Overcoming antibiotic resistance in biofilms using glycopeptide dendrimers.

Antibiotic resistance in the opportunistic pathogen is partly caused by biofilms forming a physical barrier to antibiotic penetration. Here we focused on modifying tetravalent glycopeptide dendrimer ligands of lectins LecB or LecA to increase their biofilm inhibition activity. First heteroglycoclusters were investigated displaying one pair each of LecB specific fucosyl groups and LecA specific galactosyl groups and binding simultaneously to both lectins, one of which gave the first fully resolved crystal structure of a peptide dendrimer as LecB complex providing a structural model for dendrimer-lectin interactions (PDB ; 5D2A).

A cancer therapeutic vaccine based on clustered Tn-antigen mimetics induces strong antibody-mediated protective immunity.

Tumor-associated carbohydrate antigens (TACAs) are key components of cancer vaccines. A variety of vaccines based on native TACAs such as α-Tn have shown immunogenicity and protection in preclinical animal studies, however, their weak immunogenicity, low in vivo instability, and poor bioavailability, have discouraged their further evaluations in clinical studies. A new improved vaccine prototype is reported.

Synthesis of a selective inhibitor of a fucose binding bacterial lectin from Burkholderia ambifaria.

Burkholderia ambifaria is a bacterium member of the Burkholderia cepacia complex (BCC), a closely related group of Gram-negative bacteria responsible for "cepacia syndrome" in immunocompromised patients. B. ambifaria produces BambL, a fucose-binding lectin that displays fine specificity to human fucosylated epitopes.

Controlled-release oxycodone tablets after transdermal-based opioid therapy in patients with cancer and non-cancer pain.

Background And Aims: Several publications and guidelines stress the efficacy and safety of opioid-based therapy for cancer and non-cancer pain management. The first point of the World Health Organization (WHO) guidelines recommends that, if possible, analgesics should be given by mouth. This advice fully matches the European Society for Medical Oncology (ESMO) guidelines, which advise that opioids should be titrated to take effect as rapidly as possible.