Atropisomerism in the pharmaceutically relevant realm

M Basilaia, MH Chen, J Secka… - Accounts of Chemical …, 2022 - ACS Publications
Conspectus Atropisomerism is a conformational chirality that occurs when there is hindered
rotation about a σ-bond. While atropisomerism is exemplified by biaryls, it is observed in …

Targeting RET-driven cancers: lessons from evolving preclinical and clinical landscapes

A Drilon, ZI Hu, GGY Lai, DSW Tan - Nature reviews Clinical oncology, 2018 - nature.com
The gene encoding the receptor-tyrosine kinase RET was first discovered more than three
decades ago, and activating RET rearrangements and mutations have since been identified …

RET aberrant cancers and RET inhibitor therapies: current state-of-the-art and future perspectives

A Addeo, E Miranda-Morales, P den Hollander… - Pharmacology & …, 2023 - Elsevier
Precision oncology informed by genomic information has evolved in leaps and bounds over
the last decade. Although non-small cell lung cancer (NSCLC) has moved to center-stage as …

RET gene fusions in malignancies of the thyroid and other tissues

M Santoro, M Moccia, G Federico, F Carlomagno - Genes, 2020 - mdpi.com
Following the identification of the BCR-ABL1 (Breakpoint Cluster Region-ABelson murine
Leukemia) fusion in chronic myelogenous leukemia, gene fusions generating chimeric …

Mechanisms that drive inflammatory tumor microenvironment, tumor heterogeneity, and metastatic progression

L Yang, PC Lin - Seminars in cancer biology, 2017 - Elsevier
Abstract Treatment of cancer metastasis has been largely ineffective. It is paramount to
understand the mechanisms underlying the metastatic process, of which the tumor …

Receptor tyrosine kinases in osteosarcoma treatment: which is the key target?

Z Tian, X Niu, W Yao - Frontiers in Oncology, 2020 - frontiersin.org
Recent clinical trials have shown several multi-target tyrosine kinase inhibitors (TKIs) to be
effective in the treatment of osteosarcoma. However, these TKIs have a number of targets …

Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations

I Miyazaki, I Odintsov, K Ishida, AJW Lui, M Kato… - Nature Cancer, 2023 - nature.com
RET receptor tyrosine kinase is activated in various cancers (lung, thyroid, colon and
pancreatic, among others) through oncogenic fusions or gain-of-function single-nucleotide …

Molecular pathology of lung cancer: current status and perspectives

F Oberndorfer, L Müllauer - Current opinion in oncology, 2018 - journals.lww.com
The discoveries of cancer research have been translated into the clinical management of
lung cancer patients. So far, the approach of targeted therapy that is directed towards certain …

Androgen receptor antagonists for prostate cancer therapy

C Helsen, T Van den Broeck, A Voet… - Endocrine-related …, 2014 - erc.bioscientifica.com
Medullary thyroid carcinomas (MTC) arise from thyroid parafollicular, calcitonin-producing C-
cells and can occur either as sporadic or as hereditary diseases in the context of familial …

Role of RET protein-tyrosine kinase inhibitors in the treatment RET-driven thyroid and lung cancers

R Roskoski Jr, A Sadeghi-Nejad - Pharmacological Research, 2018 - Elsevier
RET is a transmembrane receptor protein-tyrosine kinase that is required for the
development of the nervous system and several other tissues. The mechanism of activation …