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Journal articles on the topic 'ABCB1 transporters'

Author: Grafiati

Published: 10 September 2021

Last updated: 29 July 2025

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1

van der Kolk, Dorina M., Susan D. P. W. M. Peeters, Gerald de Haan, Leonid Bystrykh, Elisabeth G. E. de Vries, and Edo Vellenga. "Selective Expression of a Number of ABC Transporter Genes in Normal CD34+CD38− Versus CD34+CD38− Cells, with a Reverse Pattern in a Subgroup of AML Patients." Blood 104, no. 11 (2004): 4291. http://dx.doi.org/10.1182/blood.v104.11.4291.4291.

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Abstract Several ABC transporters involved in drug transport have been identified in hematopoietic stem cells, including ABCB1, ABCC1 and ABCG2. The ABC transporters play a role in chemotherapy resistant AML, although the relevant information is mostly obtained from the total AML cell population instead of the leukemic stem cells characterized by the CD34+CD38− phenotype. In this study we investigated which ABC transporters are selectively expressed in normal CD34+CD38− hematopoietic stem cells versus CD34+CD38+ cells, and to what extent lineage-restricted modulation is aberrantly regulated in

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Michaelis, Martin, Florian Rothweiler, Thomas Nerreter, Mohsen Sharifi, Taravat Ghafourian, and Jindrich Cinatl. "Karanjin interferes with ABCB1, ABCC1, and ABCG2." Journal of Pharmacy & Pharmaceutical Sciences 17, no. 1 (2014): 92. http://dx.doi.org/10.18433/j3bw2s.

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PURPOSE: The prominent ATP-binding cassette (ABC) transporters ABCB1, ABCC1, and ABCG2 are involved in substance transport across physiological barriers and therefore in drug absorption, distribution, and elimination. They also mediate multi-drug resistance in cancer cells. Different flavonoids are known to interfere with different ABC transporters. Here, the effect of the furanoflavonol karanjin, a potential drug with antiglycaemic, gastroprotective, antifungal, and antibacterial effects, was investigated on ABCB1, ABCC1, and ABCG2-mediated drug transport in comparison to the flavonoids apige

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Tsyganov, M. M., M. K. Ibragimova, A. M. Pevzner, et al. "Gene expression analysis of ABC transporter family in breast tumors: relationship with chemotherapy effect and disease prognosis." Advances in Molecular Oncology 7, no. 2 (2020): 29–38. http://dx.doi.org/10.17650/2313-805x-2020-7-2-29-38.

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Background. One of the main reasons of the ineffectiveness of chemotherapy is still considered to be the formation of the multidrug resistance phenotype of the tumor due to the expression of energy-dependent proteins of ABC transporters. Our previous studies for some ABC genes have established that the expression of these genes correlates with the effectiveness of neoadjuvant chemotherapy (NAC). Some of the clinical studies indicate that ABC transporters can influence not only the formation of chemoresistance in the tumor, but also the progression, invasion and metastasis of the tumor node. Ob

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Malinowski, Damian, Paweł Grzegółkowski, Katarzyna Piotrowska, Marcin Słojewski, and Marek Droździk. "Membrane Transporters and Carriers in Human Seminal Vesicles." Journal of Clinical Medicine 11, no. 8 (2022): 2213. http://dx.doi.org/10.3390/jcm11082213.

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Seminal vesicles play an important role in the male reproductive system, producing seminal fluid and thus adequate environment for sperm. However, mechanisms underlying secretory functions of the seminal vesicles’ epithelium have not been defined yet. The aim of the present study was to characterize expression and immunolocalization of selected membrane transporters and carriers in the seminal vesicles. The study included biopsy specimens collected from non-affected parts of seminal vesicles from 53 patients of Caucasian origin subjected for prostatectomy. RT-PCR was used to define expression

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Khalaf, Ban Hamid, Ahmed AbdulJabbar Suleiman, and Mohammed A. Suwaid. "In-silico Elucidation of the Role of ABC-Transporter Genes Expression Regulation by OncomiRs (miR-21, miR-15, and miR-let-7) in Drug Efflux and Chemoresistance in Breast Cancer." Mathematical Biology and Bioinformatics 18, no. 1 (2023): 128–44. http://dx.doi.org/10.17537/2023.18.128.

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Breast cancer is the most common and aggressive malignancy in females with a high prevalence rate of 77.9 million worldwide. Chemotherapy and tyrosine kinase inhibitors have been used to treat invasive and malignant tumors; however, invasive tumors have showed resistance to conventional therapies. ABC transporters play a crucial role in breast cancer due to their chemo-resistance and drug efflux abilities. Additionally, chemo-resistant roles of ABC transporters have been reported in several cancers such as cervical cancer, colon cancer, esophageal squamous cell carcinoma, glioma and HCC. The g

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Phon, Brandon Wee Siang, Shalini Sundramurthi Chelliah, Dina El-Rabie Osman, Saatheeyavaane Bhuvanendran, Ammu Kutty Radhakrishnan, and Muhamad Noor Alfarizal Kamarudin. "Revisiting ABC Transporters and Their Clinical Significance in Glioblastoma." Pharmaceuticals 18, no. 1 (2025): 102. https://doi.org/10.3390/ph18010102.

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Background: The multiple drug-resistant phenomenon has long since plagued the effectiveness of various chemotherapies used in the treatment of patients with glioblastoma (GBM), which is still incurable to this day. ATP-binding cassette (ABC) transporters function as drug transporters and have been touted to be the main culprits in developing resistance to xenobiotic drugs in GBM. Methods: This review systematically analyzed the efficacy of ABC transporters against various anticancer drugs from 16 studies identified from five databases (PubMed, Medline, Embase, Scopus, and ScienceDirect). Resul

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Battista, Theo, Annarita Fiorillo, Valerio Chiarini, Ilaria Genovese, Andrea Ilari, and Gianni Colotti. "Roles of Sorcin in Drug Resistance in Cancer: One Protein, Many Mechanisms, for a Novel Potential Anticancer Drug Target." Cancers 12, no. 4 (2020): 887. http://dx.doi.org/10.3390/cancers12040887.

