Globally approved EGFR inhibitors: Insights into their syntheses, target kinases, biological activities, receptor interactions, and metabolism

MAS Abourehab, AM Alqahtani, BGM Youssif… - Molecules, 2021 - mdpi.com
Targeting the EGFR with small-molecule inhibitors is a confirmed valid strategy in cancer
therapy. Since the FDA approval of the first EGFR-TKI, erlotinib, great efforts have been …

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 …

Precision Targeted Therapy with BLU-667 for RET-Driven Cancers

V Subbiah, JF Gainor, R Rahal, JD Brubaker, JL Kim… - Cancer discovery, 2018 - AACR
The receptor tyrosine kinase rearranged during transfection (RET) is an oncogenic driver
activated in multiple cancers, including non–small cell lung cancer (NSCLC), medullary …

Pathogenesis of cancers derived from thyroid follicular cells

JA Fagin, GP Krishnamoorthy, I Landa - Nature reviews Cancer, 2023 - nature.com
The genomic simplicity of differentiated cancers derived from thyroid follicular cells offers
unique insights into how oncogenic drivers impact tumour phenotype. Essentially, the main …

A comprehensive review of protein kinase inhibitors for cancer therapy

R Kannaiyan, D Mahadevan - Expert review of anticancer therapy, 2018 - Taylor & Francis
Introduction: Protein kinases are involved in various cellular functions. About 2% of the
human genome encodes for protein kinases. Dysregulation of protein kinases is implicated …

The importance of the RET gene in thyroid cancer and therapeutic implications

D Salvatore, M Santoro, M Schlumberger - Nature Reviews …, 2021 - nature.com
Since the discovery of the RET receptor tyrosine kinase in 1985, alterations of this protein
have been found in diverse thyroid cancer subtypes. RET gene rearrangements are …

Vandetanib in patients with locally advanced or metastatic medullary thyroid cancer: a randomized, double-blind phase III trial

SA Wells Jr, BG Robinson, RF Gagel… - Journal of clinical …, 2012 - ascopubs.org
Purpose There is no effective therapy for patients with advanced medullary thyroid
carcinoma (MTC). Vandetanib, a once-daily oral inhibitor of RET kinase, vascular …

State-of-the-Art Strategies for Targeting RET-Dependent Cancers

V Subbiah, D Yang, V Velcheti, A Drilon… - Journal of Clinical …, 2020 - ascopubs.org
Activating receptor tyrosine kinase RET (rarranged during transfection) gene alterations
have been identified as oncogenic in multiple malignancies. RET gene rearrangements …

A comprehensive overview of the role of the RET proto-oncogene in thyroid carcinoma

C Romei, R Ciampi, R Elisei - Nature Reviews Endocrinology, 2016 - nature.com
The rearranged during transfection (RET) proto-oncogene was identified in 1985 and, very
soon thereafter, a rearrangement named RET/PTC was discovered in papillary thyroid …

Vandetanib in patients with previously treated RET-rearranged advanced non-small-cell lung cancer (LURET): an open-label, multicentre phase 2 trial

K Yoh, T Seto, M Satouchi, M Nishio… - The Lancet …, 2017 - thelancet.com
Background RET rearrangements are rare oncogenic alterations in non-small-cell lung
cancer (NSCLC). Vandetanib is a multitargeted tyrosine kinase inhibitor exhibiting RET …