更新于：2024-11-01

A3R x COX-2

更新于：2024-11-01

基本信息

关联

项与 A3R x COX-2 相关的药物

Cannabinoid-COX-2

靶点

A3R x COX-2

作用机制

A3R激动剂 [+1]

在研机构

Enveric Biosciences, Inc.

原研机构

Enveric Biosciences, Inc.

在研适应症

关节疾病

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期1800-01-20

100 项与 A3R x COX-2 相关的临床结果

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100 项与 A3R x COX-2 相关的转化医学

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0 项与 A3R x COX-2 相关的专利（医药）

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项与 A3R x COX-2 相关的文献（医药）

2021-11-01·Computers in Biology and Medicine3区 · 工程技术

Effects of Bacille Calmette Guerin (BCG) vaccination during COVID-19 infection

3区 · 工程技术

Article

作者: Azad, A K M ; Islam, M Babul ; Faruqe, Md Omar ; Shoombuatong, Watshara ; Mehedy, Md ; Ahmad, Shamim ; Chowdhury, Utpala Nanda ; Moni, Mohammad Ali

The coronavirus disease 2019 (COVID-19) is caused by the infection of highly contagious severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), also known as the novel coronavirus. In most countries, the containment of this virus spread is not controlled, which is driving the pandemic towards a more difficult phase. In this study, we investigated the impact of the Bacille Calmette Guerin (BCG) vaccination on the severity and mortality of COVID-19 by performing transcriptomic analyses of SARS-CoV-2 infected and BCG vaccinated samples in peripheral blood mononuclear cells (PBMC). A set of common differentially expressed genes (DEGs) were identified and seeded into their functional enrichment analyses via Gene Ontology (GO)-based functional terms and pre-annotated molecular pathways databases, and their Protein-Protein Interaction (PPI) network analysis. We further analysed the regulatory elements, possible comorbidities and putative drug candidates for COVID-19 patients who have not been BCG-vaccinated. Differential expression analyses of both BCG-vaccinated and COVID-19 infected samples identified 62 shared DEGs indicating their discordant expression pattern in their respected conditions compared to control. Next, PPI analysis of those DEGs revealed 10 hub genes, namely ITGB2, CXCL8, CXCL1, CCR2, IFNG, CCL4, PTGS2, ADORA3, TLR5 and CD33. Functional enrichment analyses found significantly enriched pathways/GO terms including cytokine activities, lysosome, IL-17 signalling pathway, TNF-signalling pathways. Moreover, a set of identified TFs, miRNAs and potential drug molecules were further investigated to assess their biological involvements in COVID-19 and their therapeutic possibilities. Findings showed significant genetic interactions between BCG vaccination and SARS-CoV-2 infection, suggesting an interesting prospect of the BCG vaccine in relation to the COVID-19 pandemic. We hope it may potentially trigger further research on this critical phenomenon to combat COVID-19 spread.

2015-10-01·Vascular Pharmacology3区 · 医学

Mechanisms underlying uridine adenosine tetraphosphate-induced vascular contraction in mouse aorta: Role of thromboxane and purinergic receptors

3区 · 医学

Article

作者: Tilley, Stephen L ; Sun, Changyan ; Mustafa, S Jamal ; Zhou, Zhichao

Uridine adenosine tetraphosphate (Up4A), a novel endothelium-derived vasoactive agent, is proposed to play a role in cardiovascular disorders and induces aortic contraction through activation of cyclooxygenases (COXs). We and others demonstrated that activation of A1 or A3 adenosine receptors (ARs) results in vascular contraction via thromboxane (TX) A2 production. However, the mechanisms of Up4A-induced vascular contraction in mouse aorta are not understood. We hypothesize that Up4A-induced aortic contraction is through COX-derived TXA2 production, which requires activation of A1 and/or A3AR. Concentration responses to Up4A were conducted in isolated aorta. The TXB2 production, a metabolite of TXA2, was also measured. Up4A (10(-9)-10(-5)M) produced a concentration-dependent contraction >70%, which was markedly attenuated by COX and COX1 but not by COX2 inhibition. Notably, Up4A-induced aortic contraction was blunted by both TX synthase inhibitor ozagrel and TXA2 receptor (TP) antagonist SQ29548. Surprisingly, A3AR deletion had no effect on Up4A-induced contraction. Moreover, A1AR deletion or antagonism as well as A1/A3AR deletion potentiated Up4A-induced aortic contraction, suggesting a vasodilator influence of A1AR. In contrast, non-selective purinergic P2 receptor antagonist PPADS significantly blunted Up4A-induced aortic contraction to a similar extent as selective P2X1R antagonist MRS2159, the latter of which was further reduced by addition of ozagrel. Endothelial denudation almost fully attenuated Up4A-induced contraction. Furthermore, Up4A (3μM) increased TXB2 formation, which was inhibited by either MRS2159 or ozagrel. In conclusion, Up4A-induced aortic contraction depends on activation of TX synthase and TP, which partially requires the activation of P2X1R but not A1 or A3AR through an endothelium-dependent mechanism.

