Targeting gatekeeper mutations for kinase drug discovery
Y Zhou, S Xiang, F Yang, X Lu - Journal of medicinal chemistry, 2022 - ACS Publications
Clinically acquired resistance is a major challenge in cancer therapies with small-molecule
kinase inhibitors (SMKIs). Gatekeeper mutations in the ATP-binding pocket of kinases are …
kinase inhibitors (SMKIs). Gatekeeper mutations in the ATP-binding pocket of kinases are …
Role of protein phosphorylation in cell signaling, disease, and the intervention therapy
K Pang, W Wang, JX Qin, ZD Shi, L Hao, YY Ma… - MedComm, 2022 - Wiley Online Library
Protein phosphorylation is an important post‐transcriptional modification involving an
extremely wide range of intracellular signaling transduction pathways, making it an …
extremely wide range of intracellular signaling transduction pathways, making it an …
Sporadic medullary thyroid carcinoma: towards a precision medicine
A Matrone, C Gambale, A Prete, R Elisei - Frontiers in endocrinology, 2022 - frontiersin.org
Medullary thyroid carcinoma (MTC) is a neuroendocrine malignant tumor originating from
parafollicular C-cells producing calcitonin. Most of cases (75%) are sporadic while the …
parafollicular C-cells producing calcitonin. Most of cases (75%) are sporadic while the …
Precision oncology for RET-related tumors
A Verrienti, G Grani, M Sponziello, V Pecce… - Frontiers in …, 2022 - frontiersin.org
Aberrant activation of the RET proto-oncogene is implicated in a plethora of cancers. RET
gain-of-function point mutations are driver events in multiple endocrine neoplasia 2 (MEN2) …
gain-of-function point mutations are driver events in multiple endocrine neoplasia 2 (MEN2) …
Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations
ZX Wang, QQ Li, J Cai, JZ Wu, JJ Wang… - Journal of Medicinal …, 2024 - ACS Publications
Over the past decades, the role of rearranged during transfection (RET) alterations in
tumorigenesis has been firmly established. RET kinase inhibition is an essential therapeutic …
tumorigenesis has been firmly established. RET kinase inhibition is an essential therapeutic …
Approved small-molecule ATP-competitive kinases drugs containing indole/azaindole/oxindole scaffolds: R&D and binding patterns profiling
H Zhang, F He, G Gao, S Lu, Q Wei, H Hu, Z Wu… - Molecules, 2023 - mdpi.com
Kinases are among the most important families of biomolecules and play an essential role in
the regulation of cell proliferation, apoptosis, metabolism, and other critical physiological …
the regulation of cell proliferation, apoptosis, metabolism, and other critical physiological …
Synthetic Approaches to Piperazine-Containing Drugs Approved by FDA in the Period of 2011–2023
MN Romanelli, L Braconi, A Gabellini, D Manetti… - Molecules, 2023 - mdpi.com
The piperazine moiety is often found in drugs or in bioactive molecules. This widespread
presence is due to different possible roles depending on the position in the molecule and on …
presence is due to different possible roles depending on the position in the molecule and on …
YAP Regulates HER3 Signaling–Driven Adaptive Resistance to RET Inhibitors in RET-Aberrant Cancers
Y Katayama, T Yamada, K Tanimura… - Clinical Cancer …, 2024 - aacrjournals.org
Purpose: Rearranged during transfection (RET) aberrations represent a targetable
oncogene in several tumor types, with RET inhibitors displaying marked efficacy. However …
oncogene in several tumor types, with RET inhibitors displaying marked efficacy. However …
Novel therapeutic strategies for rare mutations in non-small cell lung cancer
Q Gou, Q Gou, X Gan, Y Xie - Scientific Reports, 2024 - nature.com
Lung cancer is still the leading cause of cancer-related mortality. Over the past two decades,
the management of non-small cell lung cancer (NSCLC) has undergone a significant …
the management of non-small cell lung cancer (NSCLC) has undergone a significant …
Insights into pralsetinib resistance to the non-gatekeeper RET kinase G810C mutation through molecular dynamics simulations
S Cao, C Tan, A Fei, G Hu, M Fu, J Lv - Journal of Molecular Modeling, 2023 - Springer
Objective RET (rearranged during transfection) kinase, as a transmembrane receptor
tyrosine kinase, is a therapeutic target for several human cancer such as non-small cell lung …
tyrosine kinase, is a therapeutic target for several human cancer such as non-small cell lung …