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The development of drug resistance is one of the main causes of failure in anti-cancer treatments. Tumor cells adopt many strategies to counteract the action of chemotherapeutic agents, e.g., enhanced DNA damage repair, inactivation of apoptotic pathways, alteration of drug targets, drug inactivation, and overexpression of ABC (Adenosine triphosphate-binding cassette, or ATP-binding cassette) transporters. These are broad substrate-specificity ATP-dependent efflux pumps able to export toxins or drugs out of cells; for instance, ABCB1 (MDR1, or P-glycoprotein 1), overexpressed in most cancer ce

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Hao, Pengchao, Jian Xia, Jie Liu, et al. "Auxin-transporting ABC transporters are defined by a conserved D/E-P motif regulated by a prolylisomerase." Journal of Biological Chemistry 295, no. 37 (2020): 13094–105. http://dx.doi.org/10.1074/jbc.ra120.014104.

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The plant hormone auxin must be transported throughout plants in a cell-to-cell manner to affect its various physiological functions. ABCB transporters are critical for this polar auxin distribution, but the regulatory mechanisms controlling their function is not fully understood. The auxin transport activity of ABCB1 was suggested to be regulated by a physical interaction with FKBP42/Twisted Dwarf1 (TWD1), a peptidylprolyl cis-trans isomerase (PPIase), but all attempts to demonstrate such a PPIase activity by TWD1 have failed so far. By using a structure-based approach, we identified several

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da Costa, Kelli Monteiro, Leonardo Freire-de-Lima, Leonardo Marques da Fonseca, José Osvaldo Previato, Lucia Mendonça-Previato та Raphael do Carmo Valente. "ABCB1 and ABCC1 Function during TGF-β-Induced Epithelial-Mesenchymal Transition: Relationship between Multidrug Resistance and Tumor Progression". International Journal of Molecular Sciences 24, № 7 (2023): 6046. http://dx.doi.org/10.3390/ijms24076046.

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Multidrug resistance (MDR) and induction of metastasis are some of the puzzles encountered during cancer chemotherapy. The MDR phenotype is associated with overexpression of ABC transporters, involved in drug efflux. Metastasis originates from the epithelial-mesenchymal transition (EMT), in which cells acquire a migratory phenotype, invading new tissues. ABC transporters’ role during EMT is still elusive, though cells undergoing EMT exhibit enhanced ABCB1 expression. We demonstrated increased ABCB1 expression but no change in activity after TGF-β-induced EMT in A549 cells. Moreover, ABCB1 inhi

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Franko, Ondrej, Martina Čižmáriková, Martin Kello, et al. "Acridine-Based Chalcone 1C and ABC Transporters." International Journal of Molecular Sciences 26, no. 9 (2025): 4138. https://doi.org/10.3390/ijms26094138.

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Chalcones, potential anticancer agents, have shown promise in the suppression of multidrug resistance due to the inhibition of drug efflux driven by certain adenosine triphosphate (ATP)-binding cassette (ABC) transporters. The gene and protein expression of chosen ABC transporters (multidrug resistance protein 1, ABCB1; multidrug resistance-associated protein 1, ABCC1; and breast cancer resistance protein, ABCG2) in human colorectal cancer cells (COLO 205 and COLO 320, which overexpress active ABCB1) was mainly studied in this work under the influence of a novel synthetic acridine-based chalco

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Kannan, Pavitra, András Füredi, Sabina Dizdarevic, et al. "In vivo characterization of [18F]AVT-011 as a radiotracer for PET imaging of multidrug resistance." European Journal of Nuclear Medicine and Molecular Imaging 47, no. 8 (2019): 2026–35. http://dx.doi.org/10.1007/s00259-019-04589-w.

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Abstract Purpose Multidrug resistance (MDR) impedes cancer treatment. Two efflux transporters from the ATP-binding cassette (ABC) family, ABCB1 and ABCG2, may contribute to MDR by restricting the entry of therapeutic drugs into tumor cells. Although a higher expression of these transporters has been correlated with an unfavorable response to chemotherapy, transporter expression does not necessarily correlate with function. In this study, we characterized the pharmacological properties of [18F]AVT-011, a new PET radiotracer for imaging transporter-mediated MDR in tumors. Methods AVT-011 was rad

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Tsyganov, Matvey M., Marina K. Ibragimova, Kseniya A. Gaptulbarova, et al. "DNA Copy Number Aberrations and Expression of ABC Transporter Genes in Breast Tumour: Correlation with the Effect of Neoadjuvant Chemotherapy and Prognosis of the Disease." Pharmaceutics 14, no. 5 (2022): 948. http://dx.doi.org/10.3390/pharmaceutics14050948.

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One of the important reasons for the ineffectiveness of chemotherapy in breast cancer (BC) is considered to be the formation of a multidrug resistance phenotype in tumour cells, which is caused by the expression of energy-dependent ABC transporters. The aim of this work was to assess chromosomal aberrations and the level of transcripts of all 49 known ABC transporter genes in breast tumours. Materials and Methods. The study included 129 patients with breast cancer. A microarray study of all tumour samples was carried out on microchips. Results. This study established that the presence of a del

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Nedeljković, Milica, Nasta Tanić, Mirjana Prvanović, Zorka Milovanović, and Nikola Tanić. "Friend or foe: ABCG2, ABCC1 and ABCB1 expression in triple-negative breast cancer." Breast Cancer 28, no. 3 (2021): 727–36. https://doi.org/10.1007/s12282-020-01210-z.

