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The MNK–eIF4E Signaling Axis Contributes to Injury-Induced Nociceptive Plasticity and the Development of Chronic Pain
It is found that cold hypersensitivity induced by peripheral nerve injury is reduced in eIF4ES209A and Mnk1/2−/− mice and following cercosporamide treatment, and a new mechanistic target for the development of a chronic pain state is revealed.
Noninvasive continuous monitoring of solid-phase peptide synthesis by acid-base indicator.
Utilisation du bleu de bromophenol pour suivre l'acylation de groupes amino en synthese peptidique en phase solide
Synthesis and evaluation of bivalent NDP-alpha-MSH(7) peptide ligands for binding to the human melanocortin receptor 4 (hMC4R).
This manuscript details the synthesis and evaluation of a series of bivalent ligands containing two copies of the truncated heptapeptide version of [Nle4-D-Phe7]-alpha-melanocyte stimulating hormone (NDP-alpha-MSH), referred to as MSH(7), and suggests these ligands may be capable of cross-linking adjacent receptors.
Enhanced targeting with heterobivalent ligands
Results indicate that synthetic heterobivalent ligands can noncovalently crosslink two unrelated cell surface receptors, making feasible the targeting of receptor combinations identified in human cancers.
Enzyme-mediated spatial segregation on individual polymeric support beads: application to generation and screening of encoded combinatorial libraries.
Proteolysis of short N alpha-protected peptide substrates bound to polyoxyethylene-polystyrene beads releases selectively free amino sites in the enzyme-accessible "surface" area, which allows generation of two structures on the same bead.
The novel PAR2 ligand C391 blocks multiple PAR2 signalling pathways in vitro and in vivo
Proteinase‐activated receptor‐2 is a GPCR linked to diverse pathologies, including acute and chronic pain, and several peptide and peptidomimetic agonists, with high potency and efficacy have been developed to probe the functions of PAR2, in vitro and in vivo.
Gold Nanorods Targeted to Delta Opioid Receptor: Plasmon-Resonant Contrast and Photothermal Agents
The molecularly targeted nanorods can be used as an in vitro ligand-binding and cytotoxic treatment assay platform and could potentially be applied in vivo for diagnostic and therapeutic purposes with endoscopic technology.
Backbone Amide Linker (BAL) Strategy for Solid-Phase Synthesis of C-Terminal-Modified and Cyclic Peptides1,2,3
Peptide targets for synthesis are often desired with C-terminal end groups other than the more usual acid and amide functionalities. Relatively few routes exist for synthesis of C-terminal-modified
Heterobivalent ligands crosslink multiple cell-surface receptors: the human melanocortin-4 and delta-opioid receptors.
The synthesis and bioevaluation of heterobivalent ligands (htBVLs) targeted to two heterologous cell-surface receptors are detailed.