4 documents found, page 1 of 1
Side-effects of analgesic kyotorphin derivatives : advantages over clinical opi...
Ribeiro, Marta M. B.; Santos, Sónia Sá; Sousa, David S. C.; Oliveira, Margarida; Santos, Sara M.; Heras, Montserrat; Bardaji, Eduard; Tavares, IsauraThe adverse side-effects associated with opioid administration restrain their use as analgesic drugs and call for new solutions to treat pain. Two kyotorphin derivatives, kyotorphin-amide (KTP–NH2) and ibuprofen–KTP–NH2 (IbKTP–NH2) are promising alternatives to opioids: they trigger analgesia via an indirect opioid mechanism and are highly effective in several pain models following systemic delivery. In vivo si...
Translocating the blood-brain barrier using electrostatics
Ribeiro, Marta M. B.; Domingues, Marco M.; Freire, João M.; Santos, Nuno C.; Castanho, Miguel A. R. B.Mammalian cell membranes regulate homeostasis, protein activity, and cell signaling. The charge at the membrane surface has been correlated with these key events. Although mammalian cells are known to be slightly anionic, quantitative information on the membrane charge and the importance of electrostatic interactions in pharmacokinetics and pharmacodynamics remain elusive. Recently, we reported for the first ti...
Antimicrobial properties of analgesic kyotorphin peptides unraveled through ato...
Ribeiro, Marta M. B.; Franquelim, Henri G.; Torcato, Inês M.; Ramu, Vasanthakumar G.; Heras, Montserrat; Bardaji, Eduard R.; Castanho, Miguel A. R. B.Antimicrobial peptides (AMPs) are promising candidates as alternatives to conventional antibiotics for the treatment of resistant pathogens. In the last decades, new AMPs have been found from the cleavage of intact proteins with no antibacterial activity themselves. Bovine hemoglobin hydrolysis, for instance, results in AMPs and the minimal antimicrobial peptide sequence was defined as Tyr-Arg plus a positively...
Drug–lipid interaction evaluation : why a 19th century solution?
Ribeiro, Marta M. B.; Melo, Manuel N.; Serrano, Isa D.; Santos, Nuno C.; Castanho, Miguel A. R. B.The affinity of a drug candidate for a biological membrane (its lipophilicity) is closely related to the pharmacologically crucial events of absorption, biodistribution, metabolization and excretion. The evolution of knowledge of biological membranes during the past two decades contrasts with the rudimentary parameter most commonly used to assess lipophilicity: Po/w, the octanol–water partition coefficient. Po/...