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After years of living with unresolved pain following surgery for a pilonidal cyst, Alex was left without This is a story about how chronic pain doesn't just shape lives — it reshapes careers. “I wasn’t able to get stronger pain meds,” he said. “So I had to understand the biology myself.” Mike Caterina on pain mechanisms in the peripheral nervous system. , pain neuroscience

Watch Episode 170 What We’re Missing in Pain Research In GPCR drug discovery, receptors typically steal Signaling (RGS proteins)  might hold some of the most untapped therapeutic opportunities, particularly in pain neuroscience. Venetia Zachariou  introduced him to the power of RGS proteins — particularly RGS4  — in modulating pain models and hints that RGS proteins could modulate pain chronification itself .

Watch Episode 170 Thinking Differently Pain research has long followed a familiar route: from molecule conventional bottom-up approach often fails to deliver therapies that truly help patients, especially in the pain patient-centric and behavior-first approach uncovered robust gene expression signatures  linked to pain Why This Approach Matters In pain research, bottom-up approaches often fail to translate. Alex Serafini makes the case for building pain research from the clinic down, not the bench up. _____

CXCR4 takes on a nuclear role in red blood cell maturation CXCL13/CXCR5 emerges as a high-potential pain target ST171, a biased 5‑HT1A agonist, delivers selective pain relief in preclinical models Dr.GPCR Blocking this chemokine axis reduces pain  hypersensitivity by dampening neuroinflammation and glial This novel agonist activates Gi/o selectively , avoiding β-arrestin and showing strong pain relief in

Company’s novel S1P1 receptor modulator being developed as a potential treatment for diabetic neuropathic pain

November 22, 2021 JUPITER, FL—Scientists at Scripps Research in Florida have created a collection of new pain-relieving

of curiosity, persistence, and using science to meet unmet clinical needs, especially in the chronic pain Clifford Woolf, a leader in pain biology. slow down or prevent good science from reaching patients — particularly in underfunded fields like pain seeds for what would later become Blue Therapeutics, a startup he co-founded to develop non-addictive pain Whether it's chronic pain, addiction, or another unmet need, keeping the real-world impact in focus can

John Streicher talks about his work on terpenes found in cannabis as these may be a novel way to treat pain These compounds may be a novel way to treat pain without the negative side effects of cannabinoids or

a variety of potential clinical applications with a great interest in the treatment of neuropathic pain optimization, this series of compounds could represent potential clinically useful S1R ligands for pain

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), which ought to facilitate neurotransmission, and improve cognition. Yet, despite this upregulation, associated physiological effects are not observed in AD patients. This paradox solicits urgent attention to find a suitable justification for disturbed neurotransmission in AD. This article focuses on the role of Aβ granules and their possible interaction with GPCRs that modulate neurotransmission and AD progression." Read more at the source #DrGPCR #GPCR #IndustryNews

Therapeutics Doses First Subjects In Phase 1 Clinical Trial Of CFTX-1554 For The Treatment Of Neuropathic Pain CFTX-1554 is being developed as a non-opioid approach to the treatment of neuropathic pain, a debilitating

August 2022 GPR3 expression in retinal ganglion cells contributes to neuron survival and accelerates axonal regeneration after optic nerve crush in mice "Glaucoma is an optic neuropathy and is currently one of the most common diseases that leads to irreversible blindness. The axonal degeneration that occurs before retinal ganglion neuronal loss is suggested to be involved in the pathogenesis of glaucoma. G protein-coupled receptor 3 (GPR3) belongs to the class A rhodopsin-type GPCR family and is highly expressed in various neurons. GPR3 is unique in its ability to constitutively activate the Gαs protein without a ligand, which elevates the basal intracellular cAMP level. Our earlier reports suggested that GPR3 enhances both neurite outgrowth and neuronal survival. However, the potential role of GPR3 in axonal regeneration after neuronal injury has not been elucidated. Herein, we investigated retinal GPR3 expression and its possible involvement in axonal regeneration after retinal injury in mice. GPR3 was relatively highly expressed in retinal ganglion cells (RGCs). Surprisingly, RGCs in GPR3 knockout mice were vulnerable to neural death during aging without affecting high intraocular pressure (IOP) and under ischemic conditions. Primary cultured neurons from the retina showed that GPR3 expression was correlated with neurite outgrowth and neuronal survival. Evaluation of the effect of GPR3 on axonal regeneration using GPR3 knockout mice revealed that GPR3 in RGCs participates in axonal regeneration after optic nerve crush (ONC) under zymosan stimulation. In addition, regenerating axons were further stimulated when GPR3 was upregulated in RGCs, and the effect was further augmented when combined with zymosan treatment. These results suggest that GPR3 expression in RGCs helps maintain neuronal survival and accelerates axonal regeneration after ONC in mice." Read more at the source #DrGPCR #GPCR #IndustryNews

astrocytes sense diverse neurotransmitters and neuromodulators and, in turn, orchestrate regulation of neuroactive

August 2022 "The calcium-permeable cation channel TRPM3 can be activated by heat and the endogenous steroid pregnenolone sulfate. TRPM3's best understood function is its role as a peripheral noxious heat sensor in mice. However, the channel is expressed in various tissues and cell types including neurons as well as glial and epithelial cells. TRPM3 expression patterns differ between species and change during development. Furthermore, a plethora of TRPM3 variants that result from alternative splicing have been identified and the majority of these isoforms are yet to be characterized. Moreover, the mechanisms underlying regulation of TRPM3 are largely unexplored. In addition, a micro-RNA gene (miR-204) is located within the TRPM3 gene. This complexity makes it difficult to obtain a clear picture of TRPM3 characteristics. However, a clear picture is needed to unravel TRPM3's full potential as experimental tool, diagnostic marker and therapeutic target. Therefore, the newest data related to TRPM3 have to be discussed and to be put in context as soon as possible to be up-to-date and to accelerate the translation from bench to bedside. The aim of this review is to highlight recent results and developments with particular focus on findings from studies involving ocular tissues and cells or peripheral neurons of rodents and humans." Read more at the source #DrGPCR #GPCR #IndustryNews

