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Gerald Zamponi

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https://www.readbyqxmd.com/read/27807163/long-term-potentiation-at-the-mossy-fiber-granule-cell-relay-invokes-postsynaptic-second-messenger-regulation-of-kv4-channels
#1
Arsalan P Rizwan, Xiaoqin Zhan, Gerald W Zamponi, Ray W Turner
: Mossy fiber afferents to cerebellar granule cells form the primary synaptic relay into cerebellum, providing an ideal site to process signal inputs differentially. Mossy fiber input is known to exhibit a long-term potentiation (LTP) of synaptic efficacy through a combination of presynaptic and postsynaptic mechanisms. However, the specific postsynaptic mechanisms contributing to LTP of mossy fiber input is unknown. The current study tested the hypothesis that LTP induces a change in intrinsic membrane excitability of rat cerebellar granule cells through modification of Kv4 A-type potassium channels...
November 2, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27768908/regulation-of-voltage-gated-calcium-channels-by-gpcrs-and-post-translational-modification
#2
Junting Huang, Gerald W Zamponi
Calcium entry via voltage gated calcium channels mediates a wide range of physiological functions, whereas calcium channel dysregulation has been associated with numerous pathophysiological conditions. There are myriad cell signaling pathways that act on voltage gated calcium channels to fine tune their activities and to regulate their cell surface expression. These regulatory mechanisms include the activation of G protein-coupled receptors and downstream phosphorylation events, and their control over calcium channel trafficking through direct physical interactions...
October 18, 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27756538/block-of-voltage-gated-calcium-channels-by-peptide-toxins
#3
Emmanuel Bourinet, Gerald W Zamponi
Venoms from various predatory species, such as fish hunting mollusks scorpions, snakes and arachnids contain a large spectrum of toxins that include blockers of voltage-gated calcium channels. These peptide blockers act by two principal manners - physical occlusion of the pore and prevention of activation gating. Many of the calcium channel-blocking peptides have evolved to tightly occupy their binding pocket on the principal pore forming subunit of the channel, often rendering block poorly reversible. Moreover, several of the best characterized blocking peptides have developed a high degree of channel subtype selectivity...
October 15, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27659162/cooperative-roles-of-glucose-and-asparagine-linked-glycosylation-in-t-type-calcium-channel-expression
#4
Joanna Lazniewska, Yuriy Rzhepetskyy, Fang-Xiong Zhang, Gerald W Zamponi, Norbert Weiss
T-type calcium channels are key contributors to neuronal physiology where they shape electrical activity of nerve cells and contribute to the release of neurotransmitters. Enhanced T-type channel expression has been causally linked to a number of pathological conditions including peripheral painful diabetic neuropathy. Recently, it was demonstrated that asparagine-linked glycosylation not only plays an essential role in regulating cell surface expression of Cav3.2 channels, but may also support glucose-dependent potentiation of T-type currents...
September 23, 2016: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/27130589/a-cell-permeant-peptide-corresponding-to-the-cubp-domain-of-usp5-reverses-inflammatory-and-neuropathic-pain
#5
Agustin Garcia-Caballero, Vinicius M Gadotti, Lina Chen, Gerald W Zamponi
BACKGROUND: Cav3.2 T-type calcium currents in primary afferents are enhanced in various painful pathological conditions, whereas inhibiting Cav3.2 activity or expression offers a strategy for combating the development of pain hypersensitivity. We have shown that Cav3.2 channel surface density is strongly regulated by the ubiquitination machinery and we identified the deubiquitinase USP5 as a Cav3.2 channel interacting protein and regulator of its cell surface expression. We also reported that USP5 is upregulated in chronic pain conditions...
