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Advantages and Disadvantages of Using Structural Information in the Development of Anti-Cancer Inhibitors

One of the benefits of structural information is that it helps in the determination of the best type of molecules to be used in the elaboration of the inhibitors. Thus, it is important to note that in anticancer discovery campaigns, various structural molecules are utilized during the starting points. One type of particles used is the artificial structures which are either naturally or chemically modified to suit the structural characteristics of the intended body organ. When using the artificial structures, the “rule of five,” which is an awareness framework is applied to determine the compatibility of the structures and the target body (Garrett-Mayer, 2010, p.97). Another merit of using structural information is that medics can determine the oral absorption rates of the compounds to be utilized in the development of the inhibitors. For example, compounds with more than 5-H bonds, more than 500g weight, and water/oil distribution ratio of over 5 are poor absorbers do not make ideal structural inhibitors.

Structural information has also been historically relied upon in the determination of the best natural products to be used in drug development.  Some of the experimented compounds include taxanes, vincas, cytosines, and camptothecins. In this respect, structural information has played a significant role in examining the nature of the natural structures when used as biological inhibitors. For example, it has been discovered that taxanes, which are naturally obtained from the bark of yew tree species are predisposed to exotic fungi (Wicki et al., 2015, p. 138). Besides, with the aid of structural information, some of the compounds that were traditionally used in anticancer inhibitor development are now employed in experimental analyses to discover new and more efficient drugs. Through bioengineering, scientists can develop anticancer inhibitors in the form of vaccines, which are made from a combination of proteins, peptides, and monoclonal antibodies (Lee et al., 2011, p.4). In cases where current screening programs are used to develop anticancer inhibitors, real-time structural information is employed in the generation of data and continuous monitoring of the effectiveness of the drugs. For example, the National Cancer Institute utilizes the COMPARE algorithm to contrast primary data with refined information to make rational drug discoveries.

The discovery of anticancer inhibitors also faces a myriad of challenges, one of them being the fact that some structures inhibit normal cell growth, deterring the functionality of the drugs. For example, the epidermal growth factor receptor (EGFR), which has mostly been linked to primary target when developing inhibitors for humans, has been discovered to have the minimal clinical advantage to the process (Gryder, Sodji, & Oyelere, 2012, p.2). Instead, some scholars suggest that the molecule inhibits the functionality of some drugs. Therefore, the molecule has been associated with the progression of tumors and the administration of inhibitors is limited by EGFR. Another compound that has been established to hinder therapeutic reactions in a human body is Ras, which is linked to the inhabitation of the GTPase pathway. Continued mutation of ras proteins results from the disintegration of the Ras molecule, an element that results in resistance of the cells anticancer inhibitors (Dempke & Heinemann, 2010, par 2). Another challenge encountered during anticancer inhibitor development is the acquisition of relevant and updated information on various structural bodies and their reactions to the proposed drugs. Thus, scientists have to continually develop a new base of knowledge to counter new cases of cancerous cells.

References

Dempke, WC. & Heinemann, V 2010, ‘Ras mutational status is a biomarker for resistance to EGFR inhibitors in colorectal carcinoma,’ Anticancer research, vol. 30, no. 11, pp.4673-4677.

Garrett-Mayer, E 2010, Principles of Anticancer Drug Development, Springer Science & Business Media, New York.

Gryder, BE., Sodji, QH. & Oyelere, AK 2012, ‘Targeted cancer therapy: giving histone deacetylase inhibitors all they need to succeed,’ Future medicinal chemistry, vol. 4, no. 4, pp.505-524.

Lee, S., Kim, Y., Sun, JM., La Choi, Y., Kim, JG., Shim, YM., Park, YH., Ahn, JS., Park, K., Han, JH. & Ahn, MJ 2011, ‘Molecular profiles of EGFR, K-ras, c-met, and FGFR in pulmonary pleomorphic carcinoma, a rare lung malignancy,’ Journal of cancer research and clinical oncology, vol. 137, no. 8, pp.1203-1211.

Wicki, A., Witzigmann, D., Balasubramanian, V. & Huwyler, J 2015, ‘Nanomedicine in cancer therapy: challenges, opportunities, and clinical applications,’ Journal of Controlled Release, vol. 200, pp.138-157.

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