Dianne Alewood

TL;DR: In this paper, simple, effective protocols have been developed for manual and machine-assisted Boc-chemistry solid phase peptide synthesis on polystyrene resins, which use in situ neutralization [i.e. neutralization simultaneous with coupling], high concentrations (> 0.2 M) of Bocamino acid-OBt esters plus base for rapid coupling, 100% TFA for rapid Boc group removal, and a single short (30 s) DMF flow wash between deprotection/coupling and between coupling/deprotection.

TL;DR: The in situ neutralization protocols gave a significant increase in the efficiency of chain assembly, especially for “difficult” sequences arising from sequence-dependent peptide chain aggregation in standard (neutralization prior to coupling) Boc-chemistry SPPS protocols or in Fmoc- chemistry SPPS.

TL;DR: Together with modern analytical techniques for peptide analysis such as mass spectrometry (MS) and MS combined with liquid chromatography (LC–MS), it is now feasible to observe and determine the nature of the various side products in solid-phase peptide synthesis (SPPS).

TL;DR: Xen2174 appears to be a promising candidate for development as a novel therapeutic for i.t. administration to patients with persistent neuropathic pain, after confirming the noradrenergic mechanism of action.

TL;DR: A pharmacophore model for the allosteric binding of 3 to NET is proposed and it is shown that 3 interacts with NET predominantly through amino acids in the first loop, forming a tight inverse turn presenting amino acids Tyr7, Lys8, and Leu9 in an orientation allowing for high affinity interaction with NET.