Luc Brunsveld

TL;DR: Insertion of 3 to 4 mutations, based on in silico modelling, in a diverse set of natural miniproteins generates potent androgen receptor binders and a clear insight into the structure-activity relationship of such coactivator mimics concerning helix length is revealed.

TL;DR: The data provide a rationale for the design of RXR ligands consisting of a highly conserved hydrophilic region, strongly contributing to the ligand affinity, and a variable hydrophobic region, which efficiently probes the effects of structural changes at the level of the ligands on co-regulator recruitment or the RXRα–NURR1 dimerization interface.

TL;DR: It is demonstrated that critical residues in the putative isoprenoid pocket of PDEδ can be mapped by coupling with a semisynthetic N‐Ras lipoprotein in which the native farnesyl group of the processed protein was replaced by a photoactivatable geranyl benzophenone moiety.

TL;DR: In this paper, the authors present protocols for the synthesis of a fluorescent analogue of geranylgeranyl pyrophosphate NBD-FPP, which can be used to design a high-throughput fluorometric assay of Rab prenylation.

TL;DR: In this paper, a trimesic amide derivative with peripheral oligo(ethylene oxide) side chains (compound 1) shows discotic mesomorphism in a broad temperature range due to stacking of the extended core.