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Last update 23 Jan 2025

CACNG8

Last update 23 Jan 2025

Basic Info

Synonyms

CACNG6, CACNG8, calcium voltage-gated channel auxiliary subunit gamma 8

+ [4]

Introduction

Regulates the activity of L-type calcium channels that contain CACNA1C as pore-forming subunit (By similarity). Regulates the trafficking and gating properties of AMPA-selective glutamate receptors (AMPARs). Promotes their targeting to the cell membrane and synapses and modulates their gating properties by slowing their rates of activation, deactivation and desensitization and by mediating their resensitization. Does not show subunit-specific AMPA receptor regulation and regulates all AMPAR subunits.

Drugs associated with CACNG8

CERC-611

Target

CACNG8

Mechanism

CACNG8 inhibitors

Active Org.

ES Therapeutics Australia Pty Ltd

Originator Org.

Eli Lilly & Co. [+1]

Active Indication

Essential Tremor [+1]

Inactive Indication

Pain [+1]

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

RAP-219

Target

CACNG8

Mechanism

CACNG8 modulators

Active Org.

Rapport Therapeutics, Inc.Startup

Originator Org.

Rapport Therapeutics, Inc.Startup

Active Indication

Epilepsies, Partial [+2]

Inactive Indication-

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

11C-TARP-2105

Target

CACNG8

Mechanism

CACNG8 inhibitors

Active Org.

Southern University of Science & Technology [+2]

Originator Org.

The General Hospital Corp.

Active Indication

Central Nervous System Diseases

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with CACNG8

NCT06377930

/ RecruitingPhase 2

A Phase 2A, Multicenter, Open-label Study Evaluating the Safety and Efficacy of RAP-219 in Adult Participants With Refractory Focal Epilepsy

This is a clinical research study for an investigational drug called RAP-219 in patients with Refractory Focal Epilepsy. This study is being conducted to determine if RAP-219 works and is safe in patients with Refractory Focal Epilepsy.

Start Date10 Oct 2024

Sponsor / Collaborator

Rapport Therapeutics, Inc.Startup

CTIS2024-512151-21-00

/ Not yet recruitingPhase 1

- RAP-219-103

Start Date19 Jun 2024

Sponsor / Collaborator

Rapport Therapeutics, Inc.Startup

NCT05234762

/ RecruitingPhase 2

A Phase 2A, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy, Safety, and Pharmacokinetics of ES-481 in Adult Patients With Essential Tremors

This Pilot Phase 2A study will investigate the safety, tolerability, and pharmacokinetics (PK) of ES-481 in adult patients with essential tremor.

Start Date21 Nov 2021

Sponsor / Collaborator

ES Therapeutics Australia Pty Ltd

100 Clinical Results associated with CACNG8

100 Translational Medicine associated with CACNG8

0 Patents (Medical) associated with CACNG8

Literatures (Medical) associated with CACNG8

01 Feb 2025·American Journal of Hematology

Blood Plasma Methylated DNA Markers in the Detection of Lymphoma: Discovery, Validation, and Clinical Pilot

Article

Author: Katerov, Slava ; Graham, Rondell P. ; Novak, Anne J. ; Jevremovic, Dragan ; Burger, Kelli N. ; Berger, Calise K. ; Mahoney, Douglas W. ; O'Connell, Maria C. ; Taylor, William R. ; Cerhan, James R. ; Witzig, Thomas E. ; Dao, Linda N. ; Allawi, Hatim T. ; Foote, Patrick H. ; Kisiel, John B. ; Doering, Karen A. ; Hennek, Jacquelyn ; Bamlet, William R. ; Devens, Mary E. ; Arndt, Jacquelyn R.

ABSTRACTLymphoma is one of the leading causes of cancer and cancer deaths and yet has not been amenable to population screening. The role of methylated DNA markers (MDMs) in the detection of lymphoma has not been extensively studied. We aimed to discover, validate, and test tissue–derived MDMs of lymphoma in archival plasma specimens. Reduced representation bisulfite sequencing (RRBS) was performed on a discovery set of frozen tissues. MDMs identified were converted to methylation–specific PCR assays and validated on independent formalin–fixed, paraffin‐embedded (FFPE) tissues. Target enrichment long–probe quantitative‐amplified signal (TELQAS) assays were developed and assayed in plasma–extracted, bisulfite‐converted DNA from independent treatment‐naïve lymphoma patients and healthy controls. Prediction of cancer status was modeled using random forest model with in silico cross‐validation. After discovery and validation in tissue, 16 TELQAS assays (ZNF503, VWA5B1, HOXA9, GABRG3, ITGA5, MAX.chr17.7190, BNC1, CDK20, MAX.chr4.4069, TPBG, DNAH14, SYT6, CACNG8, FAM110B, ADRA1D, and NRN1) were selected for testing in plasma. These detected 78% (95% CI, 74%–82%) of lymphoma cases at 90% specificity. Excluding marginal zone and T‐cell lymphomas, sensitivity increased to 84% (80%–88%). MDMs in plasma show promise to detect lymphoma and are candidates for inclusion in multi‐cancer detection studies.

