A5061719307- Neuropeptides and Animal Physiology
- Receptor Mechanisms and Signaling
- Pain Mechanisms and Treatments
- Chemical Synthesis and Analysis
- Hypothalamic control of reproductive hormones
- Pharmacological Receptor Mechanisms and Effects
- Sleep and Wakefulness Research
- Cardiovascular, Neuropeptides, and Oxidative Stress Research
- Regulation of Appetite and Obesity
- Immunotherapy and Immune Responses
- Stress Responses and Cortisol
- Hormonal Regulation and Hypertension
- Biochemical effects in animals
- Apelin-related biomedical research
- Peptidase Inhibition and Analysis
- Monoclonal and Polyclonal Antibodies Research
- Neuroendocrine regulation and behavior
- Neuroscience and Neuropharmacology Research
- Biochemical and Structural Characterization
- Trace Elements in Health
- Alzheimer's disease research and treatments
- Urinary Bladder and Prostate Research
- Enzyme Structure and Function
- Circadian rhythm and melatonin
- Sexual function and dysfunction studies
University of Ferrara
2016-2025
Center for Translational Neurophysiology of Speech and Communication
2020-2021
Tecnologie Avanzate (Italy)
2014-2020
Wake Forest University
2015
University of California, Irvine
2007-2009
Istituto di Chimica Biomolecolare
2007
National Institute of Environmental Health Sciences
1996-2005
Leicester Royal Infirmary
2000-2005
University of Cagliari
2002-2005
University of Naples Federico II
1994-2004
The major components of neuritic plaques found in Alzheimer disease (AD) are peptides known as amyloid beta-peptides (Abeta), which derive from the proteolitic cleavage precursor proteins. In vitro Abeta may undergo a conformational transition soluble form to aggregated, fibrillary beta-sheet structures, seem be neurotoxic. Alternatively, it has been suggested that an alpha-helical can involved process membrane poration, would then trigger cellular death. Conformational studies on these...
Current views of the role beta-amyloid (Abeta) peptide fibrils range from regarding them as cause Alzheimer's pathology to having a protective function. In last few years, it has also been suggested that soluble oligomers might be most important toxic species. all cases, study conformational properties Abeta peptides in form constitutes basic approach design molecules with "antiamyloid" activity. We have experimentally investigated path can lead Abeta-(1-42) native state, which is...
[Phe1psi(CH2-NH)Gly2]NC(1-13)NH2 has been tested in the electrically stimulated guinea pig ileum and mouse vas deferens, two nociceptin sensitive preparations. The new compound showed per se little or no effect tissues, but it displaced to right concentration-response curves of a concentration-dependent manner. Schild analyses data indicated competitive type antagonism pA2 values 7.02 6.75 guinea-pig respectively. At 10 microM does not modify either inhibitory deltorphin I (the selective...
Nociceptin (NC) and some of its fragments as well nociceptin-(1-13)-peptide amide [NC- (1-13)-NH2] a series analogues were prepared tested in the mouse vas deferens an attempt to identify sequences involved activation (message) binding (address) nociceptin receptor. The NC receptor that inhibits electrically evoked twitches was demonstrated be distinct from delta opioid receptor, since naloxone Dmt-Tic-OH (a selective antagonist) block but have no effect on Results structure-activity...
Neuropeptide S (NPS) was recently identified as the endogenous ligand of an orphan receptor, now referred to NPS receptor. In vivo, produces a unique behavioural profile by increasing wakefulness and exerting anxiolytic-like effects. present study, we further evaluated effects in vivo supraspinal mice.Effects NPS, injected intracerebroventricularly (i.c.v.), on locomotor activity (LA), righting reflex (RR) recovery anxiety states (measured with elevated plus maze (EPM) stress-induced...
Nociceptin (orphanin FQ) is a novel neuropeptide capable of inducing variety biological actions via activation specific G‐protein coupled receptor. However, the lack selective nociceptin receptor antagonist has hampered our understanding and role this peptide in pathophysiological states. As part broader programme research, geared to identification characterization ligands, we report that [Nphe 1 ]nociceptin(1‐13)NH 2 acts as first truly competitive devoid any residual agonist activity....
