Dataset Information

Targeting CDK6 in cancer: State of the art and new insights.

ABSTRACT: Cyclin-dependent kinase 6 (CDK6) plays a vital role in regulating the progression of the cell cycle. More recently, CDK6 has also been shown to have a transcriptional role in tumor angiogenesis. Up-regulated CDK6 activity is associated with the development of several types of cancers. While CDK6 is over-expressed in cancer cells, it has a low detectable level in non-cancerous cells and CDK6-null mice develop normally, suggesting a specific oncogenic role of CDK6, and that its inhibition may represent an ideal mechanism-based and low toxic therapeutic strategy in cancer treatment. Identification of selective small molecule inhibitors of CDK6 is thus needed for drug development. Herein, we review the latest understandings of the biological regulation and oncogenic roles of CDK6. The potential clinical relevance of CDK6 inhibition, the progress in the development of small-molecule CDK6 inhibitors and the rational design of potential selective CDK6 inhibitors are also discussed.

SUBMITTER: Tadesse S

PROVIDER: S-EPMC4825601 | biostudies-literature | 2015

REPOSITORIES: biostudies-literature

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Targeting CDK6 in cancer: State of the art and new insights.

Tadesse Solomon S Yu Mingfeng M Kumarasiri Malika M Le Bich Thuy BT Wang Shudong S

Cell cycle (Georgetown, Tex.) 20150101 20

Cyclin-dependent kinase 6 (CDK6) plays a vital role in regulating the progression of the cell cycle. More recently, CDK6 has also been shown to have a transcriptional role in tumor angiogenesis. Up-regulated CDK6 activity is associated with the development of several types of cancers. While CDK6 is over-expressed in cancer cells, it has a low detectable level in non-cancerous cells and CDK6-null mice develop normally, suggesting a specific oncogenic role of CDK6, and that its inhibition may repr ...[more]

PMID: 26315616

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Project description:The first hormonal contraceptive was introduced onto the market in several countries 50 years ago; however, the portfolio of contraceptive methods remains restricted with regards to their steroid composition, their cost, and their ability to satisfy the requirements of millions of women/couples in accordance with their different reproductive intentions, behaviors, cultures, and settings.A literature review was conducted using Medline, Embase, and Current Contents databases, up to September 1, 2013 to identify publications reporting new contraceptives in development using combinations of the search terms: contraception, contraceptives, oral contraceptives, patch, vaginal ring, implants, intrauterine contraceptives, and emergency contraception (EC). Also, several experts in the field were also consulted to document ongoing projects on contraception development. Additionally, the Clinicaltrial.gov website was searched for ongoing studies on existing contraceptive methods and new and emerging female contraceptives developed over the past 5 years. Information was also obtained from the pharmaceutical industry.Early sexual debut and late menopause means that women may require contraception for up to 30 years. Although oral, injectable, vaginal, transdermal, subdermal, and intrauterine contraceptives are already available, new contraceptives have been developed in an attempt to reduce side effects and avoid early discontinuation, and to fulfill women's different requirements. Research efforts are focused on replacing ethinyl-estradiol with natural estradiol to reduce thrombotic events. In addition, new, less androgenic progestins are being introduced and selective progesterone receptor modulators and new delivery systems are being used. In addition, research is being conducted into methods that offer dual protection (contraception and protection against human immunodeficiency virus transmission), and contraceptives for use "on demand." Studies are also investigating non-hormonal contraceptive methods that have additional, non-contraceptive benefits.The most pressing need worldwide is, first, that the highly effective contraceptive methods already available should be affordable to most of the population and also that these methods should fulfill the needs of women of different ages and with different reproductive requirements. The development of new contraceptive methods should also take advantage of the knowledge obtained over the past 30 years on gamete physiology and gamete interaction to avoid the use of steroid compounds.

Dataset Information

Targeting CDK6 in cancer: State of the art and new insights.

Publications

Targeting CDK6 in cancer: State of the art and new insights.

Similar Datasets

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