01 Jan 2025·Aging Cell

CaMKIIα‐TARPγ8 signaling mediates hippocampal synaptic impairment in aging

Article

Author: Chazot, Paul ; Ren, Xinyi ; JianHua, Zhao ; Hu, Qilin ; Du, Jingzhi ; Lu, Chengbiao ; Zhang, Ziyuan ; Donoghue, Peter ; Li, Songji ; Jiang, Sanwei ; Li, MingCan ; Yu, Yi ; Li, Junmei

AbstractAging‐related decline in memory and synaptic function are associated with the dysregulation of calcium homeostasis, attributed to the overexpression of voltage‐gated calcium channels (VGCC). The membrane insertion of AMPAR governed by the AMPAR auxiliary proteins is essential for synaptic transmission and plasticity (LTP). In this study, we demonstrated the hippocampal expression of the transmembrane AMPAR regulatory proteins γ‐8 (TARPγ8) was reduced in aged mice along with the reduced CaMKIIα activity and memory impairment. We further showed that TARPγ8 expression was dependent on CaMKIIα activity. Inhibition of CaMKIIα activity significantly reduced the hippocampal TARPγ8 expression and CA3‐CA1 LTP in young mice to a similar level to that of the aged mice. Furthermore, the knockdown of hippocampal TARPγ8 impaired LTP and memory in young mice, which mimicked the aging‐related changes. We confirmed the enhanced hippocampal VGCC (Cav‐1.3) expression in aged mice and found that inhibition of VGCC activity largely increased both p‐CaMKIIα and TARPγ8 expression in aged mice, whereas inhibition of NMDAR or Calpains had no effect. In addition, we found that the exogenous expression of human TARPγ8 in the hippocampus in aged mice restored LTP and memory function. Collectively, these results indicate that the synaptic and cognitive impairment in aging is associated with the downregulation of CaMKIIα‐TARPγ8 signaling caused by VGCC activation. Our results suggest that TARPγ8 may be a key molecular biomarker for brain aging and that boosting CaMKIIα‐TARPγ8 signaling may be critical for the restoration of synaptic plasticity of aging and aging‐related diseases.

19 Sep 2024·Cells

Cannabinol (CBN) Influences the Ion Channels and Synaptic-Related Genes in NSC-34 Cell Line: A Transcriptomic Study.

Article

Author: Trainito, Alessandra ; Gugliandolo, Agnese ; D'Angiolini, Simone ; Salamone, Stefano ; Muscarà, Claudia ; Mazzon, Emanuela ; Chiricosta, Luigi ; Pollastro, Federica

Neurological disorders such as Alzheimer's, Parkinson's, amyotrophic lateral sclerosis, and schizophrenia are associated with altered neuronal excitability, resulting from dysfunctions in the molecular architecture and physiological regulation of ion channels and synaptic transmission. Ion channels and synapses are regarded as suitable therapeutic targets in modern pharmacology. Cannabinoids have received great attention as an original therapeutic approach for their effects on human health due to their ability to modulate the neurotransmitter release through interaction with the endocannabinoid system. In our study, we explored the effect of cannabinol (CBN) through next-generation sequencing analysis of NSC-34 cell physiology. Our findings revealed that CBN strongly influences the ontologies related to ion channels and synapse activity at all doses tested. Specifically, the genes coding for calcium and potassium voltage-gated channel subunits, and the glutamatergic and GABAergic receptors (Cacna1b, Cacna1h, Cacng8, Kcnc3, Kcnd1, Kcnd2, Kcnj4, Grik5, Grik1, Slc17a7, Gabra5), were up-regulated. Conversely, the genes involved into serotoninergic and cholinergic pathways (Htr3a, Htr3b, Htr1b, Chrna3, Chrnb2, Chrnb4), were down-regulated. These findings highlight the influence of CBN in the expression of genes involved into ion influx and synaptic transmission.

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