@article{
 title = {Synthesis and biological investigation of (+)-JD1, an organometallic BET bromodomain inhibitor},
 type = {article},
 year = {2019},
 month = {12},
 publisher = {American Chemical Society},
 id = {4e441339-de60-3755-a52e-8f72a5f0ac6a},
 created = {2020-01-26T16:10:50.720Z},
 file_attached = {false},
 profile_id = {64f7fb50-d000-335d-a02d-06c5f340a97a},
 last_modified = {2020-01-26T16:10:50.720Z},
 read = {false},
 starred = {false},
 authored = {true},
 confirmed = {true},
 hidden = {false},
 citation_key = {hassellhart2019synthesisinhibitor},
 source_type = {article},
 notes = {© 2019 American Chemical Society.},
 private_publication = {false},
 abstract = {(+)-JD1, a rationally designed ferrocene analogue of the BET bromodomain (BRD) probe molecule (+)-JQ1, has been synthesized and evaluated in biophysical, cell-based assays as well as in pharmacokinetic studies. It displays nanomolar activity against BRD isoforms, and its cocrystal structure was determined in complex with the first bromodomain of BRD4 and compared with that of (+)-JQ1, a known BRD4 small-molecule probe. At 1 μM concentration, (+)-JD1 was able to inhibit c-Myc, a key driver in cancer and an indirect target of BRD4.},
 bibtype = {article},
 author = {Hassell-Hart, S and Runcie, A and Krojer, T and Doyle, J and Lineham, E and Ocasio, C A and Neto, B A D and Fedorov, O and Marsh, G and Maple, H and Felix, R and Ciulli, A and Banks, R and Picaud, S and Filippakopoulos, P and von Delft, F and Brennan, P and Stewart, H J S and Chevassut, T J and Walker, M and Austin, C and Morley, S and Spencer, J},
 doi = {10.1021/acs.organomet.9b00750},
 journal = {Organometallics}
}

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