2016: Molecular Pain
https://www.readbyqxmd.com/read/27053601/synthesis-and-characterization-of-a-disubstituted-piperazine-derivative-with-t-type-channel-blocking-action-and-analgesic-properties
#6
Zubaidha Pudukulatham, Fang-Xiong Zhang, Vinicius M Gadotti, Said M'Dahoma, Prabhuling Swami, Yasinalli Tamboli, Gerald W Zamponi
BACKGROUND: T-type calcium channels are important contributors to signaling in the primary afferent pain pathway and are thus important targets for the development of analgesics. It has been previously reported that certain piperazine-based compounds such as flunarizine are able to inhibit T-type calcium channels. Thus, we hypothesized that novel piperazine compounds could potentially act as analgesics. RESULTS: Here, we have created a series of 14 compound derivatives around a diphenyl methyl-piperazine core pharmacophore...
2016: Molecular Pain
https://www.readbyqxmd.com/read/27047338/reduced-hyperpolarization-activated-current-contributes-to-enhanced-intrinsic-excitability-in-cultured-hippocampal-neurons-from-prp-mice
#7
Jing Fan, Patrick L Stemkowski, Maria A Gandini, Stefanie A Black, Zizhen Zhang, Ivana A Souza, Lina Chen, Gerald W Zamponi
Genetic ablation of cellular prion protein (PrP(C)) has been linked to increased neuronal excitability and synaptic activity in the hippocampus. We have previously shown that synaptic activity in hippocampi of PrP-null mice is increased due to enhanced N-methyl-D-aspartate receptor (NMDAR) function. Here, we focused on the effect of PRNP gene knock-out (KO) on intrinsic neuronal excitability, and in particular, the underlying ionic mechanism in hippocampal neurons cultured from P0 mouse pups. We found that the absence of PrP(C) profoundly affected the firing properties of cultured hippocampal neurons in the presence of synaptic blockers...
2016: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/26542628/anticonvulsant-mechanisms-of-piperine-a-piperidine-alkaloid
#8
Awanish Mishra, Jasmine Kaur Punia, Chris Bladen, Gerald W Zamponi, Rajesh Kumar Goel
Piperine, a natural compound isolated from the fruits of Piper, is known to modulate several neurotransmitter systems such as serotonin, norepinephrine, and GABA, all of which have been linked to the development of convulsions. Fruits of Piper species have been suggested as means for managing seizure disorders. The present study was designed to elucidate the anticonvulsant effect of piperine and its mechanisms of action using in-silico, in-vivo and in-vitro techniques.PASS software was used to determine its possible activity and mechanisms...
2015: Channels
https://www.readbyqxmd.com/read/26542451/targeting-voltage-gated-calcium-channels-in-neurological-and-psychiatric-diseases
#9
REVIEW
Gerald W Zamponi
Voltage-gated calcium channels are important regulators of brain, heart and muscle functions, and their dysfunction can give rise to pathophysiological conditions ranging from cardiovascular disorders to neurological and psychiatric conditions such as epilepsy, pain and autism. In the nervous system, calcium channel blockers have been used successfully to treat absence seizures, and are emerging as potential therapeutic avenues for pathologies such as pain, Parkinson disease, addiction and anxiety. This Review provides an overview of calcium channels as drug targets for nervous system disorders, and discusses potential challenges and opportunities for the development of new clinically effective calcium channel inhibitors...
January 2016: Nature Reviews. Drug Discovery
https://www.readbyqxmd.com/read/26362469/the-physiology-pathology-and-pharmacology-of-voltage-gated-calcium-channels-and-their-future-therapeutic-potential
#10
REVIEW
Gerald W Zamponi, Joerg Striessnig, Alexandra Koschak, Annette C Dolphin
Voltage-gated calcium channels are required for many key functions in the body. In this review, the different subtypes of voltage-gated calcium channels are described and their physiologic roles and pharmacology are outlined. We describe the current uses of drugs interacting with the different calcium channel subtypes and subunits, as well as specific areas in which there is strong potential for future drug development. Current therapeutic agents include drugs targeting L-type Ca(V)1.2 calcium channels, particularly 1,4-dihydropyridines, which are widely used in the treatment of hypertension...
