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GENE:

HTR2A (5-Hydroxytryptamine Receptor 2A)

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Other names: HTR2A, 5-Hydroxytryptamine Receptor 2A, 5-HT2A, HTR2, 5-Hydroxytryptamine (Serotonin) Receptor 2A, G Protein-Coupled, 5-Hydroxytryptamine (Serotonin) Receptor 2A, Serotonin 5-HT-2A Receptor, Serotonin Receptor 2A, 5-HT2 Receptor, 5-HT-2A, 5-HT-2
Associations
Trials
3ms
Impact of pesticide diazinon on gastric cancer cell lines and the alteration of cholinergic and serotonergic pathway genes affecting cell proliferation. (PubMed, Sci Rep)
Collectively, these data indicate that submicromolar DZN promotes proliferation and suppresses apoptosis of GC cells by perturbing neuronal signaling networks. Our findings provide novel evidence linking environmental OP exposure to dysregulated neurotransmitter pathways in gastric carcinogenesis and highlight neuronal signaling components as potential therapeutic or preventive targets.
Preclinical • Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • PCNA (Proliferating cell nuclear antigen) • CHRM3 (Cholinergic Receptor Muscarinic 3) • SLC6A4 (Solute Carrier Family 6 Member 4) • HTR2A (5-Hydroxytryptamine Receptor 2A)
3ms
Integrating machine learning and molecular dynamics simulation to decipher the molecular network of dioxin-associated liposarcoma. (PubMed, Sci Rep)
The selective HTR2A receptor antagonist ketanserin has the potential to alleviate this toxicological impact. Our study presents an efficient, cost-effective toxicological analysis using network toxicology, offering new insights into dioxin-associated liposarcoma.
Journal
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CDH3 (Cadherin 3) • MMP14 (Matrix Metallopeptidase 14) • ADORA2B (Adenosine A2b Receptor) • HTR2A (5-Hydroxytryptamine Receptor 2A)
6ms
Repurposing terfenadine and domperidone for inhibition of apoptotic gene association in colorectal cancer: A system pharmacology approach integrated with molecular docking, MD simulations, and post-MD simulation analysis. (PubMed, Bioinform Biol Insights)
In conclusion, this integrative computational analysis highlights terfenadine and domperidone as promising candidates capable of modulating key apoptotic pathways in CRC. The findings provide a strong rationale for subsequent in vitro and in vivo studies to validate their therapeutic potential and facilitate clinical translation in CRC management.
Journal
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EGFR (Epidermal growth factor receptor) • DRD2 (Dopamine Receptor D2) • SLC6A4 (Solute Carrier Family 6 Member 4) • HTR2A (5-Hydroxytryptamine Receptor 2A)
8ms
Serotonin receptor 5-HT2A as a potential target for HCC immunotherapy. (PubMed, J Immunother Cancer)
Together, our data describe a role for 5-HT2A as a negative regulator of the cytotoxic effector phenotype in CD8 T cells and highlight the therapeutic potential of targeting 5-HT2A for HCC immunotherapy.
Journal • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • GZMB (Granzyme B) • HTR2A (5-Hydroxytryptamine Receptor 2A)
9ms
Integrating network pharmacology and experimental validation to reveal the anti-growth mechanism of panaxadiol against glioblastoma via calcium signaling. (PubMed, Front Mol Biosci)
Furthermore, we conducted experiments in vitro and in vivo experiments, which encompassed CCK-8, colony formation, flow cytometry apoptosis, intracellular calcium ion measurement, and xenograft tumor experiments utilizing nude mice, to validate the function of Panaxadiol in suppressing the growth of GBM via the modulation of calcium ion levels. This study not only revealed the anti-GBM mechanisms of Panaxadiol through network pharmacology but also validated its inhibitory effects on GBM via calcium ion release through in vitro and in vivo experiments.
Journal
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GRM1 (Glutamate Metabotropic Receptor 1) • GRIN2B (Glutamate Ionotropic Receptor NMDA Type Subunit 2B) • HTR2A (5-Hydroxytryptamine Receptor 2A)
11ms
Repurposing serotonergic drugs for gastric cancer: induction of apoptosis in vitro. (PubMed, Mol Biol Rep)
This study highlights the potential of Tropisetron, Imipramine, Ketanserin, and Cyproheptadine as repurposed drugs for gastric cancer therapy, with Tropisetron and Imipramine showing particularly promising apoptotic effects. These findings pave the way for further preclinical and clinical investigations, offering a foundation for personalized therapeutic strategies in gastric cancer management.
