Gerald W. Zamponi
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View article: N-terminal α-amino SUMOylation promotes phosphorylation-independent cofilin-1 translocation to the mitochondrial matrix and induces apoptosis
N-terminal α-amino SUMOylation promotes phosphorylation-independent cofilin-1 translocation to the mitochondrial matrix and induces apoptosis Open
Cofilin is a central regulator of actin filament turnover, traditionally thought to act through phosphorylation-dependent control of filament assembly. However, its mitochondrial functions remain poorly understood. Here we show that N-term…
View article: Pharmacological inhibition of NaV1.8 by suzetrigine reveals potent analgesic potential without tolerance development in mice
Pharmacological inhibition of NaV1.8 by suzetrigine reveals potent analgesic potential without tolerance development in mice Open
View article: A pathological missense mutation in the deubiquitinase USP5 leads to insensitivity to pain
A pathological missense mutation in the deubiquitinase USP5 leads to insensitivity to pain Open
Cav3.2 T-type calcium channels and their dysregulation by the deubiquitinase USP5 contribute to development of inflammatory and neuropathic pain. We report on a pediatric patient with a de novo heterozygous missense mutation R24W in USP5 w…
View article: The terpenes alpha-bisabolol and camphene modulate pruritus via an action on Cav3.2 T-type calcium channels
The terpenes alpha-bisabolol and camphene modulate pruritus via an action on Cav3.2 T-type calcium channels Open
View article: Biginelli dihydropyrimidines and their acetylated derivatives as L‐/T‐type calcium channel blockers: Synthesis, enantioseparation, and molecular modeling studies
Biginelli dihydropyrimidines and their acetylated derivatives as L‐/T‐type calcium channel blockers: Synthesis, enantioseparation, and molecular modeling studies Open
Biginelli dihydropyrimidines (DHPMs) are considered superior over 1,4‐dihydropyridines (DHPs) in terms of both light and metabolic stabilities. Nevertheless, DHPs dominate the market as the most prescribed calcium channel blockers with str…
View article: The N-type calcium channel rises from the ashes
The N-type calcium channel rises from the ashes Open
Chronic pain is a debilitating condition that affects up to 1.5 billion people globally. Advancing pain management depends on a thorough understanding of the types of pain experienced by patients and the underlying mechanisms driving it. N…
View article: Ca2+ signaling in vascular smooth muscle and endothelial cells in blood vessel remodeling: a review
Ca2+ signaling in vascular smooth muscle and endothelial cells in blood vessel remodeling: a review Open
View article: CaV3.2 T-type calcium channels contribute to CGRP- induced allodynia in a rodent model of experimental migraine
CaV3.2 T-type calcium channels contribute to CGRP- induced allodynia in a rodent model of experimental migraine Open
View article: Navigating the Controversies: Role of TRPM Channels in Pain States
Navigating the Controversies: Role of TRPM Channels in Pain States Open
Chronic pain is a debilitating condition that affects up to 1.5 billion people worldwide and bears a tremendous socioeconomic burden. The success of pain medicine relies on our understanding of the type of pain experienced by patients and …
View article: Non-small cell lung cancer sensitisation to platinum chemotherapy via new thiazole-triazole hybrids acting as dual T-type CCB/MMP-9 inhibitors
Non-small cell lung cancer sensitisation to platinum chemotherapy via new thiazole-triazole hybrids acting as dual T-type CCB/MMP-9 inhibitors Open
Cisplatin remains the unchallenged standard therapy for NSCLC. However, it is not completely curative due to drug resistance and oxidative stress-induced toxicity. Drug resistance is linked to overexpression of matrix metalloproteinases (M…
View article: Determinants of interactions of a novel next-generation gabapentinoid NVA1309 and mirogabalin with the Cavα2δ-1 subunit
Determinants of interactions of a novel next-generation gabapentinoid NVA1309 and mirogabalin with the Cavα2δ-1 subunit Open
NVA1309 is a non-brain penetrant next-generation gabapentinoid shown to bind Cavα2δ at R243 within a triple Arginine motif forming the binding site for gabapentin and pregabalin. In this study we have compared the effects of NVA1309 with M…
View article: Spared nerve injury leads to reduced activity of neurons projecting from the ventrolateral periaqueductal gray to the locus coeruleus
Spared nerve injury leads to reduced activity of neurons projecting from the ventrolateral periaqueductal gray to the locus coeruleus Open
View article: Pannexin-1 channel inhibition alleviates opioid withdrawal in rodents by modulating locus coeruleus to spinal cord circuitry
Pannexin-1 channel inhibition alleviates opioid withdrawal in rodents by modulating locus coeruleus to spinal cord circuitry Open
View article: Expression of GAD2 in excitatory neurons projecting from the ventrolateral periaqueductal gray to the locus coeruleus
Expression of GAD2 in excitatory neurons projecting from the ventrolateral periaqueductal gray to the locus coeruleus Open
View article: Functional remodeling of presynaptic voltage-gated calcium channels in superficial layers of the dorsal horn during neuropathic pain
Functional remodeling of presynaptic voltage-gated calcium channels in superficial layers of the dorsal horn during neuropathic pain Open
N- and P/Q-type voltage-gated Ca2+ channels are critical for synaptic transmission. While their expression is increased in the dorsal root ganglion (DRG) neuron cell bodies during neuropathic pain conditions, less is known about…
View article: A tale of two calcium channels: structural pharmacology of Cav2.1 and Cav3.2
A tale of two calcium channels: structural pharmacology of Cav2.1 and Cav3.2 Open
View article: A next generation peripherally restricted Cavα2δ-1 ligand with inhibitory action on Cav2.2 channels and utility in neuropathic pain
A next generation peripherally restricted Cavα2δ-1 ligand with inhibitory action on Cav2.2 channels and utility in neuropathic pain Open
The Voltage-Gated Calcium Channel (VGCC) auxiliary subunit Cavα2δ-1 (CACNA2D1) is the target/receptor of gabapentinoids which are known therapeutics in epilepsy and neuropathic pain. Following damage to the peripheral sensory nervous syste…
View article: Opening the KV3.1 gates: A therapeutic strategy for progressive myoclonus epilepsy type 7?