October 2015: Pharmacological Reviews
https://www.readbyqxmd.com/read/26354962/effect-of-the-t-type-channel-blocker-kys-05090s-in-mouse-models-of-acute-and-neuropathic-pain
#11
Saïd M'Dahoma, Vinicius M Gadotti, Fang-Xiong Zhang, Byeongyeon Park, Ji Hye Nam, Valentina Onnis, Gianfranco Balboni, Jae Yeol Lee, Gerald W Zamponi
T-type channels are important contributors to the initiation and the maintenance of chronic pain states. Blocking T-type channels is therefore a possible therapeutic strategy for relieving pain. Here, we report the Cav3.2 T-type channel blocking action of a previously reported small organic molecule, KYS-05090S. This compound was able to reduce transiently expressed Cav3.2 currents with low micromolar affinity and mediated a hyperpolarizing shift in half-inactivation potential. KYS-05090S was then tested in models of acute and neuropathic pain...
February 2016: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/26286466/analgesic-effect-of-a-broad-spectrum-dihydropyridine-inhibitor-of-voltage-gated-calcium-channels
#12
Vinicius M Gadotti, Chris Bladen, Fang Xiong Zhang, Lina Chen, Miyase Gözde Gündüz, Rahime Şimşek, Cihat Şafak, Gerald W Zamponi
Voltage-activated calcium channels are important facilitators of nociceptive transmission in the primary afferent pathway. Consequently, molecules that block these channels are of potential use as pain therapeutics. Our group has recently reported on the identification of a novel class of dihydropyridines (DHPs) that included compounds with preferential selectivity for T-type over L-type channels. Among those compounds, M4 was found to be an equipotent inhibitor of both Cav1.2 L- and Cav3.2 T-type calcium channels...
December 2015: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/26283201/all-roads-lead-to-presynaptic-calcium-channel-inhibition-by-the-ghrelin-receptor-separate-agonist-dependent-and-independent-signaling-pathways
#13
COMMENT
Norbert Weiss, Gerald W Zamponi
No abstract text is available yet for this article.
September 2015: Journal of General Physiology
https://www.readbyqxmd.com/read/26212331/role-of-prelimbic-gabaergic-circuits-in-sensory-and-emotional-aspects-of-neuropathic-pain
#14
Zizhen Zhang, Vinicius M Gadotti, Lina Chen, Ivana A Souza, Patrick L Stemkowski, Gerald W Zamponi
Noxious stimuli are detected by peripheral nociceptors and then transmitted to higher CNS centers, where they are perceived as an unpleasant sensation. The mechanisms that govern the emotional component associated with pain are still incompletely understood. Here, we used optogenetic approaches both in vitro and in vivo to address this issue. We found that peripheral nerve injury inhibits pyramidal cell firing in the prelimbic area of the prefrontal cortex as a result of feed-forward inhibition mediated by parvalbumin-expressing GABAergic interneurons...
August 4, 2015: Cell Reports
https://www.readbyqxmd.com/read/26206192/the-triggle-effect
#15
REVIEW
Terrance P Snutch, Gerald W Zamponi
Dr. David Triggle is considered a pioneer in the area of ion channel pharmacology. Over the course of his career, he made a number of particularly important contributions to our understanding of dihydropyridine interactions with L-type calcium channels. He also contributed his highly sought after expertise towards the drug discovery platform of the Canadian biopharmaceutical company, NeuroMed Pharmaceuticals (subsequently Zalicus). Here we briefly highlight his contributions to the field of calcium channel pharmacology, and then provide examples of his impact on NeuroMed...
November 15, 2015: Biochemical Pharmacology
https://www.readbyqxmd.com/read/26192347/inhibitory-effect-of-positively-charged-triazine-antagonists-of-prokineticin-receptors-on-the-transient-receptor-vanilloid-type-1-trpv1-channel
#16
Luciano De Petrocellis, Aniello Schiano Moriello, Joon Seok Byun, Joo Mi Sohn, Jae Yeol Lee, Ana Vázquez-Romero, Maria Garrido, Angel Messeguer, Fang-Xiong Zhang, Gerald W Zamponi, Alessandro Deplano, Cenzo Congiu, Valentina Onnis, Gianfranco Balboni, Vincenzo Di Marzo
Four positively charged compounds, previously shown to produce analgesic activity by interacting with prokineticin receptor or T-type calcium channels, were tested for their ability to inhibit capsaicin-induced elevation of intracellular Ca(2+) in HEK-293 cells stably transfected with the human recombinant TRPV1, with the goal of identifying novel TRPV1 open-pore inhibitors. KYS-05090 showed the highest potency as a TRPV1 antagonist, even higher than that of the open-pore triazine inhibitor 8aA. The latter showed quite remarkable agonist/desensitizer activity at the rat recombinant TRPM8 channel...