Preclinical • Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • PCNA (Proliferating cell nuclear antigen) • ANXA5 (Annexin A5) • SLC6A4 (Solute Carrier Family 6 Member 4) • HTR2A (5-Hydroxytryptamine Receptor 2A) • HTR2B (5-Hydroxytryptamine Receptor 2B)
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imipramine
1year
Synthesis and Biological Evaluation of Peripheral HTR2A Antagonists for Colorectal Cancer. (PubMed, J Med Chem)
15f induced sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells via the activation of p53/p21/caspase 3 signaling. In vivo treatment with 15f led to a marked delay in tumor growth in a colorectal cancer model in a dose-dependent manner.
Journal
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CASP3 (Caspase 3) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • HTR2A (5-Hydroxytryptamine Receptor 2A)
1year
Identification of Goat Supernumerary Teat Phenotype Using Wide-Genomic Copy Number Variants. (PubMed, Animals (Basel))
These genes include LOC102185621, LOC102190481, and UDP-glucose pyrophosphorylase 2, which potentially affect the occurrence of BC through multiple biological processes, such as cell detoxification, glycogen synthesis, and phospholipid metabolism. In conclusion, we discovered numerous genes related to mammary development and breast cancer (BC) through a GWS, which suggests the mechanism of SNTs in goats and a certain association between mammary cancer and SNTs.
Journal
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CEBPA (CCAAT Enhancer Binding Protein Alpha) • MCM3 (Minichromosome maintenance complex component 3) • RBM4 (RNA Binding Motif Protein 4) • HTR2A (5-Hydroxytryptamine Receptor 2A)
over1year
Polypharmacological profiling across protein target families and cellular pathways using the multiplexed cell-based assay platform safetyProfiler reveals efficacy, potency and side effects of drugs. (PubMed, Biomed Pharmacother)
For example, the neuroleptics clozapine, paliperidone, and risperidone potently inhibited primary targets DRD2 and HTR2A as well as cAMP and calcium pathways...Additionally, precise potency data for LY2452473, an androgen receptor antagonist, that completed a phase 2 clinical trial for prostate cancer, are presented. The non-selective kinase inhibitor staurosporine was observed to potently inactivate the two RTKs EGFR and ERBB4 as well as MAPK signaling, while eliciting stress-related cAMP responses. Our findings underscore the value of comprehensive profiling in elucidating the pharmacological properties of established and novel therapeutics, thereby facilitating the development of novel multi-target drugs with enhanced efficacy and selectivity.
Journal • Adverse events
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EGFR (Epidermal growth factor receptor) • ERBB4 (erb-b2 receptor tyrosine kinase 4) • DRD2 (Dopamine Receptor D2) • HTR2A (5-Hydroxytryptamine Receptor 2A)
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OPK 88004
over1year
Exploring Candidate Gene Studies and Alexithymia: A Systematic Review. (PubMed, Genes (Basel))
The results of this study showed that only case-control gene studies have been performed in alexithymia. On the basis of our findings, the majority of alexithymia genes and polymorphisms in this study belong to the serotoninergic pathway and neurotransmitter metabolism genes. These data suggest a role of serotoninergic neurotransmission in alexithymia. Nevertheless, more and future research is required to learn about the role of these genes in alexithymia.
Review • Journal
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BDNF (Brain Derived Neurotrophic Factor) • DRD2 (Dopamine Receptor D2) • SLC6A4 (Solute Carrier Family 6 Member 4) • COMT (Catechol-O-Methyltransferase) • HTR2A (5-Hydroxytryptamine Receptor 2A)
almost2years
Desloratadine ameliorates paclitaxel-induced peripheral neuropathy and hypersensitivity reactions in mice. (PubMed, Acta Pharmacol Sin)
A recommended anti-allergic agent diphenhydramine (DIP) has been used to alleviate PTX-induced HSR. DLT inhibited astrocytic NLRP3 inflammasome activation-mediated spinal neuronal damage through 5HTR2A/c-FOS pathway. Our findings have supported that spinal 5HTR2A inhibition shows promise as a therapeutic strategy for PIPN and highlighted the potential advantage of DLT as a dual-functional agent in preventing against PTX-induced both PIPN and HSR effects in anticancer chemotherapy.
Preclinical • Journal
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NLRP3 (NLR Family Pyrin Domain Containing 3) • FOS (Fos Proto-Oncogene AP-1 Transcription Factor Subunit 2) • HTR2A (5-Hydroxytryptamine Receptor 2A)
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paclitaxel
almost2years
Pain, Central Sensitization and Psychoemotional State in Patients With Chronic Masticatory Muscle Pain (clinicaltrials.gov)
P=N/A, N=102, Enrolling by invitation, Wroclaw Medical University | Not yet recruiting --> Enrolling by invitation | Trial completion date: Jan 2025 --> Dec 2025 | Trial primary completion date: Jan 2024 --> Dec 2024
Enrollment open • Trial completion date • Trial primary completion date
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HTR2A (5-Hydroxytryptamine Receptor 2A)