Recent advancement in drug design and discovery of pyrazole biomolecules as cancer and inflammation therapeutics
Pyrazole, an important pharmacophore and a privileged scaffold of immense significance, is
a five-membered heterocyclic moiety with an extensive therapeutic profile, viz., anti …
a five-membered heterocyclic moiety with an extensive therapeutic profile, viz., anti …
The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer
V De Falco, F Carlomagno, H Li, M Santoro - Best practice & research …, 2017 - Elsevier
RET receptor tyrosine kinase acts as a mutated oncogenic driver in several human
malignancies and it is over-expressed in other cancers. Small molecule compounds with …
malignancies and it is over-expressed in other cancers. Small molecule compounds with …
Discovery of a first-in-class gut-restricted RET kinase inhibitor as a clinical candidate for the treatment of IBS
H Schenck Eidam, J Russell, K Raha… - ACS medicinal …, 2018 - ACS Publications
Abdominal pain and abnormal bowel habits represent major symptoms for irritable bowel
syndrome (IBS) patients that are not adequately managed. Although the etiology of IBS is …
syndrome (IBS) patients that are not adequately managed. Although the etiology of IBS is …
Recent advances in pain management: relevant protein kinases and their inhibitors
F Giraud, E Pereira, F Anizon, P Moreau - Molecules, 2021 - mdpi.com
The purpose of this review is to underline the protein kinases that have been established,
either in fundamental approach or clinical trials, as potential biological targets in pain …
either in fundamental approach or clinical trials, as potential biological targets in pain …
Recent developments of RET protein kinase inhibitors with diverse scaffolds as hinge binders
CC Jia, W Chen, ZL Feng, ZP Liu - Future Medicinal Chemistry, 2021 - Future Science
RET is a proto-oncogene encoding a receptor tyrosine kinase. RET regulates key aspects of
cellular proliferation, differentiation and survival. The activation of RET via gene fusions or …
cellular proliferation, differentiation and survival. The activation of RET via gene fusions or …
Novel targeted therapeutics for MEN2
S Redaelli, I Plaza-Menacho… - Endocrine-related …, 2018 - erc.bioscientifica.com
The rearranged during transfection (RET) proto-oncogene was recognized as the multiple
endocrine neoplasia type 2 (MEN2) causing gene in 1993. Since then, much effort has been …
endocrine neoplasia type 2 (MEN2) causing gene in 1993. Since then, much effort has been …
Design and Synthesis of Novel Thieno[3,2-c]quinoline Compounds with Antiproliferative Activity on RET-Dependent Medullary Thyroid Cancer Cells
RET kinase gain-of-function mutations represent the main cause of the high aggressiveness
and invasiveness of medullary thyroid cancer (MTC). The selective inhibition of the RET …
and invasiveness of medullary thyroid cancer (MTC). The selective inhibition of the RET …
1-Methyl-3-((4-(quinolin-4-yloxy) phenyl) amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during Transfection (RET) kinase inhibitors capable of …
Y Zhang, S Chan, R He, Y Liu, X Song, ZC Tu… - European Journal of …, 2022 - Elsevier
REarranged during Transfection (RET) is a validated target for anticancer drug discovery
and two selective RET inhibitors were approved by US FDA in 2020. However, acquired …
and two selective RET inhibitors were approved by US FDA in 2020. However, acquired …
Recent advances in transfer hydration of nitriles with amides or aldoximes
H Naka, A Naraoka - Tetrahedron letters, 2020 - Elsevier
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Molecular modelling studies on pyrazole derivatives for the design of potent rearranged during transfection kinase inhibitors
SP Bhujbal, S Keretsu, SJ Cho - Molecules, 2021 - mdpi.com
RET (rearranged during transfection) kinase, one of the receptor tyrosine kinases, plays a
crucial role in the development of the human nervous system. It is also involved in various …
crucial role in the development of the human nervous system. It is also involved in various …