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Analysis of methotrexate and folate transport by multidrug resistance protein 4 (ABCC4): MRP4 is a component of the methotrexate efflux system.
It is shown that MRP4 is active in the transport of MTX as well as the physiological folates folic acid (FA) and N(5)-formyltetrahydrofolic Acid (leucovorin) and that MRp4 represents a common efflux system for both MTX and certain nucleotide analogues.
Characterization of the drug resistance and transport properties of multidrug resistance protein 6 (MRP6, ABCC6).
It is shown that expression of MRP6 is specifically associated with the MgATP-dependent transport of the glutathione S-conjugates leukotriene C(4) and S-(2, 4-dinitrophenyl)glutathione and the cyclopentapeptide BQ123 but not glucuronate conjugates such as 17beta-estradiol 17-(beta-D-glucuronide).
Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport.
The capacity of MRP3 to transport folates indicates that it may reduce intracellular levels of these compounds and thereby indirectly influence antifolate cytotoxicity, and it implies that this pump may play a role in the response to chemotherapeutic regimens in which leucovorin is a component.
Analysis of the structure and expression pattern of MRP7 (ABCC10), a new member of the MRP subfamily.
Transport of amphipathic anions by human multidrug resistance protein 3.
MRP3, like MRP1 and cMOAT, is concluded to be competent in the transport of glutathione S-conjugates, glucuronides, and methotrexate, albeit at low to moderate affinity.
MRP Subfamily Transporters and Resistance to Anticancer Agents
It is hoped that elucidation of the resistance profiles and physiological functions of the different members of the MRP subfamily will provide new insights into the molecular basis of clinical drug resistance and spawn new strategies for combating this phenomenon.
Expression of multidrug resistance protein-3 (multispecific organic anion transporter-D) in human embryonic kidney 293 cells confers resistance to anticancer agents.
Results indicate that MRP3 confers resistance to some anticancer agents but that its resistance pattern is distinct from the resistance patterns of other ABC transporters involved in resistance to natural product chemotherapeutic agents.
Global mapping of CARM1 substrates defines enzyme specificity and substrate recognition
It is demonstrated that the N-terminus of CARM1 is involved in substrate recognition and nearly indispensable for substrate methylation, and proposed that development ofCARM1-specific inhibitors should focus on its N- terminus.
Genome-wide CRISPR screening reveals genetic modifiers of mutant EGFR dependence in human NSCLC
A genome-wide CRISPR-Cas9 screening uncovered a spectrum of previously unidentified regulators of EGFR TKI sensitivity in EGFR-mutant human NSCLC, providing insights into the heterogeneity of EGfr TKI treatment responses.
MED12 methylation by CARM1 sensitizes human breast cancer cells to chemotherapy drugs
This study identified MED12 methylation as a sensor for predicting response to commonly used chemotherapy drugs in human cancers and showed that the methylation-dependent drug response mechanism is distinct from activation of TGF-βR signaling.