Paul Bamborough

TL;DR: The use of thienopyridone compounds of formula (I) or a salt thereof in the treatment of diseases or conditions for which a bromodomain inhibitor is indicated is discussed in this paper.

TL;DR: An orthogonal conformational restriction strategy of the piperidine ring is described to give potent and selective tropane inhibitors and structural insights are shown into why this was more challenging than expected.

TL;DR: In this article, the authors discuss the published data and recent developments in the research area of bromodomains in parasitic protozoa and further work is needed to evaluate the tractability of this target class in the context of infectious diseases and launch drug discovery campaigns to identify and develop antiparasite drugs that can offer differentiated mechanisms of action.

TL;DR: The development and application of atypical acetyl-lysine (KAc) methyl mimetics to take advantage of the differential stability of conserved water molecules in the bromodomain binding side are reported.

TL;DR: The discovery and hit-to-lead exploration of a novel series of selective IKK-β kinase inhibitors led to potent inhibitors, such as 12, which demonstrate efficacy in cellular assays and possess encouraging developability profiles.