Histone methyltransferase and drug resistance in cancers
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(2020) 39:173
REVIEW
Open Access
Histone methyltransferase and drug resistance in cancers Cheng Yang1,2, Jiayu Zhang1,2, Yukui Ma3, Chunfu Wu1,2, Wei Cui1* and Lihui Wang1,2*
Abstract A number of novel anticancer drugs have been developed in recent years. However, the mortality of cancer patients remains high because of the emergence of drug resistance. It was reported that drug resistance might involved in changes in gene expression without changing genotypes, which is similar to epigenetic modification. Some studies indicated that targeting histone methyltransferase can reverse drug resistance. Hence, the use of histone methyltransferase inhibitors or histone demethylase inhibitors opens new therapeutic approaches for cancer treatment. While the relationship between histone methyltransferase and tumor resistance has been determined, there is a lack of updated review on the association between them. In this review, we summarized the mechanisms of histone methyltransferases in cancer drug resistance and the therapeutic strategies of targeting histone methyltransferase to reverse drug resistance. Keywords: Drug resistance, Cancer, Histone methyltransferase, Therapeutic strategy
Background Epigenetics is a branch of biology and its concept was proposed by a British biologist named Conrad Waddington in 1939 [1, 2]. “Epigenetics” is refered to the inheritable changes of gene expression without alteration in DNA sequence [3]. With the expansion of the field of epigenetics, epigenetic modifications is divided into DNA methylation, histone methylation and acetylation according to the location and type of modifications [4]. It has been suggested that epigenetic modification is closely associated with cancer development [5, 6]. Histone methylation, which can be reversibly modified, has received a lot of attention. Histone methylation depends on histone methyltransferases (HMTs) in cells, which can reversibly methylate specific residues of histones, thereby regulating gene expression [4]. In recent years, a number of evidence have shown that regulation of
* Correspondence: [email protected]; [email protected] 1 Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang, People’s Republic of China Full list of author information is available at the end of the article
HMTs can affect various biological characteristics of tumors [7, 8]. Cancer treatment is still challenging worldwide. Although new therapeutic drugs are being developed, such as tyrosine kinase inhibitors (TKIs), immune checkpoint inhibitors and epigenetic inhibitors [9], and these new drugs have achieved good therapeutic effects within a period of time, drug resistance might develop after initial use. Therefore, in addition to the continuous development of new drugs, solving the problem of drug resistance remains critical for cancer treatment. Recently, many experimental results have proved that histone methylase inhibitors can reverse drug resistance [10]. In this review, we describe the relationship between various types of HMTs and th
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