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<strong>Background: </strong>ATP-binding cassette (ABC) transporters are responsible for the efflux of a wide variety of anti-cancer agents and have been implicated in the chemoresistance of various solid tumors. Chemoresistance is a major cause of therapeutic failure, especially in the highly aggressive triple-negative breast cancer (TNBC) in which, unlike estrogen receptor-expressing (ER+) BC, both endocrine and targeted treatments are ineffectual. We aimed to investigate the level and frequency of expression of the three most important ABC transporter, ABCG2, ABCC1, and ABCB1, accordin

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Kropf, Christian, Karl Fent, Stephan Fischer, Ayako Casanova, and Helmut Segner. "ABC transporters in gills of rainbow trout (Oncorhynchus mykiss)." Journal of Experimental Biology 223, no. 15 (2020): jeb221069. http://dx.doi.org/10.1242/jeb.221069.

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ABSTRACTFish gills are a structurally and functionally complex organ at the interface between the organism and the aquatic environment. Gill functions include the transfer of organic molecules, both natural ones and xenobiotic compounds. Whether the branchial exchange of organic molecules involves active transporters is currently not known. Here, we investigated the presence, diversity and functional activity of ATP-binding cassette (ABC) transporters in gills of juvenile rainbow trout. By means of RT-qPCR, gene transcripts of members from the abcb, abcc and abcg subfamilies were identified. C

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Abbasifarid, Elnaz, Sayed Mahmoud Sajjadi-Jazi, Maryam Beheshtian, Hilda Samimi, Bagher Larijani, and Vahid Haghpanah. "The Role of ATP-Binding Cassette Transporters in the Chemoresistance of Anaplastic Thyroid Cancer: A Systematic Review." Endocrinology 160, no. 8 (2019): 2015–23. http://dx.doi.org/10.1210/en.2019-00241.

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AbstractAnaplastic thyroid cancer (ATC) is an aggressive type of thyroid cancer with a high mortality rate. Cytotoxic drugs are among the treatment modalities usually used for ATC treatment. However, systemic chemotherapies for ATC have not been shown to have remarkable efficacy. ATP-binding cassette (ABC) transporters have been suggested as a possible mechanism in ATC resistance to chemotherapy. This systematic review was aimed to define the possible roles of ABC transporters in ATC resistance to chemotherapy. Numerous databases, including Scopus, Web of Science, PubMed, Cochrane Library, Ovi

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Gu, Song, Shao-Wen Xiao, Jian-Wei Zheng, Hong-Ye Li, Jie-Sheng Liu, and Wei-Dong Yang. "ABC Transporters in Prorocentrum lima and Their Expression Under Different Environmental Conditions Including Okadaic Acid Production." Marine Drugs 17, no. 5 (2019): 259. http://dx.doi.org/10.3390/md17050259.

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Prorocentrum lima is a typical benthic toxic dinoflagellate, which can produce phycotoxins such as okadaic acid (OA). In this study, we identified three ABC transporter genes (ABCB1, ABCC1 and ABCG2) and characterized their expression patterns, as well as OA production under different environmental conditions in P. lima. We found that the three ABC transporters all showed high identity with related ABC proteins from other species, and contained classical features of ABC transport proteins. Among them, ABCG2 was a half size transporter. The three ABC transporter genes displayed various expressi

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Ben Saad, Amel, Alix Bruneau, Elodie Mareux, et al. "Molecular Regulation of Canalicular ABC Transporters." International Journal of Molecular Sciences 22, no. 4 (2021): 2113. http://dx.doi.org/10.3390/ijms22042113.

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The ATP-binding cassette (ABC) transporters expressed at the canalicular membrane of hepatocytes mediate the secretion of several compounds into the bile canaliculi and therefore play a key role in bile secretion. Among these transporters, ABCB11 secretes bile acids, ABCB4 translocates phosphatidylcholine and ABCG5/G8 is responsible for cholesterol secretion, while ABCB1 and ABCC2 transport a variety of drugs and other compounds. The dysfunction of these transporters leads to severe, rare, evolutionary biliary diseases. The development of new therapies for patients with these diseases requires

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Abraham, Ajay, Savitha Varatharajan, Sreeja Karathedath, et al. "ABC Transporter Expression in Acute Myeloid Leukemia: Association with in Vitro Cytotoxicity and Prognostic Markers." Blood 120, no. 21 (2012): 1438. http://dx.doi.org/10.1182/blood.v120.21.1438.1438.

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Abstract Abstract 1438 Combination chemotherapy in Acute Myeloid Leukemia (AML) can cure approximately 25% of patients but the majority is still non-responsive. Drug resistance and relapse are considered to be the major reasons for treatment failure. Though overexpression of ATP-Binding-Cassette (ABC) transporters including ABCB1 and ABCG2 have been shown associated with lower remission rates and survival in AML, the role of majority of ABC transporter genes are still unknown. Present study aims to determine the role of candidate ABC transporter RNA expression (that are shown to directly or in

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Vahdati, Sahel, and Alf Lamprecht. "Membrane-Fusing Vehicles for Re-Sensitizing Transporter-Mediated Multiple-Drug Resistance in Cancer." Pharmaceutics 16, no. 4 (2024): 493. http://dx.doi.org/10.3390/pharmaceutics16040493.