Nociceptin/orphanin FQ (N/OFQ) modulates several biological functions by activating a specific G‐protein coupled receptor (NOP). Few molecules are available that selectively activate or block the NOP receptor. Here we describe in vitro and vivo pharmacological profile of novel ligand, [Nphe 1 ,Arg 14 ,Lys 15 ]N/OFQ‐NH 2 (UFP‐101). UFP‐101 binds to human recombinant expressed Chinese hamster ovary (CHO) cells with high affinity (pK i 10.2) shows more than 3000 fold selectivity over classical...
The design of molecules able to interact with the amyloid peptides either as inhibitors fibril formation or membrane pore represents one most relevant approaches in development anti-Alzheimer therapies. Aβ-(25−35), sequence GSNKGAIIGLM, is a highly toxic synthetic derivative β-peptides (Aβ-peptides), which forms fibrillary aggregates. Here, we report NMR and CD investigation Aβ-(25−35) membrane-mimicking environment isotropic mixtures water fluoro-alcohols scan its conformational properties...
The opioid-like neuropeptide nociceptin/orphanin FQ (N/OFQ) and its receptor (NOP) are expressed in the substantia nigra (SN), a brain area containing dopamine neurons that degenerate Parkinson's disease. Endogenous N/OFQ facilitates nigral glutamate release inhibits nigrostriatal transmission motor behavior. Here, we present evidence suggesting endogenous may contribute to Pharmacological blockade of SN N/OFQ-NOP system attenuated parkinsonian-like akinesia/hypokinesia 6-hydroxydopamine...
Human thymidylate synthase is a homodimeric enzyme that plays key role in DNA synthesis and target for several clinically important anticancer drugs bind to its active site. We have designed peptides specifically dimer interface. Here we show through X-ray diffraction, spectroscopic, kinetic, calorimetric evidence the do indeed at interface of dimeric protein stabilize di-inactive form. The "LR" peptide binds previously unknown binding site shows undescribed mechanism allosteric inhibition...
Nociceptin/orphanin FQ (N/OFQ), the endogenous ligand of NOP receptor, regulates several central functions such as pain transmission, learning and memory, fear anxiety feeding locomotor activity. It has been recently reported that receptor antagonists induce antidepressant-like effects in mouse forced swimming test (FST), i.e. reduce immobility time. This assay was used present study for further investigating involvement depression states. In male Swiss mice, intracerebroventricular...
The protease activated receptor-2 (PAR-2) belongs to a family of G-protein-coupled receptors that are by proteolysis. Trypsin cleaves PAR-2, exposing an N-terminal tethered ligand (SLIGRL) activates the receptor. Messenger RNA (mRNA) for PAR-2 was found in guinea pig airway tissue reverse transcription-polymerase chain reaction, and immunohistochemistry epithelial smooth-muscle cells. In anesthetized pigs, trypsin SLIGRL-NH(2) (given intratracheally or intravenously) caused...
The newly discovered neuropeptide nociceptin (NC) has recently been reported to be the endogenous ligand of opioid‐like orphan receptor. Despite its structural similarity opioids, when injected intracerebroventricularly (i.c.v.) in mouse, NC exerts a direct hyperalgesic effect and reverses opioid‐induced analgesia. In present investigation, these two effects were evaluated under same experimental conditions; addition, pharmacological characterization receptor mediating central was attempted....
A multidisciplinary approach was followed to investigate whether the opioid-like peptide nociceptin/orphanin FQ (N/OFQ) regulates nigrostriatal dopaminergic pathway and motor behavior. Nigrostriatal cells, which express N/OFQ (NOP) receptors, are located in substantia nigra pars compacta extend their dendrites reticulata, thereby modulating basal ganglia output neurons. In vitro electrophysiological recordings demonstrated that hyperpolarized cells of inhibited firing activity. vivo...
Neuropeptide S (NPS) has been recently recognized as the endogenous ligand for previous orphan G-protein-coupled receptor GPR154, now referred to NPS (NPSR). The NPS-NPSR system regulates important biological functions such sleeping/wakening, locomotion, anxiety, and food intake. To collect information on mechanisms of interaction between its receptor, a classical structure-activity relationship study was performed. Human (h) derivatives obtained by Ala d-scan N- C-terminal truncation were...