September 2015: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/25966707/calcium-channel-signaling-complexes-with-receptors-and-channels
#17
REVIEW
Gerald W Zamponi
Voltage-gated calcium channels are not only mediators of cell signalling events, but also are recipients of signalling inputs from G protein coupled receptors (GPCRs) and their associated second messenger pathways. The coupling of GPCRs to calcium channels is optimized through the formation of receptor-channel complexes. In addition, this provides a mechanism for receptorchannel co-trafficking to and from the plasma membrane. On the other hand, voltage-gated calcium channel activity affects other types of ion channels such as voltage-and calcium-activated potassium channels...
2015: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/25889575/small-organic-molecule-disruptors-of-cav3-2-usp5-interactions-reverse-inflammatory-and-neuropathic-pain
#18
Vinicius M Gadotti, Agustin Garcia Caballero, N Daniel Berger, Clare M Gladding, Lina Chen, Tom A Pfeifer, Gerald W Zamponi
BACKGROUND: Cav3.2 channels facilitate nociceptive transmission and are upregulated in DRG neurons in response to nerve injury or peripheral inflammation. We reported that this enhancement of Cav3.2 currents in afferent neurons is mediated by deubiquitination of the channels by the deubiquitinase USP5, and that disrupting USP5/Cav3.2 channel interactions protected from inflammatory and neuropathic pain. RESULTS: Here we describe the development of a small molecule screening assay for USP5-Cav3...
March 14, 2015: Molecular Pain
https://www.readbyqxmd.com/read/25888324/glutamate-receptors-function-as-scaffolds-for-the-regulation-of-%C3%AE-amyloid-and-cellular-prion-protein-signaling-complexes
#19
REVIEW
Alison Hamilton, Gerald W Zamponi, Stephen S G Ferguson
Alzheimer's disease (AD) is a progressive neurodegenerative disorder that affects 36 million people worldwide, but currently has no effective treatment options. One of the original hallmarks of AD are plaques comprised of beta amyloid (Aβ) and neurofibrillary tangles comprised of phosphorylated Tau protein. However, it is soluble oligomeric Aβ which is more closely correlated with cognitive decline and is therefore considered to be the neurotoxic species. Oligomeric Aβ has recently been shown to form complexes with the glycosylphosphatidylinositol (GPI)-anchored membrane protein, cellular prion protein (PrP(c)), and these complexes are believed to play an important role in the progression of AD pathogenesis...
2015: Molecular Brain
https://www.readbyqxmd.com/read/25865881/ikca-channels-are-a-critical-determinant-of-the-slow-ahp-in-ca1-pyramidal-neurons
#20
Brian King, Arsalan P Rizwan, Hadhimulya Asmara, Norman C Heath, Jordan D T Engbers, Steven Dykstra, Theodore M Bartoletti, Shahid Hameed, Gerald W Zamponi, Ray W Turner
Control over the frequency and pattern of neuronal spike discharge depends on Ca2+-gated K+ channels that reduce cell excitability by hyperpolarizing the membrane potential. The Ca2+-dependent slow afterhyperpolarization (sAHP) is one of the most prominent inhibitory responses in the brain, with sAHP amplitude linked to a host of circuit and behavioral functions, yet the channel that underlies the sAHP has defied identification for decades. Here, we show that intermediate-conductance Ca2+-dependent K+ (IKCa) channels underlie the sAHP generated by trains of synaptic input or postsynaptic stimuli in CA1 hippocampal pyramidal cells...
April 14, 2015: Cell Reports
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