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Reversing the multiple drug resistance (MDR) arising from the overexpression of the efflux transporters often fails mainly due to the high toxicity or the poor water solubility of the inhibitors of these transporters. Here, we demonstrate the delivery of an inhibitor targeting three ABC transporters (ABCB1, ABCC1 and ABCG2) directly to the cell membrane using membrane-fusing vehicles (MFVs). Three different transfected MDCK II cell lines, along with parental cells, were used to investigate the inhibitory effect of cyclosporine A (CsA) in solution versus direct delivery to the cell membrane. Cs

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Zhang, Wandong, Qing Yan Liu, Arsalan S. Haqqani, et al. "Differential Expression of ABC Transporter Genes in Brain Vessels vs. Peripheral Tissues and Vessels from Human, Mouse and Rat." Pharmaceutics 15, no. 5 (2023): 1563. http://dx.doi.org/10.3390/pharmaceutics15051563.

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Background: ATP-binding cassette (ABC) transporters comprise a superfamily of genes encoding membrane proteins with nucleotide-binding domains (NBD). These transporters, including drug efflux across the blood–brain barrier (BBB), carry a variety of substrates through plasma membranes against substrate gradients, fueled by hydrolyzing ATP. The expression patterns/enrichment of ABC transporter genes in brain microvessels compared to peripheral vessels and tissues are largely uncharacterized. Methods: In this study, the expression patterns of ABC transporter genes in brain microvessels, periphera

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Pang, Li, Beverly Word, Joshua Xu, et al. "ATP-Binding Cassette Genes Genotype and Expression: A Potential Association with Pancreatic Cancer Development and Chemoresistance?" Gastroenterology Research and Practice 2014 (2014): 1–9. http://dx.doi.org/10.1155/2014/414931.

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Genetic polymorphisms in ABC (ATP-binding cassette) transporter genes are associated with differential responses to chemotherapy in various cancers including pancreatic cancer. In this study, four SNPs in the ABCB1, ABCC1, and ABCG2 genes were investigated in normal and pancreatic cancerous specimens. The expression of the three transporters was also analyzed. The TT genotypes of G2677T and C3435T in ABCB1 gene were associated with lower risk of developing pancreatic cancer (P=0.013, OR = 0.35 andP=0.015, OR = 0.29, resp.). To our knowledge, this is the first report of the common polymorphisms

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Romão, Carolina Martinez, Felipe de Lara Janz, Jorge Luis Maria Ruiz, et al. "Expression of ABCB1, ABCC1, and LRP in Mesenchymal Stem Cells from Human Amniotic Fluid and Bone Marrow in Culture—Effects of In Vitro Osteogenic and Adipogenic Differentiation." International Journal of Molecular Sciences 26, no. 2 (2025): 510. https://doi.org/10.3390/ijms26020510.

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Mesenchymal stem cells (MSCs) are multipotent cells with the potential to differentiate into various lineages. They have also the potential to protect themselves against harmful stimuli to maintain their functional integrity. Drug resistance-related transporters such as ABCB1 (P-glycoprotein; P-gp), ABCC1 (MRP1; multidrug resistance-related Protein 1), and LRP (lung resistance protein) may protect MSCs against toxic substances such as chemotherapeutic agents. This study evaluated ABCB1, ABCC1, and LRP before and after the differentiation of MSCs derived from human amniotic fluid (AF) and bone

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Teng, Qiu-Xu, Xiaofang Luo, Zi-Ning Lei, et al. "The Multidrug Resistance-Reversing Activity of a Novel Antimicrobial Peptide." Cancers 12, no. 7 (2020): 1963. http://dx.doi.org/10.3390/cancers12071963.

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The overexpression of ATP-binding cassette (ABC) transporters is a common cause of multidrug resistance (MDR) in cancers. The intracellular drug concentration of cancer cells can be decreased relative to their normal cell counterparts due to increased expression of ABC transporters acting as efflux pumps of anticancer drugs. Over the past decades, antimicrobial peptides have been investigated as a new generation of anticancer drugs and some of them were reported to have interactions with ABC transporters. In this article, we investigated several novel antimicrobial peptides to see if they coul

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Tamaki, Akina, Caterina Ierano, Gergely Szakacs, Robert W. Robey, and Susan E. Bates. "The controversial role of ABC transporters in clinical oncology." Essays in Biochemistry 50 (September 7, 2011): 209–32. http://dx.doi.org/10.1042/bse0500209.

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The phenomenon of multidrug resistance in cancer is often associated with the overexpression of the ABC (ATP-binding cassette) transporters Pgp (P-glycoprotein) (ABCB1), MRP1 (multidrug resistance-associated protein 1) (ABCC1) and ABCG2 [BCRP (breast cancer resistance protein)]. Since the discovery of Pgp over 35 years ago, studies have convincingly linked ABC transporter expression to poor outcome in several cancer types, leading to the development of transporter inhibitors. Three generations of inhibitors later, we are still no closer to validating the ‘Pgp hypothesis’, the idea that increas

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Mlejnek, Petr, Petr Dolezel, and Eliska Ruzickova. "Drug resistance of cancer cells is crucially affected by expression levels of ABC-transporters." BioDiscovery 20 (February 8, 2017): e11211. https://doi.org/10.3897/biodiscovery.20.e11211.

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Dasatinib (DAS), a second generation of tyrosine kinase inhibitor (TKI), represents excellent choice for the treatment of chronic myeloid leukemia resistant to imatinib. Unfortunately, recent laboratory studies suggested that antiproliferative effect of DAS might be significantly reduced due to the overexpression of the ATP-binding cassette (ABC) transporters, ABCB1 and ABCG2. However, whether these drug transporters might compromise therapeutic effect of DAS in clinic is unclear. We believe that the drug transporter expression level is a crucial factor that affects the results and thus may he

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Choudhuri, Supratim, and Curtis D. Klaassen. "Structure, Function, Expression, Genomic Organization, and Single Nucleotide Polymorphisms of Human ABCB1 (MDR1), ABCC (MRP), and ABCG2 (BCRP) Efflux Transporters." International Journal of Toxicology 25, no. 4 (2006): 231–59. http://dx.doi.org/10.1080/10915810600746023.

