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RRx-001, a first-in-class small molecule inhibitor of MYC and a downregulator of CD47, is an "erythrophagoimmunotherapeutic".RRx-001是一种一流的MYC小分子抑制剂和CD47下调剂,是一种“红细胞吞噬免疫疗法”。
Oncoimmunology. 2020 Apr 3;9(1):1746172. doi: 10.1080/2162402X.2020.1746172.
2
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Nrf2 activity as a potential biomarker for the pan-epigenetic anticancer agent, RRx-001.Nrf2活性作为泛表观遗传抗癌剂RRx-001的潜在生物标志物。
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本文引用的文献

1
RRx-001 protects normal tissues but not tumors via Nrf2 induction and Bcl-2 inhibition.RRx-001 通过诱导 Nrf2 和抑制 Bcl-2 来保护正常组织而不影响肿瘤。
J Cancer Res Clin Oncol. 2019 Aug;145(8):2045-2050. doi: 10.1007/s00432-019-02958-4. Epub 2019 Jun 27.
2
Magnetic resonance imaging of RRx-001 pharmacodynamics in preclinical tumors.RRx-001在临床前肿瘤中药效学的磁共振成像
Oncotarget. 2017 Jun 12;8(60):102511-102520. doi: 10.18632/oncotarget.18455. eCollection 2017 Nov 24.
3
NO and HNO donors, nitrones, and nitroxides: Past, present, and future.NO 和 HNO 供体、硝酮和氮氧自由基:过去、现在和未来。
Med Res Rev. 2018 Jul;38(4):1159-1187. doi: 10.1002/med.21461. Epub 2017 Nov 2.
4
The immunomodulatory anticancer agent, RRx-001, induces an interferon response through epigenetic induction of viral mimicry.免疫调节抗癌药物RRx-001通过病毒模拟的表观遗传诱导来引发干扰素反应。
Clin Epigenetics. 2017 Jan 19;9:4. doi: 10.1186/s13148-017-0312-z. eCollection 2017.
5
RRx-001: a systemically non-toxic M2-to-M1 macrophage stimulating and prosensitizing agent in Phase II clinical trials.RRx-001:一种正在进行II期临床试验的全身无毒的M2型巨噬细胞刺激和致敏剂。
Expert Opin Investig Drugs. 2017 Jan;26(1):109-119. doi: 10.1080/13543784.2017.1268600.
6
Targeting tumor hypoxia with the epigenetic anticancer agent, RRx-001: a superagonist of nitric oxide generation.用表观遗传抗癌剂RRx-001靶向肿瘤缺氧:一种一氧化氮生成的超级激动剂。
Med Oncol. 2016 Aug;33(8):85. doi: 10.1007/s12032-016-0798-9. Epub 2016 Jul 4.
7
RRx-001, an epigenetic-based radio- and chemosensitizer, has vascular normalizing effects on SCCVII and U87 tumors.RRx-001是一种基于表观遗传学的放射和化学增敏剂,对SCCVII和U87肿瘤具有血管正常化作用。
Clin Epigenetics. 2016 May 11;8:53. doi: 10.1186/s13148-016-0220-7. eCollection 2016.
8
NO to cancer: The complex and multifaceted role of nitric oxide and the epigenetic nitric oxide donor, RRx-001.对癌症说“不”:一氧化氮及表观遗传一氧化氮供体RRx-001的复杂多面作用
Redox Biol. 2015 Dec;6:1-8. doi: 10.1016/j.redox.2015.07.002. Epub 2015 Jul 2.
9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.RRx-001 新型抗癌药物的临床前代谢和处置研究。
Drug Metab Dispos. 2012 Sep;40(9):1810-6. doi: 10.1124/dmd.112.046755. Epub 2012 Jun 14.

RRx-001是一种一流的MYC小分子抑制剂和CD47下调剂,是一种“红细胞吞噬免疫疗法”。

RRx-001, a first-in-class small molecule inhibitor of MYC and a downregulator of CD47, is an "erythrophagoimmunotherapeutic".

作者信息

Oronsky Bryan, Carter Corey A, Caroen Scott, Scribner Curtis, Oronsky Arnold, Reid Tony R

机构信息

Clinical and Scientific Department, EpicentRx, Inc, La Jolla, CA, USA.

Clinical and Scientific Department, InterWest Partners, Menlo Park, CA, USA.

出版信息

Oncoimmunology. 2020 Apr 3;9(1):1746172. doi: 10.1080/2162402X.2020.1746172.

DOI:10.1080/2162402X.2020.1746172
PMID:33457091
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7790525/
Abstract

The main mechanism of action of RRx-001, a pharmaceutically unprecedented Phase 3 small molecule that is derived from the aerospace industry, is clarified. RRx-001 has demonstrated anticancer activity through antiangiogenic, immune, epigenetic, antioxidant, apoptotic and nitric oxide (NO) pathways, resulting in its pleiomorphic description as an antiangiogenic/vascular normalizer.

摘要

RRx-001是一种源自航空航天工业的、前所未有的3期小分子药物,其主要作用机制已得到阐明。RRx-001已通过抗血管生成、免疫、表观遗传、抗氧化、凋亡和一氧化氮(NO)途径展现出抗癌活性,因此被多方面描述为一种抗血管生成/血管正常化药物。