The transporter, multidrug resistance protein 1 (MRP1, ABCC1), plays a critical role in the development of (MDR). Ibrutinib is an inhibitor Bruton's tyrosine kinase. Here we investigated reversal effect ibrutinib on MRP1-mediated MDR.Cytotoxicity was determined by MTT assay. expression detected Western blot. RT-PCR and Q-PCR were performed to detect MRP1 mRNA. intracellular accumulation efflux substrates for measured scintillation counter flow cytometry. HEK293/MRP1 cell xenografts nude mice...

Paclitaxel displays clinical activity against a wide variety of solid tumors. However, resistance to paclitaxel significantly attenuates the response chemotherapy. The ABC transporter subfamily C member 10 (ABCC10), also known as multidrug protein 7 (MRP7) efflux transporter, is major mediator resistance. In this study, we show that masitinib, small molecule stem-cell growth factor receptor (c-Kit) tyrosine kinase inhibitor, at nontoxic concentrations, in HEK293 cells transfected with...

// Rishil J. Kathawala 1,8,* , Liuya Wei 1,2,* Nagaraju Anreddy 1 Kang Chen 3,4,5,6 Atish Patel Saeed Alqahtani 7 Yun-Kai Zhang Yi-Jun Wang Kamlesh Sodani Amal Kaddoumi Charles R. Ashby Jr. and Zhe-Sheng Department of Pharmaceutical Sciences, College Pharmacy Health St. John’s University, Queens, NY, USA 2 School Biological Weifang Medical Weifang, People’s Republic China 3 Obstetrics Gynecology, Wayne State University Medicine, Detroit, Michigan, 4 Perinatology Research Branch,...

// Yi-Jun Wang 1 , Yujian Huang 2 Nagaraju Anreddy Guan-Nan Zhang Yun-Kai Meina Xie Derrick Lin Dong-Hua Yang Mingjun Zhe-Sheng Chen Department of Pharmaceutical Sciences, College Pharmacy and Health St. John's University, Queens, NY 11439, USA Biomedical Engineering, The Ohio State Columbus, OH 43210, Correspondence to: Chen, e-mail: chenz@stjohns.edu Zhang, zhang.4882@osu.edu Keywords: tea nanoparticle, tumor xenograft, multidrug resistance, drug delivery, biocompatibility Received:...

ATP-binding cassette subfamily G member 2 (ABCG2) is a of the ABC transporter superfamily proteins, which has been implicated in development multidrug resistance (MDR) cancer, apart from its physiological role to remove toxic substances out cells. The diverse range substrates ABCG2 includes many antineoplastic agents such as topotecan, doxorubicin and mitoxantrone. expression reported be significantly increased some solid tumors hematologic malignancies, correlated poor clinical outcomes. In...

Multidrug resistance protein 7 (MRP7, ABCC10) is a recently identified member of the ATP-binding cassette (ABC) transporter family, which adequately confers to diverse group antineoplastic agents, including taxanes, vinca alkaloids and nucleoside analogs among others. Clinical studies indicate an increased MRP7 expression in non-small cell lung carcinomas (NSCLC) compared normal healthy tissue. Recent revealed paclitaxel sensitivity Mrp7−/− mouse model their wild-type counterparts. This...

Previous reports have shown that some tyrosine kinase inhibitors (TKIs) could inhibit the ATP-binding cassette (ABC) transporters involved in multidrug resistance (MDR). Quizartinib (AC220), a potent class III receptor inhibitor (TKI), was synthesized to selectively FMS-like kinase-3 (FLT3), target treatment of acute myeloid leukemia (AML). is currently under clinical trials for FLT3 ITD and wild-type AML tested combination with chemotherapy. While non-toxic cell lines, quizartinib at 3 μM...

The emergence of drug resistance continues to be a major hurdle towards improving patient outcomes for the treatment Multiple Myeloma. MTI-101 is first-in-class peptidomimetic that binds CD44/ITGA4 containing complex and triggers necrotic cell death in multiple myeloma lines. In this report, we show acquisition correlates with changes expression genes predicted attenuate Ca2+ flux. Consistent acquired resistant genotype, induces rapid robust increase intracellular levels parental cells;...

