mitosis-specific drugs, and have demonstrated remarkable activities in vitro. However, a significant obstacle to the success of KSP inhibitors is that these compounds, with tremendous efficacy in vitro, have demonstrated little or even no antitumor activity in vivo. Accumulated data suggest that a combination of KSP inhibitors with various cytostatic drugs will result in a more powerful tumor-killing effect than monotherapy. Combination therapies might predominate and represent the next frontier in the discovery research of KSP inhibitors as potential anticancer drugs. Few published studies have reviewed combination therapy using KSP inhibitors. Herein we provide a comprehensive review of the literature on KSP inhibitor monotherapy and therapeutic combinations. The current state and problems are also discussed.






Song H,Zhou S,Wang R,Li S




Has Abstract


2013-11-01 00:00:00












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    authors: Vishnu MS,Pavankumar V,Kumar S,Raja AS

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    authors: Fang CJ,Gui L,Zhang X,Moen DR,Li K,Frankowski KJ,Lin HJ,Schoenen FJ,Chou TF

    更新日期:2015-01-01 00:00:00

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    authors: Costa B,Taliani S,Da Pozzo E,Barresi E,Robello M,Cavallini C,Cosconati S,Da Settimo F,Novellino E,Martini C

    更新日期:2017-08-22 00:00:00

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    authors: Xing L,Devadas B,Devraj RV,Selness SR,Shieh H,Walker JK,Mao M,Messing D,Samas B,Yang JZ,Anderson GD,Webb EG,Monahan JB

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  • A Novel Prodrug of a γ-Glutamylcyclotransferase Inhibitor Suppresses Cancer Cell Proliferation in vitro and Inhibits Tumor Growth in a Xenograft Mouse Model of Prostate Cancer.

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    pub_type: 杂志文章


    authors: Ii H,Yoshiya T,Nakata S,Taniguchi K,Hidaka K,Tsuda S,Mochizuki M,Nishiuchi Y,Tsuda Y,Ito K,Kageyama S,Yoshiki T

    更新日期:2018-01-22 00:00:00

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    pub_type: 杂志文章


    authors: Mittendorf J,Weigand S,Alonso-Alija C,Bischoff E,Feurer A,Gerisch M,Kern A,Knorr A,Lang D,Muenter K,Radtke M,Schirok H,Schlemmer KH,Stahl E,Straub A,Wunder F,Stasch JP

    更新日期:2009-05-01 00:00:00

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    pub_type: 杂志文章


    authors: Qi X,Li J,Wei W,Su T,Zuo G,Pan X,Zhang J,Dong W

    更新日期:2017-01-20 00:00:00

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    pub_type: 杂志文章


    authors: Méndez-Lucio O,Tran J,Medina-Franco JL,Meurice N,Muller M

    更新日期:2014-03-01 00:00:00

  • An efficient synthesis of a hydroxyethylamine (HEA) isostere and its α-aminophosphonate and phosphoramidate derivatives as potential anti-HIV agents.

    abstract::HIV protease is a promising drug target for AIDS therapy, and several potent HIV-1 protease inhibitors have been reported to date. Although existing inhibitors exhibit high selectivity, they have also been associated with severe side effects and the possible emergence of therapeutic resistance. As HIV protease cleaves...


    pub_type: 杂志文章


    authors: Bhattacharya AK,Rana KC,Pannecouque C,De Clercq E

    更新日期:2012-09-01 00:00:00

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    pub_type: 杂志文章


    authors: Rossato G,Ernst B,Smiesko M,Spreafico M,Vedani A

    更新日期:2010-12-03 00:00:00

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    pub_type: 杂志文章


    authors: Libardo MD,Cervantes JL,Salazar JC,Angeles-Boza AM

    更新日期:2014-08-01 00:00:00

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    authors: Di Santo R,Costi R,Artico M,Ragno R,Lavecchia A,Novellino E,Gavuzzo E,La Torre F,Cirilli R,Cancio R,Maga G

    更新日期:2006-01-01 00:00:00

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    pub_type: 杂志文章


    authors: Chakraborty I,Carrington SJ,Mascharak PK

    更新日期:2014-06-01 00:00:00

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    authors: Hocke C,Prante O,Salama I,Hübner H,Löber S,Kuwert T,Gmeiner P

