Bovine microsatellite dinucleotide repeat polymorphisms at the <i>TEXAN16, TEXAN17, TEXAN18, TEXAN19</i> and <i>TEXAN20</i> loci

Burns, B. M.; Taylor, Jeremy F.; Herring, K. L.; Herring, A. D.; Holder, Mark T.; Holder, D A; Collins, Julianne S.; Davis, Scott K.

doi:10.1111/j.1365-2052.1995.tb03174.x

Cited by 9 publications

(2 citation statements)

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“…Thus, constant efforts have been made in order to block the transport of such substrates of MRP1, with the help of modulatory agents, but with limited success. Since the discovery of MRP1, several modulators of MRP1 have been identified, including indomethacin (Duffy et al, 1998), probenecid (Gollapudi et al, 1997), the leukotriene receptor antagonists MK571 (Burns et al, 1995) and ONO-1078 (Nagayama et al, 1998;Nakano et al, 1998), but none has been successful in clinical practice. Consequently, it is necessary to develop and identify drugs that can successfully inhibit the activity of MRP1 without producing serious adverse effects.…”

Section: Introductionmentioning

confidence: 99%

In vitro, in vivo and ex vivo characterization of ibrutinib: a potent inhibitor of the efflux function of the transporter MRP1

Zhang

Patel

Lin

et al. 2014

British J Pharmacology

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BACKGROUND AND PURPOSEThe transporter, multidrug resistance protein 1 (MRP1, ABCC1), plays a critical role in the development of multidrug resistance (MDR). Ibrutinib is an inhibitor of Bruton's tyrosine kinase. Here we investigated the reversal effect of ibrutinib on MRP1-mediated MDR. EXPERIMENTAL APPROACHCytotoxicity was determined by MTT assay. The expression of protein was detected by Western blot. RT-PCR and Q-PCR were performed to detect the expression of MRP1 mRNA. The intracellular accumulation and efflux of substrates for MRP1 were measured by scintillation counter and flow cytometry. HEK293/MRP1 cell xenografts in nude mice were established to study the effects of ibrutinib in vivo. KEY RESULTSIbrutinib significantly enhanced the cytotoxicity of MRP1 substrates in HEK293/MRP1 and HL60/Adr cells overexpressing MRP1. Furthermore, ibrutinib increased the accumulation of substrates in these MRP1-overexpressing cells by inhibiting the drug efflux function of MRP1. However, mRNA and protein expression of MRP1 remained unaltered after treatment with ibrutinib in MRP1-overexpressing cells. In vivo, ibrutinib enhanced the efficacy of vincristine to inhibit the growth of HEK293/MRP1 tumour xenografts in nude mice. Importantly, ibrutinib also enhances the cytotoxicity of vincristine in primary cultures of leukaemia blasts, derived from patients. CONCLUSIONS AND IMPLICATIONSOur results indicated that ibrutinib significantly increased the efficacy of the chemotherapeutic agents which were MRP1 substrates, in MRP1-overexpressing cells, in vitro, in vivo and ex vivo. These findings will lead to further studies on the effects of a combination of ibrutinib with chemotherapeutic agents in cancer patients overexpressing MRP1. AbbreviationsABC, ATP-binding cassette; BTK, Bruton's tyrosine kinase; MDR, multidrug resistance; MRP1, multidrug resistance protein 1

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Section: Introductionmentioning

confidence: 99%

In vitro, in vivo and ex vivo characterization of ibrutinib: a potent inhibitor of the efflux function of the transporter MRP1

Zhang

Patel

Lin

et al. 2014

British J Pharmacology

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“…One of the major findings of this study was that GSK1904529A, at 0.1 µM, significantly enhanced the sensitivity of HEK293/MRP1 cells to the substrates of MRP1. This effect was more potent than that of MK571 [Burns et al, ], a well‐known inhibitor of MRP1 efflux function. Moreover, GSK1904529A did not enhance the toxic effects of cisplatin, a drug that is not a substrate for the MRP1 transporter.…”

Section: Discussionmentioning

confidence: 99%

GSK1904529A, a Potent IGF‐IR Inhibitor, Reverses MRP1‐Mediated Multidrug Resistance

Gupta

Xie

Narayanan

et al. 2017

J of Cellular Biochemistry

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Overexpression of multidrug-resistant efflux transporters is one of the major causes of chemotherapy failure. MRP1, a 190 kDa efflux transporter, confers resistance to a wide of range of chemotherapeutic drugs. Here we study the cellular effects of GSK1904529A in reversing MRP1-mediated drug resistance. Cytotoxicity of GSK1904529A was determined by MTT assay. Reversal effects of GSK1904529A in combination with MRP1 substrates were determined. The intracellular accumulation and efflux of MRP1 substrate was measured by scintillation counter and protein expression was determined by Western blotting analysis. Cell cycle effects of GSK1904529A in combination with MRP1 substrates were determined by flow cytometric analysis. GSK1904529A, at non-toxic concentrations, enhanced the cytotoxicity of MRP1 substrates in HEK293/MRP1 cells. Furthermore, GSK1904529A increased the intracellular accumulation of [3H]-vinblastine by inhibiting the efflux function of MRP1. GSK1904529A did not alter the expression level of MRP1, induced a G0/G1 phase cell cycle arrest. Our results indicated that GSK1904529A significantly increased the sensitivity of MRP1 overexpressing cells to chemotherapeutic agents. Furthermore, GSK1904529A enhanced the efficacy of chemotherapeutic drugs that are substrates of MRP1.

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Phylogenetic and population genetic analyses suggest a potential species boundary between Mountain (Gazella gazella) and Arabian Gazelles (G. arabica) in the Levant

et al. 2013

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Bovine microsatellite dinucleotide repeat polymorphisms at the TEXAN16, TEXAN17, TEXAN18, TEXAN19 and TEXAN20 loci

Cited by 9 publications

References 0 publications

In vitro, in vivo and ex vivo characterization of ibrutinib: a potent inhibitor of the efflux function of the transporter MRP1

In vitro, in vivo and ex vivo characterization of ibrutinib: a potent inhibitor of the efflux function of the transporter MRP1

GSK1904529A, a Potent IGF‐IR Inhibitor, Reverses MRP1‐Mediated Multidrug Resistance

Phylogenetic and population genetic analyses suggest a potential species boundary between Mountain (Gazella gazella) and Arabian Gazelles (G. arabica) in the Levant

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