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Receptor tyrosine kinases and downstream pathways as druggable targets for cancer treatment: the current arsenal of inhibitors

Overview of attention for article published in Molecular Cancer, February 2018
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Title
Receptor tyrosine kinases and downstream pathways as druggable targets for cancer treatment: the current arsenal of inhibitors
Published in
Molecular Cancer, February 2018
DOI 10.1186/s12943-018-0792-2
Pubmed ID
Authors

Wagner Ricardo Montor, Andrei Ronaldo Oliveira Silva Escartin Salas, Fabiana Henriques Machado de Melo

Abstract

Searching for targets that allow pharmacological inhibition of cell proliferation in over-proliferative states, such as cancer, leads us to finely understand the complex mechanisms orchestrating the perfect control of mitosis number, frequency and pace as well as the molecular arrangements that induce cells to enter functional quiescence and brings them back to cycling in specific conditions. Although the mechanisms regulating cell proliferation have been described several years ago, never before has so much light been shed over this machinery as during the last decade when therapy targets have been explored and molecules, either synthetic or in the form of antibodies with the potential of becoming cancer drugs were produced and adjusted for specific binding and function. Proteins containing tyrosine kinase domains, either membrane receptors or cytoplasmic molecules, plus the ones activated by those in downstream pathways, having tyrosine kinase domains or not, such as RAS which is a GTPase and serine/threonine kinases such as RAF, play crucial role in conducting proliferation information from cell surroundings to the nucleus where gene expression takes place. Tyrosine kinases phosphorylate tyrosine residues in an activating mode and are found in important growth factor receptors, such as for ligands from families collectively known as VEGF, PDGF and EGF, to name a few and in intracellular downstream molecules. They all play important roles in normal physiology and are commonly found mutated or overexpressed in neoplastic states. Our objective here is to present such kinases as druggable targets for cancer therapy, highlighting the ones for which the pharmacological arsenal is available, discussing specificity, resistance mechanisms and treatment alternatives in cases of resistance, plus listing potential targets that have not been successfully worked yet.

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The data shown below were collected from the profiles of 2 X users who shared this research output. Click here to find out more about how the information was compiled.
Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 100 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 100 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 15 15%
Student > Master 12 12%
Student > Bachelor 8 8%
Other 8 8%
Researcher 8 8%
Other 14 14%
Unknown 35 35%
Readers by discipline Count As %
Biochemistry, Genetics and Molecular Biology 22 22%
Medicine and Dentistry 12 12%
Agricultural and Biological Sciences 11 11%
Pharmacology, Toxicology and Pharmaceutical Science 7 7%
Immunology and Microbiology 3 3%
Other 10 10%
Unknown 35 35%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 12 May 2018.
All research outputs
#18,587,406
of 23,023,224 outputs
Outputs from Molecular Cancer
#1,298
of 1,732 outputs
Outputs of similar age
#256,884
of 330,824 outputs
Outputs of similar age from Molecular Cancer
#42
of 58 outputs
Altmetric has tracked 23,023,224 research outputs across all sources so far. This one is in the 11th percentile – i.e., 11% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,732 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 5.7. This one is in the 14th percentile – i.e., 14% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 330,824 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 11th percentile – i.e., 11% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 58 others from the same source and published within six weeks on either side of this one. This one is in the 13th percentile – i.e., 13% of its contemporaries scored the same or lower than it.