Relating to pain, RGS4 in pain regulation is a topic of increasing interest because it has been identified G-Protein Signaling (RGS) Protein Modulation of Opioid Receptor Signaling as a Potential Target for Pain Front Mol Neurosci, 2020. 13: p. 5. https://pubmed.ncbi.nlm.nih.gov/32038168/ 3. Avrampou, K., et al., RGS4 Maintains Chronic Pain Symptoms in Rodent Models. J Neurosci, 2019. 39(42): p. 8291-8304. https://pubmed.ncbi.nlm.nih.gov/31308097/ 8.

The activation of these pathways regulates pain modulation, memory consolidation, motor coordination neuroprotective functions and is now being investigated for its role in Parkinson’s disease and neuropathic pain Of the traditional GPCRs, CBRs are gaining ground as potential therapeutic targets in several CNS diseases Their integration into drug discovery neuroscience workflows helps accelerate GPCR target identification

Watch Episode 166 Pain management is broken. And Benjamin Clements is on a mission to fix it. us through how positive allosteric modulators (PAMs) targeting the mu-opioid receptor could preserve pain In fact, one of their recent neuroma pain studies showed a tenfold increase in methadone potency. That’s huge.” – Ben Clements By combining chronic pain models with receptor-level pharmacology, Ben Beyond Acute Pain: Into the Chronic Unknown Opioids work well for acute pain. Chronic pain?

Opioids are analgesic drugs consumed non-medically for euphoric feelings and medically for pain relief most important in regulating the response to nociception, i.e. the response of the nervous system to painful Given their pathophysiological significance in pain, addiction and depression opioid receptors represent Complex Persistent Opioid Dependence-an Opioid-induced Chronic Pain Syndrome. Front Mol Neurosci. 2022 Jun 15;15:919773. doi: 10.3389/fnmol.2022.919773.

But Sokhom Pin stayed loyal to GPCRs , even when big pharma turned its gaze to other targets like kinases “Companies started shutting down neuroscience and GPCR programs. But I stayed,” Sokhom said. receptor research at Alkermes and early-stage work at Cerevel and Superluminal, Sokhom’s consistency has paid

GPCR Podcast : From Personal Pain to Scientific Purpose: Alex Serafini’s Journey We sit down with Dr. Serafini’s early struggles with chronic pain sparked a career focused on innovating where pain management His work challenges outdated targets, explores overlooked roles of GPCRs and RGS proteins in pain, and Redefine your playbook:  Why Serafini believes that pain research needs to start from clinical phenotype Explore blind spots:  The underestimated role of GPCRs and RGS proteins in chronic pain mechanisms.

that contains various adhesion-related domains and a highly-conserved GPCR-autoproteolysis-inducing (GAIN The cleavage appears to occur at an atypical GPCR proteolysis site within the GAIN domain during an early

GPCRs in Neuroscience Photopharmacological manipulation of amygdala metabotropic glutamate receptor mGlu4 alleviates neuropathic pain. GPCRs in Oncology and Immunology Pan-cancer functional analysis of somatic mutations in G protein-coupled

studies reveal how phosphorylation barcodes shape arrestin engagement, a biased NTSR1 modulator targets pain Barcodes Shape Arrestin Engagement with ACKR3   A β-Arrestin-2-Biased NTSR1 Modulator for Non-Addictive Pain

GPCRs in Neuroscience PACAP key interactions with PAC1, VPAC1, and VPAC2 identified by molecular dynamics Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides sustained pain relief.

GPCRs in Neuroscience Arrestin-dependent nuclear export of phosphodiesterase 4D promotes GPCR-induced Therapeutic potential of opioid receptor heteromers in chronic pain and associated comorbidities. Investigating the potential of GalR2 as a drug target for neuropathic pain.

Don't miss this fantastic opportunity to gain valuable knowledge and prepare for the forthcoming sessions Ligand-Dependent and G Protein-Dependent Properties for the Sweet Taste Heterodimer, TAS1R2/1R3 GPCRs in Neuroscience Therapeutic Targets for the Treatment of Neurological Disease s Activation of GPR55 alleviates neuropathic pain

Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   GPCR Activation and Signaling A gain identifies 14-3-3 proteins as regulating the availability of signaling-competent receptors GPCRs in Neuroscience

GPCRs in Neuroscience Fine-tuning GPCR-mediated neuromodulation by biasing signaling through different Multi-omics integration analysis of GPCRs in pan-cancer to uncover inter-omics relationships and potential Function Identification of a potential structure-based GPCR drug for interstitial cystitis/bladder pain

reveals the critical role of GPR110 in palmitic acid-stimulated milk protein and fat synthesis GPCRs in Neuroscience Targeting sensory neuron GPCRs for peripheral neuropathic pain GPCRs in Oncology and Immunology Expression prevalence and dynamics of GPCR somatostatin receptors 2 and 3 as cancer biomarkers beyond NET: a paired

]decane-2,4-dione Derivatives as a Novel Delta Opioid Receptor-Selective Agonist Chemotype GPCRs in Neuroscience metamorphosis and spawning behavior in Pacific abalone The role of orphan G protein-coupled receptors in pain