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The ATP-binding cassette (ABC) transporters constitute a large family of membrane proteins, which transport a variety of compounds through the membrane against a concentration gradient at the cost of ATP hydrolysis. Substrates of the ABC transporters include lipids, bile acids, xenobiotics, and peptides for antigen presentation. As they transport exogenous and endogenous compounds, they reduce the body load of potentially harmful substances. One by-product of such protective function is that they also eliminate various useful drugs from the body, causing drug resistance. This review is a brief

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Stockner, Thomas, Anna Mullen, and Fraser MacMillan. "Investigating the dynamic nature of the ABC transporters: ABCB1 and MsbA as examples for the potential synergies of MD theory and EPR applications." Biochemical Society Transactions 43, no. 5 (2015): 1023–32. http://dx.doi.org/10.1042/bst20150138.

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ABC transporters are primary active transporters found in all kingdoms of life. Human multidrug resistance transporter ABCB1, or P-glycoprotein, has an extremely broad substrate spectrum and confers resistance against chemotherapy drug treatment in cancer cells. The bacterial ABC transporter MsbA is a lipid A flippase and a homolog to the human ABCB1 transporter, with which it partially shares its substrate spectrum. Crystal structures of MsbA and ABCB1 have been solved in multiple conformations, providing a glimpse into the possible conformational changes the transporter could be going throug

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do Imperio, Guinever Eustaquio, Enrrico Bloise, Mohsen Javam, et al. "Chorioamnionitis Induces a Specific Signature of Placental ABC Transporters Associated with an Increase of miR-331-5p in the Human Preterm Placenta." Cellular Physiology and Biochemistry 45, no. 2 (2018): 591–604. http://dx.doi.org/10.1159/000487100.

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Background/Aims: The ATP-binding cassette (ABC) transporters mediate drug biodisposition and immunological responses in the placental barrier. In vitro infective challenges alter expression of specific placental ABC transporters. We hypothesized that chorioamnionitis induces a distinct pattern of ABC transporter expression. Methods: Gene expression of 50 ABC transporters was assessed using TaqMan® Human ABC Transporter Array, in preterm human placentas without (PTD; n=6) or with histological chorioamnionitis (PTDC; n=6). Validation was performed using qPCR, immunohistochemistry and Western blo

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Kok, Jan Willem, Karin Klappe, and Ina Hummel. "The Role of the Actin Cytoskeleton and Lipid Rafts in the Localization and Function of the ABCC1 Transporter." Advances in Biology 2014 (May 5, 2014): 1–11. http://dx.doi.org/10.1155/2014/105898.

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ATP-binding cassette (ABC) transporters are known to be important factors in multidrug resistance of tumor cells. Lipid rafts have been implicated in their localization in the plasma membrane, where they function as drug efflux pumps. This specific localization in rafts may support the activity of ABC/Abc transporters. This raises questions regarding the nature and composition of the lipid rafts that harbor ABC/Abc transporters and the dependence of ABC/Abc transporters—concerning their localization and activity—on lipid raft constituents. Here we review our work of the past 10 years aimed at

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Zhang, Yun, Katherine M. Weh, Bridget A. Tripp, et al. "Cranberry Proanthocyanidins Mitigate Reflux-Induced Transporter Dysregulation in an Esophageal Adenocarcinoma Model." Pharmaceuticals 16, no. 12 (2023): 1697. http://dx.doi.org/10.3390/ph16121697.

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We recently reported that cranberry proanthocyanidins (C-PACs) inhibit esophageal adenocarcinoma (EAC) by 83% through reversing reflux-induced bacterial, inflammatory and immune-implicated proteins and genes as well as reducing esophageal bile acids, which drive EAC progression. This study investigated whether C-PACs’ mitigation of bile reflux-induced transporter dysregulation mechanistically contributes to EAC prevention. RNA was isolated from water-, C-PAC- and reflux-exposed rat esophagi with and without C-PAC treatment. Differential gene expression was determined by means of RNA sequencing

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Megías, Juan Eduardo, Pau Montesinos, María José Herrero, et al. "Impact of Transporter Genes Polymorphisms in Standard Induction of Acute Myeloid Leukemia." Blood 126, no. 23 (2015): 4842. http://dx.doi.org/10.1182/blood.v126.23.4842.4842.

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Abstract Background: The intake of anthracyclines in blast cells could be affected by several transporters, including influx transporters (SLC22A16 and SLCO1B1) and efflux pumps of ABC family. Previous studies suggested that single nucleotide polymorphisms (SNPs) of genes coding for anthracyclines transporters may influence their effectiveness or toxicity, although their impact in acute myeloid leukemia (AML) induction therapy remains undetermined Methods: SNPs of anthracycline transporter genes (ABCB1: rs1128503, rs1045642, rs2032582 and haplotype; ABCC1: rs4148350; ABCC2: rs8187710; ABCG2: r

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Shen, Bin, Dawei Li, Pin Dong, and Shang Gao. "Expression of ABC Transporters is an Unfavorable Prognostic Factor in Laryngeal Squamous Cell Carcinoma." Annals of Otology, Rhinology & Laryngology 120, no. 12 (2011): 820–27. http://dx.doi.org/10.1177/000348941112001208.