Opening the KV3.1 gates: A therapeutic strategy for progressive myoclonus epilepsy type 7? Open
View article: Electrophysiological characterization of a Cav3.2 calcium channel missense variant associated with epilepsy and hearing loss
Electrophysiological characterization of a Cav3.2 calcium channel missense variant associated with epilepsy and hearing loss Open
T-type calcium channelopathies encompass a group of human disorders either caused or exacerbated by mutations in the genes encoding different T-type calcium channels. Recently, a new heterozygous missense mutation in the CACNA1H gene that …
View article: Inhibitory insula-ACC projections modulate affective but not sensory aspects of neuropathic pain
Inhibitory insula-ACC projections modulate affective but not sensory aspects of neuropathic pain Open
The insula and anterior cingulate cortex (ACC) are brain regions that undergo structural and functional reorganization in neuropathic pain states. Here, we aimed to study inhibitory parvalbumin positive (PV+) posterior insula (pIC) to post…
View article: Antihyperalgesic effect of joint mobilization requires Cav3.2 calcium channels
Antihyperalgesic effect of joint mobilization requires Cav3.2 calcium channels Open
View article: Analgesia by intrathecal delta-9-tetrahydrocannabinol is dependent on Cav3.2 calcium channels
Analgesia by intrathecal delta-9-tetrahydrocannabinol is dependent on Cav3.2 calcium channels Open
View article: Differential regulation of Ca<sub>v</sub>3.2 and Ca<sub>v</sub>2.2 calcium channels by CB<sub>1</sub> receptors and cannabidiol
Differential regulation of Ca<sub>v</sub>3.2 and Ca<sub>v</sub>2.2 calcium channels by CB<sub>1</sub> receptors and cannabidiol Open
Background and Purpose Cannabinoids are a promising therapeutic avenue for chronic pain. However, clinical trials often fail to report analgesic efficacy of cannabinoids. Inhibition of voltage gate calcium (Ca v ) channels is one mechanism…
View article: Excitation-transcription coupling in smooth muscle is associated with vascular remodeling
Excitation-transcription coupling in smooth muscle is associated with vascular remodeling Open
Various stresses loaded on the arteries induce vascular remodeling. Macrophages accumulated in the vascular wall promote dedifferentiation and proliferation of smooth muscle cells (SMC) and induce vascular remodeling. However, it remains u…
View article: Regulation of N-type calcium channels by nociceptin receptors and its possible role in neurological disorders
Regulation of N-type calcium channels by nociceptin receptors and its possible role in neurological disorders Open
Activation of nociceptin opioid peptide receptors (NOP, a.k.a. opioid-like receptor-1, ORL-1) by the ligand nociceptin/orphanin FQ, leads to G protein-dependent regulation of Cav2.2 (N-type) voltage-gated calcium channels (VGCCs). This typ…
View article: Electrophysiological and computational analysis of Cav3.2 channel variants associated with familial trigeminal neuralgia
Electrophysiological and computational analysis of Cav3.2 channel variants associated with familial trigeminal neuralgia Open
View article: The road to the brain in Timothy syndrome is paved with enhanced CaV1.2 activation gating
The road to the brain in Timothy syndrome is paved with enhanced CaV1.2 activation gating Open
Specific gating effects of Timothy syndrome CaV1.2 channel mutations determine cardiovascular versus nervous system deficits.
View article: 6-Formyl Umbelliferone, a Furanocoumarin from Angelica decursiva L., Inhibits Key Diabetes-Related Enzymes and Advanced Glycation End-Product Formation
6-Formyl Umbelliferone, a Furanocoumarin from Angelica decursiva L., Inhibits Key Diabetes-Related Enzymes and Advanced Glycation End-Product Formation Open
Over the years, great attention has been paid to coumarin derivatives, a set of versatile molecules that exhibit a wide variety of biological activities and have few toxic side effects. In this study, we investigated the antidiabetic poten…
View article: Copper ions, prion protein and Aβ modulate Ca levels in central nervous system myelin in an NMDA receptor-dependent manner
Copper ions, prion protein and Aβ modulate Ca levels in central nervous system myelin in an NMDA receptor-dependent manner Open
View article: The neuronal tyrosine kinase receptor ligand ALKAL2 mediates persistent pain
The neuronal tyrosine kinase receptor ligand ALKAL2 mediates persistent pain Open
The anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase known for its oncogenic potential that is involved in the development of the peripheral and central nervous system. ALK receptor ligands ALKAL1 and ALKAL2 were recently fou…