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Medicinal-Pharmaceutical Chemistry Commons

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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Poly(Ethylene Glycol)-Based Backbones With High Peptide Loading Capacities., Aoife O'Connor, Jean-Noel Marsat, Annachiara Mitrugno, Tom Flahive, Niamh Moran, David Brayden, Marc Devocelle Oct 2014

Poly(Ethylene Glycol)-Based Backbones With High Peptide Loading Capacities., Aoife O'Connor, Jean-Noel Marsat, Annachiara Mitrugno, Tom Flahive, Niamh Moran, David Brayden, Marc Devocelle

Chemistry Articles

Polymer-peptide conjugates are a promising class of compounds, where polymers can be used to overcome some of the limitations associated with peptides intended for therapeutic and/or diagnostic applications. Linear polymers such as poly(ethylene glycol) can be conjugated through terminal moieties and have therefore limited loading capacities. In this research, functionalised linear poly(ethylene glycol)s are utilised for peptide conjugation, to increase their potential loading capacities. These poly(ethylene glycol) derivatives are conjugated to peptide sequences containing representative side-chain functionalised amino acids, using different conjugation chemistries, including copper-catalysed azide-alkyne cycloaddition, amide coupling and thiol-ene reactions. Conjugation of a ...


Computational Survey Of Peptides Derived From Disulphide-Bonded Protein Loops That May Serve As Mediators Of Protein-Protein Interactions., Fergal J. Duffy, Marc Devocelle, David R. Croucher, Denis C. Shields Sep 2014

Computational Survey Of Peptides Derived From Disulphide-Bonded Protein Loops That May Serve As Mediators Of Protein-Protein Interactions., Fergal J. Duffy, Marc Devocelle, David R. Croucher, Denis C. Shields

Chemistry Articles

BACKGROUND: Bioactive cyclic peptides derived from natural sources are well studied, particularly those derived from non-ribosomal synthetases in fungi or bacteria. Ribosomally synthesised bioactive disulphide-bonded loops represent a large, naturally enriched library of potential bioactive compounds, worthy of systematic investigation.

RESULTS: We examined the distribution of short cyclic loops on the surface of a large number of proteins, especially membrane or extracellular proteins. Available three-dimensional structures highlighted a number of disulphide-bonded loops responsible for the majority of the likely binding interactions in a variety of protein complexes, due to their location at protein-protein interfaces. We find that disulphide-bonded loops at ...


Bu4n(+) Alkoxide-Initiated/Autocatalytic Addition Reactions With Organotrimethylsilanes., Manas Das, Donal F. O'Shea Jun 2014

Bu4n(+) Alkoxide-Initiated/Autocatalytic Addition Reactions With Organotrimethylsilanes., Manas Das, Donal F. O'Shea

Chemistry Articles

The use of Me3SiO(-)/Bu4N(+) as a general activator of organotrimethylsilanes for addition reactions has been established. The broad scope of the method offers trimethylsilanes (including acetate, allyl, propargyl, benzyl, dithiane, heteroaryl, and aryl derivatives) as bench-stable organometallics that can be readily utilized as carbanion equivalents for synthesis. Reactions are achieved at rt without the requirement of specialized precautions that are commonplace for other organometallics.


Current And Potential Applications Of Bismuth-Based Drugs., Donal M. Keogan, Darren M. Griffith Jan 2014

Current And Potential Applications Of Bismuth-Based Drugs., Donal M. Keogan, Darren M. Griffith

Chemistry Articles

Bismuth compounds have been used extensively as medicines and in particular for the treatment of gastrointestinal ailments. In addition to bismuth's well known gastroprotective effects and efficacy in treating H. pylori infection it also has broad anti-microbial, anti-leishmanial and anti-cancer properties. Aspects of the biological chemistry of bismuth are discussed and biomolecular targets associated with bismuth treatment are highlighted. This review strives to provide the reader with an up to date account of bismuth-based drugs currently used to treat patients and discuss potential medicinal applications of bismuth drugs with reference to recent developments in the literature. Ultimately this review ...