6 documents found, page 1 of 1
Antifungal and anti-biofilm activity of designed derivatives from kyotorphin
Andrade, Vitor Martins de; Bardaji, Eduard; Heras, Montserrat; Ramu, Vasanthakumar G.; Junqueira, Juliana Campos [UNESP]Made available in DSpace on 2020-12-10T19:58:54Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-05-01; Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP); Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES); Kyotorphin (KTP, L-tyrosyl-L-arginine) is an endogenous analgesic neuropeptide first isolated from bovine brain in 1979. Previous studies have shown that kyotorphins posses...
Antifungal and anti-biofilm activity of designed derivatives from kyotorphin
Martins de Andrade, Vitor; Bardají, Eduard; Heras, Montserrat; Ramu, Vasanthakumar G.; Junqueira, Juliana Campos; Diane dos Santos, JéssicaKyotorphin (KTP, l-tyrosyl-l-arginine) is an endogenous analgesic neuropeptide first isolated from bovine brain in 1979. Previous studies have shown that kyotorphins possess anti-inflammatory and antimicrobial activity. Six kyotorphins—KTP-NH2, KTP–NH2–DL, ibuprofen-conjugated KTP (IbKTP), IbKTP-NH2, N-methyl-D-Tyr-L-Arg, and N-methyl-L-Tyr-D-Arg—were designed and synthesized to improve lipophilicity and resist...
The anti‑inflammatory action of the analgesic kyotorphin neuropeptide derivativ...
Conceição, Katia; Magalhães, Pedro R.; Campos, Sara R. R.; Domingues, Marco M.; Ramu, Vasanthakumar G.; Michalek, Matthias Michalek; Bertani, PhilippeRecently, a designed class of efficient analgesic drugs derived from an endogenous neuropeptide, kyotorphin (KTP, Tyr-Arg) combining C-terminal amidation (KTP-NH2) and N-terminal conjugation to ibuprofen (Ib), IbKTP-NH2, was developed. The Ib moiety is an enhancer of KTP-NH2 analgesic action. In the present study, we have tested the hypothesis that KTP-NH2 is an enhancer of the Ib anti-inflammatory action. More...
Amidated and ibuprofen-conjugated kyotorphins promote neuronal rescue and memor...
Santos, Sónia Sá; Santos, Sara M.; Pinto, Antónia R. T.; Ramu, Vasanthakumar G.; Heras, Montserrat; Bardaji, Eduard; Tavares, IsauraChronic brain ischemia is a prominent risk factor for neurological dysfunction and progression for dementias, including Alzheimer's disease (AD). In rats, permanent bilateral common carotid artery occlusion (2VO) causes a progressive neurodegeneration in the hippocampus, learning deficits and memory loss as it occurs in AD. Kyotorphin (KTP) is an endogenous antinociceptive dipeptide whose role as neuromodulator...
Correlation between membrane translocation and analgesic efficacy in kyotorphin...
Serrano, Isa D.; Ramu, Vasanthakumar G.; Pinto, Antónia R. T.; Freire, João M.; Tavares, Isaura; Heras, Montserrat; Bardaji, Eduard R.Amidated kyotorphin (L-Tyr-L-Arg-NH2; KTP-NH2) causes analgesia when systemically administered. The lipophilic ibuprofen-conjugated derivative of KTP-NH2 has improved analgesic efficacy. However, fast degradation by peptidases impacts negatively in the pharmacodynamics of these drugs. In this work, selected derivatives of KTP and KTP-NH2 were synthesized to combine lipophilicity and resistance to enzymatic degr...
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...