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Published in 2021 at "Scientific Reports"
DOI: 10.1038/s41598-021-96817-3
Abstract: P21-activated kinases (PAKs) are serine/threonine protein kinase which have six different isoforms (PAK1–6). Of those, PAK1 is overexpressed in many cancers and considered to be a major chemotherapeutic target. Most of the developed PAK1 inhibitor…
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Keywords:
novel allosteric;
inhibitor;
ester ketorolac;
triazolyl ester ... See more keywords
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Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-1176
Abstract: SHP2 is a non-receptor protein tyrosine phosphatase downstream of receptor tyrosine kinases (RTK). Mutations yielding constitutive activation of SHP2 primarily lead to activation of the MAPK pathway and have been found in multiple tumor types.…
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Keywords:
novel allosteric;
shp2;
allosteric shp2;
shp2 inhibitors ... See more keywords
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Published in 2019 at "PLoS ONE"
DOI: 10.1371/journal.pone.0211227
Abstract: Trypanosoma cruzi is the causative agent of Chagas disease, a neglected infection affecting millions of people in tropical regions. There are several chemotherapeutic agents for the treatment of this disease, but most of them are…
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Keywords:
novel allosteric;
allosteric inhibitors;
site;
allosteric mechanism ... See more keywords
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Published in 2020 at "Journal of Medicinal Chemistry"
DOI: 10.2210/pdb6p4v/pdb
Abstract: Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor 5A (eIF5A). Hypusine is essential for...
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Keywords:
discovery novel;
novel allosteric;
inhibitors deoxyhypusine;
allosteric inhibitors ... See more keywords