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New Modalities for Challenging Targets in Drug Discovery.
TLDR
This Review defines for the first time the scope of this term, which includes novel peptidic scaffolds, oligonucleotides, hybrids, molecular conjugates, as well as new uses of classical small molecules. Expand
Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
TLDR
A focused solid support-based synthesis protocol was developed, which led to ligands with submicromolar affinity for FKBP51 and FK BP52, and the molecular binding mode for one sulfonamide analogue was confirmed by X-ray crystallography. Expand
Therapeutic Potential of Foldamers: From Chemical Biology Tools To Drug Candidates?
TLDR
The current knowledge of foldamers is reviewed in a drug discovery context and recent advances in the early phases of drug discovery including hit finding, target validation, and optimization and molecular modeling are discussed. Expand
The chemical biology of immunophilin ligands.
TLDR
The immunophilin ligands cyclosporin A, FK506 and rapamycin are best known for their immunosuppressive properties and their clinical use in transplantation medicine, and this review shows the progress on three major areas made in the last five years. Expand
Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
TLDR
The cocrystal structure of FK BP51 with a simplified α-ketoamide analogue derived from FK506 is reported and the first structure-activity relationship analysis for FKBP51 and FKbp52 based on this compound is reported, which found the interaction with FKBPs was found to be surprisingly tolerant to the stereochemistry of the attached cyclohexyl substituents. Expand
Dithiol amino acids can structurally shape and enhance the ligand-binding properties of polypeptides.
TLDR
The development of a dithiol amino acid (Dtaa) that can form two disulfide bridges at a single amino acid site is described that is likely to have broad application in the rational design or directed evolution of peptides and proteins with high activity and stability. Expand
Increasing the efficiency of ligands for FK506-binding protein 51 by conformational control.
TLDR
This work exemplifies how atom-efficient ligands can be achieved by careful conformational control even in very open and thus difficult binding sites such as FKBP51. Expand
Azidobupramine, an Antidepressant-Derived Bifunctional Neurotransmitter Transporter Ligand Allowing Covalent Labeling and Attachment of Fluorophores
The aim of this study was to design, synthesize and validate a multifunctional antidepressant probe that is modified at two distinct positions. The purpose of these modifications was to allowExpand
Late-Stage Functionalization of Histidine in Unprotected Peptides.
TLDR
The exquisite selectivity for histidine functionalization was demonstrated through the alkylation of complex unprotected peptides in aqueous media, and this methodology was extended for the installation of a ketone handle, providing an unprecedented anchor for selective oxime/hydrazone conjugation at histidine. Expand
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