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The human\n                    <jats:italic>ABCG2<\/jats:italic>\n                    gene harbors a high number of polymorphisms and mutations, which may significantly modulate its expression and function. Recent high\u2010resolution structural data, complemented with molecular dynamic simulations, may significantly help to understand intramolecular movements and substrate handling, as well as the effects of mutations on the membrane transporter function of ABCG2. As reviewed here, structural alterations may result not only in direct alterations in drug binding and transporter activity, but also in improper folding or problems in the carefully regulated process of trafficking, including vesicular transport, endocytosis, recycling, and degradation. Here, we also review the clinical importance of altered ABCG2 expression and function in general drug metabolism, cancer multidrug resistance, and impaired uric acid excretion, leading to gout.\n                  <\/jats:p>","DOI":"10.1002\/1873-3468.13947","type":"journal-article","created":{"date-parts":[[2020,10,5]],"date-time":"2020-10-05T01:18:59Z","timestamp":1601860739000},"page":"4012-4034","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":64,"title":["The ABCG2\/BCRP transporter and its variants \u2013 from structure to pathology"],"prefix":"10.1002","volume":"594","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-0592-4539","authenticated-orcid":false,"given":"Bal\u00e1zs","family":"Sarkadi","sequence":"first","affiliation":[{"name":"Institute of Enzymology Research Centre for Natural Sciences Budapest Hungary"},{"name":"Department of Biophysics and Radiation Biology Semmelweis University Budapest 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