@article{
 title = {Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7},
 type = {article},
 year = {2017},
 keywords = {asymmetric catalysis,epigenetics,inhibitors,lysine demethylases},
 pages = {15555-15559},
 volume = {56},
 websites = {http://doi.wiley.com/10.1002/anie.201706788},
 month = {12},
 day = {4},
 id = {64f096da-2a2f-3e59-8ed1-d1fb205f32af},
 created = {2017-12-06T13:17:45.034Z},
 accessed = {2017-12-06},
 file_attached = {true},
 profile_id = {64f7fb50-d000-335d-a02d-06c5f340a97a},
 last_modified = {2021-03-22T09:24:59.564Z},
 read = {true},
 starred = {true},
 authored = {true},
 confirmed = {true},
 hidden = {false},
 citation_key = {Gerken2017},
 private_publication = {false},
 abstract = {Histone lysine demethylases (KDMs) are of critical importance in the epigenetic regulation of gene expression, yet there are few selective, cell-permeable inhibitors or suitable tool compounds for these enzymes. We describe the discovery of a new class of inhibitor that is highly potent towards the histone lysine demethylases KDM2A/7A. A modular synthetic approach was used to explore the chemical space and accelerate the investigation of key structure-activity relationships, leading to the development of a small molecule with around 75-fold selectivity towards KDM2A/7A versus other KDMs, as well as cellular activity at low micromolar concentrations.},
 bibtype = {article},
 author = {Gerken, Philip A. and Wolstenhulme, Jamie R. and Tumber, Anthony and Hatch, Stephanie B. and Zhang, Yijia and Müller, Susanne and Chandler, Shane A. and Mair, Barbara and Li, Fengling and Nijman, Sebastian M.B. and Konietzny, Rebecca and Szommer, Tamas and Yapp, Clarence and Fedorov, Oleg and Benesch, Justin L.P. and Vedadi, Masoud and Kessler, Benedikt M. and Kawamura, Akane and Brennan, Paul E. and Smith, Martin D.},
 doi = {10.1002/anie.201706788},
 journal = {Angewandte Chemie - International Edition},
 number = {49}
}

{"_id":"WD54osPs2vjkjoWWK","bibbaseid":"gerken-wolstenhulme-tumber-hatch-zhang-mller-chandler-mair-etal-discoveryofahighlyselectivecellactiveinhibitorofthehistonelysinedemethylaseskdm27-2017","downloads":2,"creationDate":"2018-08-31T13:28:42.475Z","title":"Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7","author_short":["Gerken, P., A.","Wolstenhulme, J., R.","Tumber, A.","Hatch, S., B.","Zhang, Y.","Müller, S.","Chandler, S., A.","Mair, B.","Li, F.","Nijman, S., M.","Konietzny, R.","Szommer, T.","Yapp, C.","Fedorov, O.","Benesch, J., L.","Vedadi, M.","Kessler, B., M.","Kawamura, A.","Brennan, P., E.","Smith, M., D."],"year":2017,"bibtype":"article","biburl":"https://bibbase.org/service/mendeley/64f7fb50-d000-335d-a02d-06c5f340a97a","bibdata":{"title":"Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7","type":"article","year":"2017","keywords":"asymmetric catalysis,epigenetics,inhibitors,lysine demethylases","pages":"15555-15559","volume":"56","websites":"http://doi.wiley.com/10.1002/anie.201706788","month":"12","day":"4","id":"64f096da-2a2f-3e59-8ed1-d1fb205f32af","created":"2017-12-06T13:17:45.034Z","accessed":"2017-12-06","file_attached":"true","profile_id":"64f7fb50-d000-335d-a02d-06c5f340a97a","last_modified":"2021-03-22T09:24:59.564Z","read":"true","starred":"true","authored":"true","confirmed":"true","hidden":false,"citation_key":"Gerken2017","private_publication":false,"abstract":"Histone