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Objectives: Two prominent and well-characterized representatives of adenosine triphosphate–binding cassette (ABC) transporter — Breast cancer resistance protein (BCRP or ABCG2) and P-glycoprotein (P-gp or ABCB1) — Are known to be membrane transporters associated with multidrug resistance. The aim of this study was to explore the correlation between ABC transporter expression and the clinicopathologic characteristics, proliferative index, and apoptotic index and their prognostic value in laryngeal squamous cell carcinoma (LSCC). Methods: Paraffin sections of 98 human LSCC specimens were investi

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Li, Wenlong, Rolf W. Sparidans, Maria C. Lebre, Jos H. Beijnen, and Alfred H. Schinkel. "ABCB1 and ABCG2 Control Brain Accumulation and Intestinal Disposition of the Novel ROS1/TRK/ALK Inhibitor Repotrectinib, While OATP1A/1B, ABCG2, and CYP3A Limit Its Oral Availability." Pharmaceutics 13, no. 11 (2021): 1761. http://dx.doi.org/10.3390/pharmaceutics13111761.

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Repotrectinib shows high activity against ROS1/TRK/ALK fusion-positive cancers in preclinical studies. We explored the roles of multidrug efflux transporters ABCB1 and ABCG2, the OATP1A/1B uptake transporter(s), and the CYP3A complex in pharmacokinetics and tissue distribution of repotrectinib in genetically modified mouse models. In vitro, human ABCB1 and ABCG2, and mouse Abcg2 efficiently transported repotrectinib with efflux transport ratios of 13.5, 5.6, and 40, respectively. Oral repotrectinib (10 mg/kg) showed higher plasma exposures in Abcg2-deficient mouse strains. Brain-to-plasma rati

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Williamson, Beth, Kelly E. Dooley, Yuan Zhang, David J. Back, and Andrew Owen. "Induction of Influx and Efflux Transporters and Cytochrome P450 3A4 in Primary Human Hepatocytes by Rifampin, Rifabutin, and Rifapentine." Antimicrobial Agents and Chemotherapy 57, no. 12 (2013): 6366–69. http://dx.doi.org/10.1128/aac.01124-13.

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ABSTRACTRifampin is a potent inducer of cytochrome P450 (CYP) enzymes and transporters. Drug-drug interactions during tuberculosis treatment are common. Induction by rifapentine and rifabutin is understudied. Rifampin and rifabutin significantly inducedCYP3A4(80-fold and 20-fold, respectively) in primary human hepatocytes. The induction was concentration dependent. Rifapentine induced CYP3A4 in hepatocytes from 3 of 6 donors. Data were also generated for ABCB1, ABCC1, ABCC2, organic anion-transporting polypeptide 1B1 (OATP1B1), and OATP1B3. This work serves as a basis for further study of the

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Jha, Niraj Kumar, Rohan Kar, and Rituraj Niranjan. "ABC Transporters in Neurological Disorders: An Important Gateway for Botanical Compounds Mediated Neuro-Therapeutics." Current Topics in Medicinal Chemistry 19, no. 10 (2019): 795–811. http://dx.doi.org/10.2174/1568026619666190412121811.

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Neurodegeneration is a distinguishing feature of many age related disorders and other vector borne neuroinflammatory diseases. There are a number of factors that can modulate the pathology of these disorders. ATP-binding cassette (ABC) transporters are primarily involved in the maintenance of normal brain homeostasis by eliminating toxic peptides and compounds from the brain. Also, ABC transporters protect the brain from the unwanted effects of endogenous and exogenous toxins that can enter the brain parenchyma. Therefore, these transporters have the ability to determine the pathological outco

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Porro, Antonio, Simona Soverini, Daniel Diolaiti, et al. "Direct and Coordinate Regulation of Multidrug Resistance Genes by the c-Myc Oncoprotein." Blood 108, no. 11 (2006): 2594. http://dx.doi.org/10.1182/blood.v108.11.2594.2594.

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Abstract The deregulation of ATP-binding cassette (ABC) transporters responsible for the efflux of anticancer agents may be achieved either by mutations or single nucleotide polymorphisms (SNPs) affecting the biophysical and biochemical properties of the transporters or by an increase in their expression level. Consequently, chemoresistance will develop. In this study we have investigated regulatory mechanisms involved in the activation of ABC transporters. We have first examined how ABC genes are regulated at the transcriptional level and which transcription factors concur to such a control.

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Mandić, Danijela, Lana Nežić, Ljiljana Amdžić, et al. "Overexpression of MRP1/ABCC1, Survivin and BCRP/ABCC2 Predicts the Resistance of Diffuse Large B-Cell Lymphoma to R-CHOP Treatment." Cancers 15, no. 16 (2023): 4106. http://dx.doi.org/10.3390/cancers15164106.

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Background: Approximately 40% of patients with diffuse large B-cell lymphoma (DLBCL) experience treatment resistance to the first-line R-CHOP regimen. ATP binding cassette (ABC) transporters and survivin might play a role in multidrug resistance (MDR) in various tumors. The aim was to investigate if the coexpression of ABC transporters and survivin was associated with R-CHOP treatment response. Methods: The expression of Bcl-2, survivin, P-glycoprotein/ABCB1, MRP1/ABCC1, and BCRP/ABCC2 was analyzed using immunohistochemistry in tumor specimens obtained from patients with DLBCL, and classified

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Dib, Shiraz, Rodrigo Azevedo Loiola, Emmanuel Sevin та ін. "TNFα Activates the Liver X Receptor Signaling Pathway and Promotes Cholesterol Efflux from Human Brain Pericytes Independently of ABCA1". International Journal of Molecular Sciences 24, № 6 (2023): 5992. http://dx.doi.org/10.3390/ijms24065992.

