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MDR is characterized by cross\u2010resistance of cells against chemotherapeutic agents, which are used for treatment of e.g., cancer, bacterial infections, or human immunodeficiency virus (HIV) infections. One group of proteins that combines all three stated aspects\u2014the metabolism and distribution of drugs as well as their own regulation\u2014is adenosine triphosphate\u2010binding cassette (ABC) transporters. These efflux pumps use the energy of adenosine triphosphate hydrolysis for drug translocation from the membrane and the cytosol to the extracellular space, often with cotransport of a cosubstrate. Multidrug resistance\u2010associated protein 1 (MRP1, ABCC1) had been discovered as one major key player in cancer\u2010related MDR. The xenobiotic substrates include anthracyclines, <jats:italic>vinca<\/jats:italic> alkaloids, podophyllotoxins, as well as glutathione (GSH)\u2010adducts of certain cytostatics. Contrary to other transport proteins involved in cancer\u2010related MDR the activity of MRP1 is related to the GSH content of cells. A modern strategy to overcome MRP1\u2010associated MDR is besides its inhibition the activation of GSH efflux, enforcing cell death due to cellular stress. In addition, it has recently been found that MRP1 contributes to the \u03b2\u2010amyloid protein clearance in Alzheimer's disease (AD). Collectively, transport activation of MRP1 is of therapeutic value, and furthermore helps to elucidate the transport protein function and the mechanisms behind it. This review is meant to summarize the known concepts of MRP1 activation, which might contribute to a further understanding of MRP1 in particular and ABC transporters in general.<\/jats:p>","DOI":"10.1002\/med.21573","type":"journal-article","created":{"date-parts":[[2019,4,3]],"date-time":"2019-04-03T07:58:36Z","timestamp":1554278316000},"page":"2031-2081","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":38,"title":["The A\u2010B\u2010C of small\u2010molecule ABC transport protein modulators: From inhibition to activation\u2014a case study of multidrug resistance\u2010associated protein 1 (ABCC1)"],"prefix":"10.1002","volume":"39","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-5851-5336","authenticated-orcid":false,"given":"Michael","family":"Wiese","sequence":"first","affiliation":[{"name":"Pharmaceutical Institute, Rheinische Friedrich\u2010Wilhelms\u2010University of Bonn  Bonn 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