lysine demethylases (KDMs) are of critical importance in the epigenetic regulation of gene expression, yet there are few selective, cell-permeable inhibitors or suitable tool compounds for these enzymes. We describe the discovery of a new class of inhibitor that is highly potent towards the histone lysine demethylases KDM2A/7A. A modular synthetic approach was used to explore the chemical space and accelerate the investigation of key structure-activity relationships, leading to the development of a small molecule with around 75-fold selectivity towards KDM2A/7A versus other KDMs, as well as cellular activity at low micromolar concentrations.","bibtype":"article","author":"Gerken, Philip A. and Wolstenhulme, Jamie R. and Tumber, Anthony and Hatch, Stephanie B. and Zhang, Yijia and Müller, Susanne and Chandler, Shane A. and Mair, Barbara and Li, Fengling and Nijman, Sebastian M.B. and Konietzny, Rebecca and Szommer, Tamas and Yapp, Clarence and Fedorov, Oleg and Benesch, Justin L.P. and Vedadi, Masoud and Kessler, Benedikt M. and Kawamura, Akane and Brennan, Paul E. and Smith, Martin D.","doi":"10.1002/anie.201706788","journal":"Angewandte Chemie - International Edition","number":"49","bibtex":"@article{\n title = {Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7},\n type = {article},\n year = {2017},\n keywords = {asymmetric catalysis,epigenetics,inhibitors,lysine demethylases},\n pages = {15555-15559},\n volume = {56},\n websites = {http://doi.wiley.com/10.1002/anie.201706788},\n month = {12},\n day = {4},\n id = {64f096da-2a2f-3e59-8ed1-d1fb205f32af},\n created = {2017-12-06T13:17:45.034Z},\n accessed = {2017-12-06},\n file_attached = {true},\n profile_id = {64f7fb50-d000-335d-a02d-06c5f340a97a},\n last_modified = {2021-03-22T09:24:59.564Z},\n read = {true},\n starred = {true},\n authored = {true},\n confirmed = {true},\n hidden = {false},\n citation_key = {Gerken2017},\n private_publication = {false},\n abstract = {Histone lysine demethylases (KDMs) are of critical importance in the epigenetic regulation of gene expression, yet there are few selective, cell-permeable inhibitors or suitable tool compounds for these enzymes. We describe the discovery of a new class of inhibitor that is highly potent towards the histone lysine demethylases KDM2A/7A. A modular synthetic approach was used to explore the chemical space and accelerate the investigation of key structure-activity relationships, leading to the development of a small molecule with around 75-fold selectivity towards KDM2A/7A versus other KDMs, as well as cellular activity at low micromolar concentrations.},\n bibtype = {article},\n author = {Gerken, Philip A. and Wolstenhulme, Jamie R. and Tumber, Anthony and Hatch, Stephanie B. and Zhang, Yijia and Müller, Susanne and Chandler, Shane A. and Mair, Barbara and Li, Fengling and Nijman, Sebastian M.B. and Konietzny, Rebecca and Szommer, Tamas and Yapp, Clarence and Fedorov, Oleg and Benesch, Justin L.P. and Vedadi, Masoud and Kessler, Benedikt M. and Kawamura, Akane and Brennan, Paul E. and Smith, Martin D.