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- W2097024182 abstract "The plasma-membrane monoamine transporters (MATs), including the serotonin (SERT), norepinephrine (NET) and dopamine (DAT) transporters, serve a pivotal role in limiting monoamine-mediated neurotransmission through the reuptake of their respective monoamine neurotransmitters. The transporters are the main target of clinically used psychostimulants and antidepressants. Despite the availability of several potent and selective MAT substrates and inhibitors the continuing need for therapeutic drugs to treat brain disorders involving aberrant monoamine signaling provides a compelling reason to identify novel ways of targeting and modulating the MATs. Designing novel modulators of MAT function have been limited by the lack of three dimensional structure information of the individual MATs. However, crystal structures of LeuT, a bacterial homolog of MATs, in a substrate-bound occluded, substrate-free outward-open, and an apo inward-open state and also with competitive and non-competitive inhibitors have been determined. In addition, several structures of the Drosophila DAT have also been resolved. Together with computational modeling and experimental data gathered over the past decade, these structures have dramatically advanced our understanding of several aspects of SERT, NET, and DAT transporter function, including some of the molecular determinants of ligand interaction at orthosteric substrate and inhibitor binding pockets. In addition progress has been made in the understanding of how allosteric modulation of MAT function can be achieved. Here we will review all the efforts up to date that has been made through computational approaches employing structural models of MATs to design small molecule modulators to the orthosteric and allosteric sites using virtual screening techniques." @default.
- W2097024182 created "2016-06-24" @default.
- W2097024182 creator A5025640535 @default.
- W2097024182 creator A5032233275 @default.
- W2097024182 date "2015-09-29" @default.
- W2097024182 modified "2023-10-07" @default.
- W2097024182 title "Designing modulators of monoamine transporters using virtual screening techniques" @default.
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- W2097024182 cites W1506737211 @default.
- W2097024182 cites W1531395975 @default.
- W2097024182 cites W1579841613 @default.
- W2097024182 cites W1969206393 @default.
- W2097024182 cites W1970124769 @default.
- W2097024182 cites W1976038420 @default.
- W2097024182 cites W1976129354 @default.
- W2097024182 cites W1982053398 @default.
- W2097024182 cites W1985176332 @default.
- W2097024182 cites W1990273816 @default.
- W2097024182 cites W1995593325 @default.
- W2097024182 cites W1997634673 @default.
- W2097024182 cites W1998573511 @default.
- W2097024182 cites W1999044153 @default.
- W2097024182 cites W2001397838 @default.
- W2097024182 cites W2004289526 @default.
- W2097024182 cites W2005072000 @default.
- W2097024182 cites W2006093410 @default.
- W2097024182 cites W2008235594 @default.
- W2097024182 cites W2008810302 @default.
- W2097024182 cites W2010145411 @default.
- W2097024182 cites W2015924519 @default.
- W2097024182 cites W2019647316 @default.
- W2097024182 cites W2020727025 @default.
- W2097024182 cites W2023867754 @default.
- W2097024182 cites W2032245417 @default.
- W2097024182 cites W2035833733 @default.
- W2097024182 cites W2039051101 @default.
- W2097024182 cites W2042285022 @default.
- W2097024182 cites W2044160244 @default.
- W2097024182 cites W2044811013 @default.
- W2097024182 cites W2046376309 @default.
- W2097024182 cites W2046508842 @default.
- W2097024182 cites W2048581104 @default.
- W2097024182 cites W2048750863 @default.
- W2097024182 cites W2049868296 @default.
- W2097024182 cites W2052116640 @default.
- W2097024182 cites W2052500414 @default.
- W2097024182 cites W2056982651 @default.
- W2097024182 cites W2059039948 @default.
- W2097024182 cites W2063752616 @default.
- W2097024182 cites W2064225780 @default.
- W2097024182 cites W2071328685 @default.
- W2097024182 cites W2072955418 @default.
- W2097024182 cites W2073471016 @default.
- W2097024182 cites W2075058728 @default.
- W2097024182 cites W2077114751 @default.
- W2097024182 cites W2077531668 @default.
- W2097024182 cites W2080766585 @default.
- W2097024182 cites W2084290194 @default.
- W2097024182 cites W2088514972 @default.
- W2097024182 cites W2089524170 @default.
- W2097024182 cites W2096242757 @default.
- W2097024182 cites W2097788470 @default.
- W2097024182 cites W2104622728 @default.
- W2097024182 cites W2109410476 @default.
- W2097024182 cites W2115620372 @default.
- W2097024182 cites W2120253418 @default.
- W2097024182 cites W2123889306 @default.
- W2097024182 cites W2123898606 @default.
- W2097024182 cites W2129495111 @default.
- W2097024182 cites W2147316618 @default.
- W2097024182 cites W2155495499 @default.
- W2097024182 cites W2161966055 @default.
- W2097024182 cites W2163694515 @default.
- W2097024182 cites W2171043072 @default.
- W2097024182 cites W2171437346 @default.
- W2097024182 cites W2330804585 @default.
- W2097024182 cites W2398613027 @default.
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- W2097024182 doi "https://doi.org/10.3389/fphar.2015.00223" @default.
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