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Research update and opportunity of non-hormonal male contraception: Histone demethylase KDM5B-based targeting

With the continued increase in global human population, diverse contraception approaches have become increasingly essential, including non-hormonal male contraception. Non-hormonal approaches to contraception are very convenient; however, such options are limited because data regarding the identification and characterization of tissue/cell-specific targets and appropriate small molecule candidate contraceptives are lacking. Based on in-silico studies of genomics, transcriptomics, and proteomics, performed by mining datasets in PubMed, we first reviewed testis-, epididymis-, and germline cell-specific genes/proteins, with the aim of presenting evidence that many of these could become 'druggable' targets for the development of non-hormonal male contraceptives in the future. Although many hurdles remain before the successful therapeutic use of non-hormonal contraceptive, to facilitate this approach, we describe here the changing perspectives on several potential non-hormonal contraceptives (e.g. small molecules, plant extracts, etc.) that are under development; continued effort may yield marketable products. Further, we highlight specific enzymes within the histone lysine demethylase subfamily that play a central role in germ line regulation. In particular, we focused on several prospective candidate small-molecules suggested to interact with the catalytic domain of histone lysine demethylase KD

 

Comments:

It sounds like you're delving into an incredibly intricate and essential area of research regarding non-hormonal male contraceptives. Identifying tissue-specific targets and exploring potential small-molecule candidates is a significant step in advancing this field.

Mining genomics, transcriptomics, and proteomics datasets from sources like PubMed is a great approach to identifying potential targets. As you've mentioned, understanding specific genes/proteins in the testis, epididymis, and germline cells could pave the way for developing 'druggable' targets for non-hormonal contraceptives.

The focus on enzymes within the histone lysine demethylase subfamily and their role in germ line regulation is particularly intriguing. Manipulating these enzymes with prospective candidate small-molecules could be a promising avenue for male contraception.

There's no denying that hurdles exist, as with any pioneering field, but the potential for these approaches to yield viable, marketable products is exciting. Continual efforts and a changing perspective on non-hormonal contraceptives, including small molecules and plant extracts, could indeed bring about transformative developments.

Research into such areas not only offers hope for effective male contraceptives but also showcases the importance of interdisciplinary studies that merge genomics, transcriptomics, proteomics, and drug development. The application of in-silico studies to explore these potential avenues is a testament to the innovative approaches being taken in this field.

Related Products

Cat.No. Product Name Information
S0269 GSK467 GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. GSK467 shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members.

Related Targets

Histone Demethylase