{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,23]],"date-time":"2026-04-23T05:04:53Z","timestamp":1776920693330,"version":"3.51.2"},"reference-count":0,"publisher":"Bentham Science Publishers Ltd.","issue":"42","content-domain":{"domain":["eurekaselect.com"],"crossmark-restriction":true},"short-container-title":["CMC"],"published-print":{"date-parts":[[2019,2,6]]},"abstract":"<jats:sec>\n<jats:title\/>\n<jats:p>Antibiotic resistance is one of the most pressing health issues of our days. It can\narise due to a multiplicity of factors, such as target modification, decrease in the drug uptake,\nchanges in the metabolic pathways and activation of efflux pumps. The overexpression of efflux\npumps is responsible for the extrusion of drugs, making antibiotic therapy fail, as the\nquantity of intracellular antibiotic is not enough to provide the desired therapeutic effect.\n<\/jats:p><\/jats:sec>\n<jats:sec>\n<jats:title\/>\n<jats:p>\nEfflux pumps can be included in five families according to their composition, nature of substrates,\nenergy source, and number of transmembrane spanning regions. The ABC superfamily\nis mainly found in Gram-positive bacteria, use ATP as an energy source, and only a limited\nnumber of ABC pumps confer multidrug resistance (MDR).\n<\/jats:p><\/jats:sec>\n<jats:sec>\n<jats:title\/>\n<jats:p>\nOn the other hand, the MFS family, most present in Gram-positive bacteria, and the RND\nfamily, characteristic of Gram-negative bacteria, are most associated with antibiotic resistance.\nA wide variety of inhibitors have been disclosed for both families, from either natural\nor synthetic sources, or even drugs that are currently in therapy for other diseases.\n<\/jats:p><\/jats:sec>\n<jats:sec>\n<jats:title\/>\n<jats:p>\nThe other two families are the SMR, which are the smallest drug efflux proteins known, and\nthe MATE family, whose pumps can also resort to the sodium gradient as an energy source.\n<\/jats:p><\/jats:sec>\n<jats:sec>\n<jats:title\/>\n<jats:p>\nIn this review, it is intended to present a comprehensive review of the classes of efflux pump\ninhibitors from the various sources, highlighting their structure-activity relationships, which\ncan be useful for medicinal chemists in the pursuit of novel efflux pump inhibitors.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/0929867325666180209142612","type":"journal-article","created":{"date-parts":[[2018,2,9]],"date-time":"2018-02-09T13:32:46Z","timestamp":1518183166000},"page":"6030-6069","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":20,"title":["Medicinal Chemistry Updates on Bacterial Efflux Pump Modulators"],"prefix":"10.2174","volume":"25","author":[{"given":"Fernando","family":"Dur\u00e3es","sequence":"first","affiliation":[{"name":"Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal"}]},{"given":"Madalena","family":"Pinto","sequence":"additional","affiliation":[{"name":"Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal"}]},{"given":"Em\u00edlia","family":"Sousa","sequence":"additional","affiliation":[{"name":"Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal"}]}],"member":"965","container-title":["Current Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/eurekaselect.com\/article\/download\/159679","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/www.eurekaselect.com\/159679\/article","content-type":"text\/html","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/eurekaselect.com\/article\/download\/159679","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2020,12,25]],"date-time":"2020-12-25T09:50:21Z","timestamp":1608889821000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.eurekaselect.com\/159679\/article"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2019,2,6]]},"references-count":0,"journal-issue":{"issue":"42","published-print":{"date-parts":[[2019,2,6]]}},"alternative-id":["LiveAll1"],"URL":"https:\/\/doi.org\/10.2174\/0929867325666180209142612","relation":{},"ISSN":["0929-8673"],"issn-type":[{"value":"0929-8673","type":"print"}],"subject":[],"published":{"date-parts":[[2019,2,6]]},"assertion":[{"value":"Peer Reviewed","order":0,"name":"review_status","label":"Review Status","group":{"name":"peer_review_details","label":"Peer Review Details"}},{"value":"Single blind","order":1,"name":"review_process","label":"Review Process","group":{"name":"peer_review_details","label":"Peer Review Details"}},{"value":"Checked with iThenticate","order":0,"name":"screening_status","label":"Screening Status","group":{"name":"plagiarism_screening","label":"Plagiarism Screening"}},{"value":"2017-10-26","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2017-12-12","order":1,"name":"revised","label":"Revised","group":{"name":"publication_history","label":"Publication History"}},{"value":"2018-01-31","order":2,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2019-02-06","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}