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Neuroinflammation and brain lipid imbalances are observed in Alzheimer’s disease (AD). Tumor necrosis factor-α (TNFα) and the liver X receptor (LXR) signaling pathways are involved in both processes. However, limited information is currently available regarding their relationships in human brain pericytes (HBP) of the neurovascular unit. In cultivated HBP, TNFα activates the LXR pathway and increases the expression of one of its target genes, the transporter ATP-binding cassette family A member 1 (ABCA1), while ABCG1 is not expressed. Apolipoprotein E (APOE) synthesis and release are diminishe

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Wang, Yaogeng, Rolf W. Sparidans, Sander Potters, et al. "P-Glycoprotein (ABCB1/MDR1) and BCRP (ABCG2) Limit Brain Accumulation and Cytochrome P450-3A (CYP3A) Restricts Oral Exposure of the RET Inhibitor Selpercatinib (RETEVMO)." Pharmaceuticals 14, no. 11 (2021): 1087. http://dx.doi.org/10.3390/ph14111087.

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Selpercatinib is a targeted, FDA-approved, oral, small-molecule inhibitor for the treatment of rearranged during transfection (RET) proto-oncogene mutation-positive cancer. Using genetically modified mouse models, we investigated the roles of the multidrug efflux transporters ABCB1 and ABCG2, the OATP1A/1B uptake transporters, and the drug-metabolizing CYP3A complex in selpercatinib pharmacokinetics. Selpercatinib was efficiently transported by hABCB1 and mAbcg2, but not hABCG2, and was not a substrate of human OATP1A2, -1B1 or -1B3 in vitro. In vivo, brain and testis penetration were increase

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Patel, Harsh, Chaoyun Cai, Zhuoxun Wu, Qiuxu Teng, Hanli Li, and Zhe-Sheng Chen. "Abstract 7193: ABCB1-mediated chemotherapeutic drug resistance is reversed by a potent p53-MDM2 inhibitor NVP-HDM201." Cancer Research 84, no. 6_Supplement (2024): 7193. http://dx.doi.org/10.1158/1538-7445.am2024-7193.

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Abstract The failure of chemotherapy in cancer persists as a result of overexpression of various ATP-binding cassette (ABC) transporters. ABCB1 is one such transporter that actively pumps out chemotherapeutic drugs and it is one of the reasons for multidrug resistance (MDR). In the last few years, activation of p53 has been targeted as a therapeutic strategy in the treatment of cancers. Siremadlin (NVP-HDM201) is a potent and selective inhibitor of p53-MDM2 interaction. The objective of this study was to explore the ability of HDM201 to reverse tumor MDR attributable to overexpression of ABC t

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Lentzas, A., M. C. de Gooijer, S. Zuidema, et al. "P10.21.A THE ABCB1/ABCG2 INHIBITOR ELACRIDAR IS A MORE POTENT PHARMACOENHANCER COMPARED TO TARIQUIDAR FOR TREATMENT OF INTRACRANIAL TUMORS WITH SMALL MOLECULE DRUGS." Neuro-Oncology 25, Supplement_2 (2023): ii67. http://dx.doi.org/10.1093/neuonc/noad137.219.

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Abstract BACKGROUND The blood-brain barrier (BBB) is a major hurdle to successful pharmacotherapy of brain tumors. ABCB1 and ABCG2 are efflux transporters that are expressed in brain tumor vessels and reduce the uptake of many small molecule drugs. Elacridar and tariquidar are both dual ABCB1 and ABCG2 inhibitors. We aim to improve pharmacotherapy of brain cancer by concomitant use of potentially effective drugs with elacridar. Since tariquidar has mostly been used to assess the effects of ABC-transporters on brain uptake in human studies with PET tracers, we decided to compare both agents in

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Moss, Darren M., Neill J. Liptrott, Paul Curley, Marco Siccardi, David J. Back, and Andrew Owen. "Rilpivirine Inhibits Drug Transporters ABCB1, SLC22A1, and SLC22A2In Vitro." Antimicrobial Agents and Chemotherapy 57, no. 11 (2013): 5612–18. http://dx.doi.org/10.1128/aac.01421-13.

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ABSTRACTRilpivirine is a nonnucleoside reverse transcriptase inhibitor approved for treatment of HIV-1 infection in antiretroviral-naive adult patients. Potential interactions with drug transporters have not been fully investigated. Transport by and inhibition of drug transporters by rilpivirine were analyzed to further understand the mechanisms governing rilpivirine exposure and determine the potential for transporter-mediated drug-drug interactions. The ability of rilpivirine to inhibit or be transported by ABCB1 was determined using ABCB1-overexpressing CEMVBL100cells and Caco-2 cell monola

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Zhang, Yongchao, Zhuo-Xun Wu, Yuqi Yang, et al. "Poziotinib Inhibits the Efflux Activity of the ABCB1 and ABCG2 Transporters and the Expression of the ABCG2 Transporter Protein in Multidrug Resistant Colon Cancer Cells." Cancers 12, no. 11 (2020): 3249. http://dx.doi.org/10.3390/cancers12113249.

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Colorectal cancer (CRC) is a leading cause of cancer deaths in the United States. Currently, chemotherapy is a first-line treatment for CRC. However, one major drawback of chemotherapy is the emergence of multidrug resistance (MDR). It has been well-established that the overexpression of the ABCB1 and/or ABCG2 transporters can produce MDR in cancer cells. In this study, we report that in vitro, poziotinib can antagonize both ABCB1- and ABCG2-mediated MDR at 0.1–0.6 μM in the human colon cancer cell lines, SW620/Ad300 and S1-M1-80. Mechanistic studies indicated that poziotinib increases the int

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Temesszentandrási-Ambrus, Csilla, Gábor Nagy, Annamária Bui, and Zsuzsanna Gáborik. "A Unique In Vitro Assay to Investigate ABCB4 Transport Function." International Journal of Molecular Sciences 24, no. 5 (2023): 4459. http://dx.doi.org/10.3390/ijms24054459.

