Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain. Chaikuad, A., Lang, S., Brennan, P., E., Temperini, C., Fedorov, O., Hollander, J., Nachane, R., Abell, C., Müller, S., Siegal, G., & Knapp, S. Journal of Medicinal Chemistry, 59(4):1648-1653, American Chemical Society, 1, 2016.
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Paper Website doi abstract bibtex The P300/CBP-associated factor plays a central role in retroviral infection and cancer development, and the C-terminal bromodomain provides an opportunity for selective targeting. Here, we report several new classes of acetyl-lysine mimetic ligands ranging from mM to low micromolar affinity that were identified using fragment screening approaches. The binding modes of the most attractive fragments were determined using high resolution crystal structures providing chemical starting points and structural models for the development of potent and selective PCAF inhibitors.
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title = {Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain},
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abstract = {The P300/CBP-associated factor plays a central role in retroviral infection and cancer development, and the C-terminal bromodomain provides an opportunity for selective targeting. Here, we report several new classes of acetyl-lysine mimetic ligands ranging from mM to low micromolar affinity that were identified using fragment screening approaches. The binding modes of the most attractive fragments were determined using high resolution crystal structures providing chemical starting points and structural models for the development of potent and selective PCAF inhibitors.},
bibtype = {article},
author = {Chaikuad, Apirat and Lang, Steffen and Brennan, Paul E. and Temperini, Claudia and Fedorov, Oleg and Hollander, Johan and Nachane, Ruta and Abell, Chris and Müller, Susanne and Siegal, Gregg and Knapp, Stefan},
doi = {10.1021/acs.jmedchem.5b01719},
journal = {Journal of Medicinal Chemistry},
number = {4}
}Downloads: 0
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