    更新日期:2008-05-01 00:00:00

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    pub_type: 杂志文章


    authors: Park SJ,Baars H,Mersmann S,Buschmann H,Baron JM,Amann PM,Czaja K,Hollert H,Bluhm K,Redelstein R,Bolm C

    更新日期:2013-02-01 00:00:00

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    pub_type: 杂志文章


    authors: Geyer M,Wellner E,Jurva U,Saloman S,Armstrong D,Tacke R

    更新日期:2015-05-01 00:00:00

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    authors: Sundriyal S,Malmquist NA,Caron J,Blundell S,Liu F,Chen X,Srimongkolpithak N,Jin J,Charman SA,Scherf A,Fuchter MJ

    更新日期:2014-10-01 00:00:00

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    pub_type: 杂志文章,评审


    authors: Jacobsen MF,Cló E,Mokhir A,Gothelf KV

    更新日期:2007-06-01 00:00:00

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    pub_type: 杂志文章


    authors: Pozzi C,Di Pisa F,De Luca F,Benvenuti M,Docquier JD,Mangani S

    更新日期:2018-07-18 00:00:00

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    pub_type: 杂志文章


    authors: Yu J,Pandey SK,Khatri H,Prakash TP,Swayze EE,Seth PP

    更新日期:2014-09-01 00:00:00

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    pub_type: 杂志文章


    authors: Drennen B,Scheenstra JA,Yap JL,Chen L,Lanning ME,Roth BM,Wilder PT,Fletcher S

    更新日期:2016-04-19 00:00:00

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    pub_type: 杂志文章


    authors: Rustler K,Pockes S,König B

    更新日期:2019-03-22 00:00:00

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    pub_type: 杂志文章,评审


    authors: Fershtat LL,Makhova NN

    更新日期:2017-05-09 00:00:00

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    pub_type: 杂志文章


    authors: Castellano S,Milite C,Ragno R,Simeoni S,Mai A,Limongelli V,Novellino E,Bauer I,Brosch G,Spannhoff A,Cheng D,Bedford MT,Sbardella G

    更新日期:2010-03-01 00:00:00

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    pub_type: 杂志文章


    authors: Figueras A,Miralles-Llumà R,Flores R,Rustullet A,Busqué F,Figueredo M,Font J,Alibés R,Maréchal JD

    更新日期:2012-06-01 00:00:00

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    pub_type: 杂志文章


    authors: Isono A,Tsuji M,Sanada Y,Matsushita A,Masunaga S,Hirayama T,Nagasawa H

    更新日期:2019-04-17 00:00:00

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    pub_type: 杂志文章


    authors: Ferlin MG,Bortolozzi R,Brun P,Castagliuolo I,Hamel E,Basso G,Viola G

    更新日期:2010-08-02 00:00:00

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    pub_type: 杂志文章


    authors: Pellicciari R,Filosa R,Fulco MC,Marinozzi M,Macchiarulo A,Novak C,Natalini B,Hermit MB,Nielsen S,Sager TN,Stensbøl TB,Thomsen C

    更新日期:2006-03-01 00:00:00

  • Repurposing of Human Kinase Inhibitors in Neglected Protozoan Diseases.

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    pub_type: 杂志文章,评审


    authors: Dichiara M,Marrazzo A,Prezzavento O,Collina S,Rescifina A,Amata E

    更新日期:2017-08-22 00:00:00

  • Synthesis and Antibacterial Evaluation of Bis-thiazolium, Bis-imidazolium, and Bis-triazolium Derivatives.

    abstract::Given the worldwide spread of bacterial drug resistance, there is an urgent need to develop new compounds that exhibit potent antibacterial activity and that are unimpaired by this phenomenon. Quaternary ammonium compounds have been used for many years as disinfectants, but recent advances have shown that polycationic...


    pub_type: 杂志文章


    authors: Thomas B,Duval RE,Fontanay S,Varbanov M,Boisbrun M

    更新日期:2019-07-03 00:00:00