Abstract Multidrug resistance (MDR) attenuates the chemotherapy efficacy and increases probability of cancer recurrence. The accelerated drug efflux mediated by ATP-binding cassette (ABC) transporters is one major MDR mechanisms. This study investigated if TTT-28, a newly synthesized thiazole-valine peptidomimetic, could reverse ABCB1-mediated in vitro vivo . TTT-28 reversed increased accumulation [ 3 H]-paclitaxel ABCB1 overexpressing cells selectively blocking function ABCB1, but not...

Abstract ABCG2 is a member of the ABC transporter superfamily, which has been implicated in development multidrug resistance (MDR) cancer. Its diverse range substrates includes many antineoplastic agents such as topotecan, doxorubicin and mitoxantrone. expression significantly increased some solid tumors hematologic malignancies, correlated to poorer clinical outcomes. In addition, distinguishing feature cancer stem cells, whereby this membrane impacts chemotherapeutic drugs. To enhance...

Abstract The ATP-binding cassette, subfamily G, isoform 2 protein (ABCG2) is a vital member of the ABC transporter superfamily, which has been involved in multidrug resistance (MDR) cancer. Its diverse range substrates includes many antineoplastic agents such as doxorubicin and mitoxantrone. ABCG2 expression significantly increased some solid tumors hematologic malignancies, correlated to poorer clinical outcomes. In addition, distinguishing feature cancer stem cells, whereby this membranous...

Abstract The ATP-binding cassette, subfamily G, isoform 2 protein (ABCG2) is a vital member of the ABC transporter superfamily, which has been involved in multidrug resistance (MDR) cancer. Its diverse range substrates includes many antineoplastic agents such as doxorubicin and mitoxantrone. ABCG2 expression significantly increased some solid tumors hematologic malignancies, correlated to poorer clinical outcomes. In addition, distinguishing feature cancer stem cells, whereby this membranous...

Abstract Paclitaxel displays clinical activity against a wide variety of solid tumors. However, resistance to paclitaxel significantly attenuates the response chemotherapy. The ABC transporter subfamily C member 10 (ABCC10), also known as multi-drug protein 7 (MRP7) efflux transporter, is major mediator resistance. In this study, we show that masitinib, small molecule stem-cell growth factor receptor (c-Kit) tyrosine kinase inhibitor, at non-toxic concentrations, in HEK293 cells transfected...

Abstract An infusion-dialysis based procedure has been developed as an approach to isolate organic nanoparticles from green tea. Tea nanoparticle (TNP) can effectively load doxorubicin (DOX) via electrostatic and hydrophobic interactions. We established ABCB1 overexpressing tumor xenograft mouse model investigate whether TNP deliver DOX into tumors bypass the efflux function of transporter, thereby increasing intratumoral accumulation potentiating anticancer activity DOX. MTT assays...

Abstract Cancer cells often exhibit either intrinsic or acquired resistance to chemotherapy through a phenomenon known as multidrug (MDR). Different mechanisms contribute the development of MDR, preeminent among them being accelerated drug efflux mediated by overexpression ATP-binding cassette (ABC) transporters. Currently, it has been found that some small molecule tyrosine kinase inhibitors (TKIs), such motesanib, linsitinib, masitinib and nilotinib, were able modulate activity ABC Thus,...

Abstract Abstract: Despite the current advances in cancer drug discovery, cells often develop resistance to chemotherapeutic agents leading poor clinical outcomes. The phenomenon of multidrug (MDR) is prevalent among tumor populations; wherein are rendered resistant structurally and mechanistically unrelated drugs. Of several factors responsible for development MDR, overexpression ATP-binding cassette (ABC) efflux transporters poses a serious threat towards attaining successful outcome....

Abstract Quizartinib (AC220), a novel and potent class II receptor tyrosine kinase inhibitor that has better therapeutic pharmacokinetic profile amongst its class. is currently under clinical trials for FLT3 ITD wild-type AML tested in combination with chemotherapy. This study examined the effects of quizartinib on ABC transporter-mediated multidrug resistance (MDR). Cytotoxic studies showed 0.75, 1.5, 3 μM are three less toxic concentrations normal as well cancer cells. Out these...

Abstract Multidrug resistance (MDR) through overexpression of ATP-binding cassette (ABC) transporters has long evaded chemotherapy in cancer patients. Specific tyrosine kinase inhibitors (TKIs) were recently reported to modulate these ABC transporters, leading an increase the intracellular concentration their substrate drugs. Here, we report for first time, PD173074 inhibitor fibroblast growth factor receptor (FGFR), selectively inhibit subfamily B member 1 (ABCB1/P-glycoprotein)...