2014-03-01·Radiation and Environmental Biophysics4区 · 环境科学与生态学

Agonist of the adenosine A3 receptor, IB-MECA, and inhibitor of cyclooxygenase-2, meloxicam, given alone or in a combination early after total body irradiation enhance survival of γ-irradiated mice

4区 · 环境科学与生态学

Article

作者: Michal Hofer ; Denisa Komůrková ; Milan Pospíšil ; Zuzana Hoferová ; Ladislav Dušek

There exists a requirement for drugs which would be useful in therapy of an acute radiation damage of a mammalian organism. The aim of the study was to evaluate survival parameters in mice exposed to a lethal γ-ray dose of 8.5 Gy and treated with single doses of an adenosine A(3) receptor agonist, IB-MECA, or a cyclooxygenase-2 (COX-2) inhibitor, meloxicam, administered alone or in a combination early after irradiation, i.e., 0.5 and 1 h post-irradiation, respectively. The assessed parameters were the mean survival time (MST) and the cumulative percentage 30-day survival (CPS). Administrations of single intraperitoneal doses of either IB-MECA 0.5 h post-irradiation or meloxicam 1 h post-irradiation resulted in statistically significant increases of MST in comparison with the control irradiated mice. Combined administration of IB-MECA and meloxicam was found to be the only treatment statistically enhancing the parameter of CPS and to lead to the most expressive increase in MST of the experimental mice. The findings add new knowledge on the action of an adenosine A3 receptor agonist and a COX-2 inhibitor in an irradiated mammalian organism and suggest the potential of both the investigated drugs in the treatment of the acute radiation damage.

项与 A3R x COX-2 相关的新闻（医药）

2024-03-19

·BioSpace

Enveric Biosciences Signs Non-Binding Term Sheets to Pursue the Exclusive Out-Licensing of New Chemical Entities for Pharmaceutical and Non-Pharmaceutical Applications in Joint Disease

