Phenotypic Screening Approaches to Develop Aurora Kinase Inhibitors: Drug Discovery Perspectives

Frontiers in Oncology
Carlos MarugánMaría José Lallena

Abstract

Targeting mitotic regulators as a strategy to fight cancer implies the development of drugs against key proteins, such as Aurora-A and -B. Current drugs, which target mitosis through a general mechanism of action (stabilization/destabilization of microtubules), have several side effects (neutropenia, alopecia, and emesis). Pharmaceutical companies aim at avoiding these unwanted effects by generating improved and selective drugs that increase the quality of life of the patients. However, the development of these drugs is an ambitious task that involves testing thousands of compounds through biochemical and cell-based assays. In addition, molecules usually target complex biological processes, involving several proteins and different molecular pathways, further emphasizing the need for high-throughput screening techniques and multiplexing technologies in order to identify drugs with the desired phenotype. We will briefly describe two multiplexing technologies [high-content imaging (HCI) and flow cytometry] and two key processes for drug discovery research (assay development and validation) following our own published industry quality standards. We will further focus on HCI as a useful tool for phenotypic screening and will provide...Continue Reading

References

Nov 12, 1965·Science·M J Fulwyler
Mar 17, 2000·Science·J Drews
Oct 23, 2002·Genes to Cells : Devoted to Molecular & Cellular Mechanisms·Tomotoshi MarumotoHideyuki Saya
Aug 20, 2003·Molecular Biology of the Cell·Reiko HondaErich A Nigg
Nov 20, 2003·Nature Reviews. Molecular Cell Biology·Mar Carmena, William C Earnshaw
Jan 5, 2005·Nature Reviews. Cancer·Tomotoshi MarumotoHideyuki Saya
Mar 16, 2007·Proceedings of the National Academy of Sciences of the United States of America·Mark G ManfrediChristopher F Claiborne
Jan 8, 2010·Molecular Cancer Therapeutics·Toshiyasu ShimomuraYoshikazu Iwasawa
Apr 16, 2013·Current Opinion in Pharmacology·Elena Doménech, Marcos Malumbres
Sep 10, 2014·Expert Opinion on Therapeutic Targets·Marcos Malumbres, Ignacio Pérez de Castro
Sep 13, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Gaëlle Mariaule, Philippe Belmont

❮ Previous
Next ❯

Citations

Apr 26, 2017·Clinical Epigenetics·Sheraz Gul

❮ Previous
Next ❯

Methods Mentioned

BETA
flow cytometry
Assay

Software Mentioned

Acumen Explorer

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

Combinatorial Chemistry & High Throughput Screening
Fabio GasparriArturo Galvani
Cellular and Molecular Life Sciences : CMLS
Florian T UngerKerstin A David
Journal of Biomolecular Screening
Sandra FoxMichael Biros
© 2022 Meta ULC. All rights reserved