LSD1 as a Biomarker and the Outcome of Its Inhibitors in the Clinical Trial: The Therapy Opportunity in Tumor.
LSD1 as a Biomarker and the Outcome of Its Inhibitors in the Clinical Trial: The Therapy Opportunity in Tumor.
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LSD1 作为生物标志物及其抑制剂的临床试验结果：肿瘤的治疗机会
DOI：
10.1155/2021/5512524
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发表时间：
2021
影响因子：
--
通讯作者：
Liu HM
中科院分区：
文献类型：
--
作者：
Agboyibor C;Dong J;Effah CY;Drokow EK;Pervaiz W;Liu HM
肿瘤是全世界最主要的死亡原因。因此，在癌症的调查、治疗方法和良好的维护实践方面有了显著的提高。然而，很多肿瘤生物标志物的敏感性和特异性都不够。因此，寻找新的生物标志物来预测肿瘤的预后和治疗靶点具有重要意义。这篇综述描述了LSD1作为不同肿瘤的生物标志物。LSD1抑制剂的临床试验也进行了讨论。最近的模式主张LSD1参与与具有精确dna结合转录因子的多蛋白复合物连接的多染色质区，确立了LSD1作为一个有利的表观遗传靶点，也为治疗不同肿瘤提供了大量的治疗靶点选择。这篇综述有力地支持了LSD1在不同肿瘤中的致癌可能性，表明LSD1水平可用于监测和识别不同的肿瘤，并可作为肿瘤患者进展和公平诊断的有用生物标志物。临床试验表明，LSD1抑制剂的临床疗效越来越明显，这是非常令人鼓舞和有希望的。然而，对于一些抑制剂，如GSK2879552，虽然选择性、强效和有效，但其疾病控制较差，因为肿瘤患者的不良事件（ae）发生率高，导致临床试验终止，风险-收益分析无法支持继续。因此，我们建议，为了使LSD1抑制剂获得良好的临床效果，需要设计合适的给药方案，深入研究LSD1抑制剂的体外/体内机制，开发可逆、安全、有效和选择性的LSD1抑制剂，从而提供更安全的应用前景。
Tumors are the foremost cause of death worldwide. As a result of that, there has been a significant enhancement in the investigation, treatment methods, and good maintenance practices on cancer. However, the sensitivity and specificity of a lot of tumor biomarkers are not adequate. Hence, it is of inordinate significance to ascertain novel biomarkers to forecast the prognosis and therapy targets for tumors. This review characterized LSD1 as a biomarker in different tumors. LSD1 inhibitors in clinical trials were also discussed. The recent pattern advocates that LSD1 is engaged at sauce chromatin zones linking with complexes of multi-protein having an exact DNA-binding transcription factor, establishing LSD1 as a favorable epigenetic target, and also gives a large selection of therapeutic targets to treat different tumors. This review sturdily backing the oncogenic probable of LSD1 in different tumors indicated that LSD1 levels can be used to monitor and identify different tumors and can be a useful biomarker of progression and fair diagnosis in tumor patients. The clinical trials showed that inhibitors of LSD1 have growing evidence of clinical efficacy which is very encouraging and promising. However, for some of the inhibitors such as GSK2879552, though selective, potent, and effective, its disease control was poor as the rate of adverse events (AEs) was high in tumor patients causing clinical trial termination, and continuation could not be supported by the risk-benefit profile. Therefore, we propose that, to attain excellent clinical results of inhibitors of LSD1, much attention is required in designing appropriate dosing regimens, developing in-depth in vitro/in vivo mechanistic works of LSD1 inhibitors, and developing inhibitors of LSD1 that are reversible, safe, potent, and selective which may offer safer profiles.
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DOI：
10.1016/j.neo.2014.10.006
发表时间：
2014-12
期刊：
Neoplasia (New York, N.Y.)
影响因子：
--
作者：
Ferrari-Amorotti G;Chiodoni C;Shen F;Cattelani S;Soliera AR;Manzotti G;Grisendi G;Dominici M;Rivasi F;Colombo MP;Fatatis A;Calabretta B
通讯作者：
Calabretta B
影响因子：
64.5
作者：
Garcia-Bassets, Ivan;Kwon, Young-Soo;Rosenfeld, Michael G.
通讯作者：
Rosenfeld, Michael G.
影响因子：
11.2
作者：
Cho, Hyun-Soo;Suzuki, Takehiro;Hamamoto, Ryuji
通讯作者：
Hamamoto, Ryuji
影响因子：
50.3
作者：
Goardon, Nicolas;Marchi, Emanuele;Vyas, Paresh
通讯作者：
Vyas, Paresh
影响因子：
6.4
作者：
Hayami, Shinya;Kelly, John D.;Hamamoto, Ryuji
通讯作者：
Hamamoto, Ryuji