Second biotechnology company to potentially out-license novel compounds from Enveric’s portfolio of assets with possible significant milestone payments and royalties CAMBRIDGE, Mass.--(BUSINESS WIRE)-- Enveric Biosciences (NASDAQ: ENVB) (“Enveric” or the “Company”), a biotechnology company dedicated to the development of novel neuroplastogenic small-molecule therapeutics for the treatment of depression, anxiety, and addiction disorders, is pleased to announce that it has signed two non-binding term sheets with an undisclosed biotechnology company to pursue the out-licensing of cannabinoid-COX-2 conjugate compounds for both pharmaceutical and non-pharmaceutical applications for treatment of joint diseases. The term sheets contemplate that, for all human and animal joint pathology, such as osteoarthritis, rheumatoid arthritis, and other joint pathology applications, the undisclosed licensee would assume responsibility for all future product development efforts and in return would receive exclusive, royalty-bearing global licenses to develop, market and sublicense the compounds. The compounds are new chemical entities that include cannabinoids in conjugate form with COX-2 inhibitors and cannabinoids in conjugate form with selected steroids. The pharmaceutical application term sheet provides that Enveric could be eligible to receive future development and sales milestone payments that in total could add up to approximately $61 million, assuming certain conditions are met, including receiving approval for the investigational new drug (IND) application and completing Phases I through III testing of the licensed product. Royalty rates could range from 2.5% up to 10% on future sales, depending on meeting certain sales criteria. The non-pharmaceutical application term sheet provides that Enveric could be eligible to receive future development and sales milestone payments, which in total could add up to approximately $21 million and with royalty rates ranging from 0.25% up to 7%, assuming certain conditions are met, including successful product development and commercial launch and on meeting certain sales criteria. Together, through the out-licensing of the two assets and meeting various development and sales milestones, Enveric could potentially receive milestone payments that total up to approximately $82 million. “We are pleased to announce that a second biotechnology company has stepped forward looking to join Enveric in moving some of the Company’s promising assets forward,” said Joseph Tucker, Ph.D., Director and CEO of Enveric. “We look forward to working with our partner, and we are confident in their leadership and capabilities to continue the development of these compounds for both pharmaceutical and non-pharmaceutical applications to advance joint disease treatment options for patients. Ultimately, we believe the definitive licensing agreements, once negotiated and finalized, could represent an excellent potential source of revenue for Enveric, and continue to demonstrate the value of Enveric’s extensive portfolio of assets.” About Enveric Biosciences Enveric Biosciences (NASDAQ: ENVB) is a biotechnology company dedicated to the development of novel neuroplastogenic small-molecule therapeutics for the treatment of depression, anxiety, and addiction disorders. Leveraging its unique discovery and development platform, Psybrary™, Enveric has created a robust intellectual property portfolio of new chemical entities for specific mental health indications. Enveric’s lead program, EB-003, is a first-in-class approach to the treatment of difficult-to-address mental health disorders designed to promote neuroplasticity without inducing hallucinations in the patient. Enveric is also developing EB-002, formerly EB-373, a next generation synthetic prodrug of the active metabolite, psilocin, being studied as a treatment of psychiatric disorders. Enveric is headquartered in Naples, FL with offices in Cambridge, MA and Calgary, AB Canada. For more information, please visit . Forward-Looking Statements This press release contains forward-looking statements and forward-looking information within the meaning of applicable securities laws. These statements relate to future events or future performance. All statements other than statements of historical fact may be forward-looking statements or information. Generally, forward-looking statements and information may be identified by the use of forward-looking terminology such as “plans,” “expects” or “does not expect,” “proposed,” “is expected,” “budgets,” “scheduled,” “estimates,” “forecasts,” “intends,” “anticipates” or “does not anticipate,” or “believes,” or variations of such words and phrases, or by the use of words or phrases which state that certain actions, events or results may, could, should, would, or might occur or be achieved. Forward-looking statements may include historical statements and statements regarding beliefs, plans, expectations, or intentions regarding the future and are based on the beliefs of management as well as assumptions made by and information currently available to management. Actual results could differ materially from those contemplated by the forward-looking statements as a result of certain factors, including, but not limited to, the ability of Enveric to: negotiate and finalize definitive agreements based on the any of its out-licensing term sheets, including the two identified herein, and perform pursuant to the terms thereof; carry out successful clinical programs in Australia; achieve the value creation contemplated by technical developments; avoid delays in planned clinical trials; establish that potential products are efficacious or safe in preclinical or clinical trials; establish or maintain collaborations for the development of therapeutic candidates; obtain appropriate or necessary governmental approvals to market potential products; obtain future funding for product development and working capital on commercially reasonable terms; scale-up manufacture of product candidates; respond to changes in the size and nature of competitors; hire and retain key executives and scientists; secure and enforce legal rights related to Enveric’s products, including patent protection; identify and pursue alternative routes to capture value from its research and development pipeline assets; continue as a going concern; and manage its future growth effectively. The two out-licensing term sheets identified herein are non-binding and may not result in definitive agreements or attainment of the licensing fees referenced therein. A discussion of these and other factors, including risks and uncertainties with respect to Enveric, is set forth in Enveric’s filings with the Securities and Exchange Commission, including Enveric’s Annual Report on Form 10-K and its Quarterly Reports on Form 10-Q. Enveric disclaims any intention or obligation to revise any forward-looking statements, whether as a result of new information, future events or otherwise, except as required by law. View source version on businesswire.com: Contacts Investor Relations Tiberend Strategic Advisors, Inc. Daniel Kontoh-Boateng (862) 213-1398 dboateng@tiberend.com Media Relations Tiberend Strategic Advisors, Inc. Casey McDonald (646) 577-8520 cmcdonald@tiberend.com Source: Enveric Biosciences View this news release online at:

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