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Design of natterins-based peptides improves antimicrobial and antiviral activities

de Cena, Gabrielle L.; Tada, Dayane B.; Lucchi, Danilo B. M.; Santos, Tiago; Heras, Montserrat; Juliano, Maria; Torres Braconi, Carla

The biochemical analysis of animal venoms has been intensifying over the years, enabling the prediction of new molecules derived from toxins, harnessing the therapeutic potential of these molecules. From the venom of the fish Thalassophryne nattereri, using in silico methods for predicting antimicrobial and cell-penetrating peptides, two peptides from Natterins with promising characteristics were synthesized an...


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...

Date: 2020   |   Origin: Oasisbr

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, Jéssica

Kyotorphin (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 neuroprotective action of amidated-kyotorphin on amyloid β peptide-induced ...

Belo, Rita F.; Martins, Margarida L. F.; Shvachiy, Liana; Costa-Coelho, Tiago; de Almeida-Borlido, Carolina; Fonseca-Gomes, João; Neves, Vera

Kyotorphin (KTP, l-tyrosyl-l-arginine) is an endogenous dipeptide initially described to have analgesic properties. Recently, KTP was suggested to be an endogenous neuroprotective agent, namely for Alzheimer's disease (AD). In fact, KTP levels were shown to be decreased in the cerebrospinal fluid of patients with AD, and recent data showed that intracerebroventricular (i.c.v.) injection of KTP ameliorates memor...


Quantitative analysis of molecular partition towards lipid membranes using surf...

Figueira, Tiago N.; Freire, João M.; Santos, Catarina Cunha; Heras, Montserrat; Gonçalves, João; Moscona, Anne; Porotto, Matteo; Veiga, Ana Salomé

Understanding the interplay between molecules and lipid membranes is fundamental when studying cellular and biotechnological phenomena. Partition between aqueous media and lipid membranes is key to the mechanism of action of many biomolecules and drugs. Quantifying membrane partition, through adequate and robust parameters, is thus essential. Surface Plasmon Resonance (SPR) is a powerful technique for studying ...


Quantitative analysis of molecular partition towards lipid membranes using surf...

Figueira, Tiago N.; Freire, João M.; Santos, Catarina Cunha; Heras, Montserrat; Gonçalves, João; Moscona, Anne; Porotto, Matteo; Veiga, Ana Salomé

Understanding the interplay between molecules and lipid membranes is fundamental when studying cellular and biotechnological phenomena. Partition between aqueous media and lipid membranes is key to the mechanism of action of many biomolecules and drugs. Quantifying membrane partition, through adequate and robust parameters, is thus essential. Surface Plasmon Resonance (SPR) is a powerful technique for studying ...


Neuropeptide kyotorphin impacts on lipopolysaccharide-induced glucocorticoid-me...

Perazzo, Juliana; Lima, Carla; Heras, Montserrat; Bardají, Eduard; Ferreira, Mônica Lopes; Castanho, Miguel A. R. B.

Neuropeptide kyotorphin (KTP) is a potent analgesic if administered directly into the brain. In contrast, KTP-amide (KTP-NH2) is analgesic, neuroprotective, and anti-inflammatory following systemic administration, albeit its mechanism of action is unknown. The aim of this study was to shed light on the mechanism of action of KTP-NH2 at the molecular level. KTP-NH2 does not inhibit the enkephalinases angiotensin...


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, Philippe

Recently, 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...


Endothelium-mediated action of analogues of the endogenous neuropeptide kyotorp...

Perazzo, Juliana; Ferreira, Mónica Lopes; Santos, Sónia Sá; Serrano, Isa; Pinto, Antónia; Lima, Carla; Bardaji, Eduard; Tavares, Isaura

Kyotorphin (KTP) is an endogenous peptide with analgesic properties when administered into the central nervous system (CNS). Its amidated form (l-Tyr-l-Arg-NH2; KTP-NH2) has improved analgesic efficacy after systemic administration, suggesting blood-brain barrier (BBB) crossing. KTP-NH2 also has anti-inflammatory action impacting on microcirculation. In this work, selected derivatives of KTP-NH2 were synthesize...


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, Isaura

Chronic 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...


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