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ABCB4 is almost exclusively expressed in the liver, where it plays an essential role in bile formation by transporting phospholipids into the bile. ABCB4 polymorphisms and deficiencies in humans are associated with a wide spectrum of hepatobiliary disorders, attesting to its crucial physiological function. Inhibition of ABCB4 by drugs may lead to cholestasis and drug-induced liver injury (DILI), although compared with other drug transporters, there are only a few identified substrates and inhibitors of ABCB4. Since ABCB4 shares up to 76% identity and 86% similarity in the amino acid sequence w

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Sato, Ryoichi, Satomi Adegawa, Xiaoyi Li, Shiho Tanaka, and Haruka Endo. "Function and Role of ATP-Binding Cassette Transporters as Receptors for 3D-Cry Toxins." Toxins 11, no. 2 (2019): 124. http://dx.doi.org/10.3390/toxins11020124.

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When ABC transporter family C2 (ABCC2) and ABC transporter family B1 (ABCB1) were heterologously expressed in non-susceptible cultured cells, the cells swelled in response to Cry1A and Cry3 toxins, respectively. Consistent with the notion that 3D-Cry toxins form cation-permeable pores, Bombyx mori ABCC2 (BmABCC2) facilitated cation-permeable pore formation by Cry1A when expressed in Xenopus oocytes. Furthermore, BmABCC2 had a high binding affinity (KD) to Cry1Aa of 3.1 × 10−10 M. These findings suggest that ABC transporters, including ABCC2 and ABCB1, are functional receptors for 3D-Cry toxins

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Fan, Wenjie, Kai Shao, and Min Luo. "Structural View of Cryo-Electron Microscopy-Determined ATP-Binding Cassette Transporters in Human Multidrug Resistance." Biomolecules 14, no. 2 (2024): 231. http://dx.doi.org/10.3390/biom14020231.

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ATP-binding cassette (ABC) transporters, acting as cellular “pumps,” facilitate solute translocation through membranes via ATP hydrolysis. Their overexpression is closely tied to multidrug resistance (MDR), a major obstacle in chemotherapy and neurological disorder treatment, hampering drug accumulation and delivery. Extensive research has delved into the intricate interplay between ABC transporter structure, function, and potential inhibition for MDR reversal. Cryo-electron microscopy has been instrumental in unveiling structural details of various MDR-causing ABC transporters, encompassing A

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Moss, Darren M., Wai San Kwan, Neill J. Liptrott, et al. "Raltegravir Is a Substrate for SLC22A6: a Putative Mechanism for the Interaction between Raltegravir and Tenofovir." Antimicrobial Agents and Chemotherapy 55, no. 2 (2010): 879–87. http://dx.doi.org/10.1128/aac.00623-10.

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ABSTRACTThe identification of transporters of the HIV integrase inhibitor raltegravir could be a factor in an understanding of the pharmacokinetic-pharmacodynamic relationship and reported drug interactions of raltegravir. Here we determined whether raltegravir was a substrate for ABCB1 or the influx transporters SLCO1A2, SLCO1B1, SLCO1B3, SLC22A1, SLC22A6, SLC10A1, SLC15A1, and SLC15A2. Raltegravir transport by ABCB1 was studied with CEM, CEMVBL100, and Caco-2 cells. Transport by uptake transporters was assessed by using aXenopus laevisoocyte expression system, peripheral blood mononuclear ce

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Moiseeva, Natalia I., Lidia A. Laletina, Timur I. Fetisov, et al. "Analysis of Multiple Drug Resistance Mechanism in Different Types of Soft Tissue Sarcomas: Assessment of the Expression of ABC-Transporters, MVP, YB-1, and Analysis of Their Correlation with Chemosensitivity of Cancer Cells." International Journal of Molecular Sciences 23, no. 6 (2022): 3183. http://dx.doi.org/10.3390/ijms23063183.

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Chemotherapy of soft tissue sarcomas (STS) is restricted by low chemosensitivity and multiple drug resistance (MDR). The purpose of our study was the analysis of MDR mechanism in different types of STS. We assessed the expression of ABC-transporters, MVP, YB-1, and analyzed their correlation with chemosensitivity of cancer cells. STS specimens were obtained from 70 patients without metastatic disease (2018–2020). Expression level of MDR-associated genes was estimated by qRT-PCR and cytofluorimetry. Mutations in ABC-transporter genes were captured by exome sequencing. Chemosensitivity (SI) of S

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Aryal, Bibek, Christophe Laurent, and Markus Geisler. "Learning from each other: ABC transporter regulation by protein phosphorylation in plant and mammalian systems." Biochemical Society Transactions 43, no. 5 (2015): 966–74. http://dx.doi.org/10.1042/bst20150128.

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The ABC (ATP-binding cassette) transporter family in higher plants is highly expanded compared with those of mammalians. Moreover, some members of the plant ABC subfamily B (ABCB) display very high substrate specificity compared with their mammalian counterparts that are often associated with multi-drug resistance phenomena. In this review, we highlight prominent functions of plant and mammalian ABC transporters and summarize our knowledge on their post-transcriptional regulation with a focus on protein phosphorylation. A deeper comparison of regulatory events of human cystic fibrosis transmem

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Aryal, Bibek, Christophe Laurent, and Markus Geisler. "Correction: Learning from each other: ABC transporter regulation by protein phosphorylation in plant and mammalian systems." Biochemical Society Transactions 44, no. 2 (2016): 663–73. http://dx.doi.org/10.1042/bst20150128_2.

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The ABC (ATP-binding cassette) transporter family in higher plants is highly expanded compared with those of mammalians. Moreover, some members of the plant ABCB subfamily display very high substrate specificity compared with their mammalian counterparts that are often associated with multidrug resistance (MDR) phenomena. In this review we highlight prominent functions of plant and mammalian ABC transporters and summarize our knowledge on their post-transcriptional regulation with a focus on protein phosphorylation. A deeper comparison of regulatory events of human cystic fibrosis transmembran

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