近年来，该领域的研究工作已大大发展，以揭示表观遗传药物及其靶标的生物学和化学机制。同时，制药公司正在该领域进行重大投资。透明市场研究predictsthat the Epigenetic drugs and Diagnostic Technologies market will be worth an estimated $5.7 billion by 2018.
The ‘Epigenetic Drugs‘ series recently published inClinical Epigeneticsdelves deeper into this arena with reviews covering the current and upcoming areas of investigation and the challenges that are faced by researchers when developing these drugs.
While epigenetic drugs have primarily been studied for their use in treating cancer, the increasing funding efforts and interest have opened up avenues for researchers to pursue their use in Alzheimer’s, asthma and a myriad of other diseases. So what does the current landscape of epigenetic drugs look like?
Cancer
The main focus point of epi-drug research has been looking into their use in cancer treatment. There are two basic types of epigenetic drugs being tested for this purpose:
组蛋白脱乙酰基酶（HDAC）抑制剂通过抵消癌症对组蛋白的作用，从而导致肿瘤抑制基因功能降低的组蛋白。这些药物使染色质结构变得更加轻松，从而使这些基因的转录激活。
There are currently three HDAC inhibitors that have been approved by the FDA and they are all being used in the treatment of rare T cell lymphomas.
DNA-methylation (DNMT), inhibitors operate by preventing the addition of methyl groups to genes in cancer cells. This is effective as DNA methylation results in gene silencing in genes that reduce the speed of cell division, resulting in uncontrolled proliferation.
Two drugs that inhibit DNA methylation,azacitidine and decitabine, have been approved by the FDA and are being utilised in the treatment of blood cancer.
现在，人们对表观遗传因素如何在包括哮喘和COPD在内的几种慢性呼吸道疾病的发展中发挥作用有了更大的了解。
Respiratory diseases
现在，人们对表观遗传因素如何在包括哮喘和COPD在内的几种慢性呼吸道疾病的发展中发挥作用有了更大的了解。Several of these factors are also reversible, so they can be ideal targets for therapeutic intervention.
Aninitiativehas been started by MRC Technology and AstraZeneca to discover new epigenetic drug targets for respiratory diseases such as asthma and COPD. Their aim is to work with academics researching epigenetic mechanisms in this area to collaborate on creating novel small molecule drugs that can target the epigenetic pathways for these diseases.
Alzheimer’s disease
There are currently afew epigenetic drugsin development that target Alzheimer’s disease. These drugs aim to alter gene expression and target genes that are linked to learning and memory. Things are looking hopeful as the first Alzheimer’s related epigenetic drug, ORY-2001, has been in development since 2010 and entered a Phase 1 clinical trial this April.
It still remains to be seen if researchers will be able to uncover the epigenetic mechanisms of disease, to allow more of these treatment options to become a reality.
The future
那么，表观遗传药物的未来是什么样的，限制其进步的限制因素是什么？制药行业的巨额投资将允许研究扩展以在新领域开发治疗药物。但是，是否能够发现疾病的表观遗传机理，以使更多这些治疗选择成为现实仍然有待观察。
Find out more in theClinical Epigenetics‘Epigenetic Drugs‘ series.
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