},\n doi = {10.1002/anie.201706788},\n journal = {Angewandte Chemie - International Edition},\n number = {49}\n}","author_short":["Gerken, P., A.","Wolstenhulme, J., R.","Tumber, A.","Hatch, S., B.","Zhang, Y.","Müller, S.","Chandler, S., A.","Mair, B.","Li, F.","Nijman, S., M.","Konietzny, R.","Szommer, T.","Yapp, C.","Fedorov, O.","Benesch, J., L.","Vedadi, M.","Kessler, B., M.","Kawamura, A.","Brennan, P., E.","Smith, M., D."],"urls":{"Paper":"https://bibbase.org/service/mendeley/64f7fb50-d000-335d-a02d-06c5f340a97a/file/7ac014c1-d247-2443-3ef9-cd772a1b8003/full_text.pdf.pdf","Website":"http://doi.wiley.com/10.1002/anie.201706788"},"biburl":"https://bibbase.org/service/mendeley/64f7fb50-d000-335d-a02d-06c5f340a97a","bibbaseid":"gerken-wolstenhulme-tumber-hatch-zhang-mller-chandler-mair-etal-discoveryofahighlyselectivecellactiveinhibitorofthehistonelysinedemethylaseskdm27-2017","role":"author","keyword":["asymmetric catalysis","epigenetics","inhibitors","lysine demethylases"],"metadata":{"authorlinks":{"brennan, p":"https://www.brennanresearchgroup.com/publications"}},"downloads":2},"search_terms":["discovery","highly","selective","cell","active","inhibitor","histone","lysine","demethylases","kdm2","gerken","wolstenhulme","tumber","hatch","zhang","müller","chandler","mair","li","nijman","konietzny","szommer","yapp","fedorov","benesch","vedadi","kessler","kawamura","brennan","smith"],"keywords":["asymmetric catalysis","epigenetics","inhibitors","lysine demethylases"],"authorIDs":["2PcjuiF3R7eQubzsS","3Wg6Evy8g6dGhA6RP","5b8cf59e29c69a10000000dd","5b8d0d2b29c69a1000000190","5df615c32b34d0de01000067","5e04257fc51eb3de0100004e","5e074383513c7fdf010000b2","5e0d5e8c24d7cbdf0100005a","5e0fad9cf350a2de01000048","5e14621a0467fede01000037","5e161098f67f7dde01000315","5e1c57dee556c6de01000117","5e1e05302cced5de010001fe","5e1edaa3875c69df01000096","5e286db66ae365de0100012e","5e29b862edf563df010000d2","5e30592357a222df01000189","5e31a6726be690de01000130","5e35c99476dd53de0100003e","5e367c8ef0f9c4de01000058","5e37e643e8908edf010000a5","5e3bd1e704fc23e401000022","5e3c19530c5519de010000eb","5e3e45f7018e1dde01000045","5e452d19605639de0100005a","5e45df30ad0603df01000105","5e46b09f8573d1de01000014","5e4c15c92dc400de01000056","5e4c21a52dc400de0100018a","5e4c2a582dc400de01000297","5e4c4ea8271596df01000048","5e4c706ef2c6ddde010000dd","5e4eb86dd9cddadf0100003c","5e4f7b5a42a908de0100000c","5e540863e81566de010000ef","5e55ee11c2c8a2df010000bb","5e5bf6d1d49321e0010000b2","5e5d6754ad47bcde01000154","5e5f76a55766d9df010000b8","5e5fae7919c3fade0100013b","5e6606d7fa8a45de01000074","5vpfcTcw8zWCJD2nF","6FKA7EN4QuMHpmwi6","An3w7fKehnECWntHD","Bu2c3DHDtJvHTYMHq","BznF7qjM756E4jqnf","DfC2nWXrsDiWAGdeK","F99s5PmgDMnmZMCrf","GWEtQQ7DK3eqH6BKs","KoTB5Qe3rxh4268Ks","LTPygeEwWdFJYM3ex","MqNwdFkRBormaL3gc","PhPZA8Ev3s7adKhQp","Sx9chhPN3Rv7ceC2x","TEr37QWFQEKfekGBX","b8tt4q6azbrxnRfyb","cjsLZWYTgsqhBfmh8","cttrvqjxXS3rH8Dse","dkaRruzTHGciJqey5","ewh6B4GHpYJvXWBFu","g4JkphGbeNea298iY","iSo57iyxSkCmqqcdD","n9wv3r7bpGdLhh2Gf","tDAsqmS4FrzLst3z7","x3SHcLfxXH8uRbJbK"],"dataSources":["Pa586au6MYhHM9r97","ya2CyA73rpZseyrZ8","2252seNhipfTmjEBQ"]}