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Molecules 2018, 23(5), 1166; https://doi.org/10.3390/molecules23051166

Clinically Applicable Inhibitors Impacting Genome Stability

1
Discipline of Pathology, Lambe Institute for Translational Research, School of Medicine, National University of Ireland Galway, H91 YR71 Galway, Ireland
2
Discipline of Surgery, Lambe Institute for Translational Research, School of Medicine, National University of Ireland Galway, H91 YR71 Galway, Ireland
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Silvia Schenone
Received: 21 March 2018 / Revised: 27 April 2018 / Accepted: 1 May 2018 / Published: 13 May 2018
(This article belongs to the Special Issue Medicinal Chemistry in Europe)
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Abstract

Advances in technology have facilitated the molecular profiling (genomic and transcriptomic) of tumours, and has led to improved stratification of patients and the individualisation of treatment regimes. To fully realize the potential of truly personalised treatment options, we need targeted therapies that precisely disrupt the compensatory pathways identified by profiling which allow tumours to survive or gain resistance to treatments. Here, we discuss recent advances in novel therapies that impact the genome (chromosomes and chromatin), pathways targeted and the stage of the pathways targeted. The current state of research will be discussed, with a focus on compounds that have advanced into trials (clinical and pre-clinical). We will discuss inhibitors of specific DNA damage responses and other genome stability pathways, including those in development, which are likely to synergistically combine with current therapeutic options. Tumour profiling data, combined with the knowledge of new treatments that affect the regulation of essential tumour signalling pathways, is revealing fundamental insights into cancer progression and resistance mechanisms. This is the forefront of the next evolution of advanced oncology medicine that will ultimately lead to improved survival and may, one day, result in many cancers becoming chronic conditions, rather than fatal diseases. View Full-Text
Keywords: clustering; HR; NHEJ; clinical; trial; centrosome; amplification; chromatin; DSB; inhibitor clustering; HR; NHEJ; clinical; trial; centrosome; amplification; chromatin; DSB; inhibitor
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Prakash, A.; Garcia-Moreno, J.F.; Brown, J.A.L.; Bourke, E. Clinically Applicable Inhibitors Impacting Genome Stability. Molecules 2018, 23, 1166.

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