[HTML][HTML] Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

L Zhong, Y Li, L Xiong, W Wang, M Wu… - Signal transduction and …, 2021 - nature.com
Due to the advantages in efficacy and safety compared with traditional chemotherapy drugs,
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …

Mechanistic insight into ALK receptor tyrosine kinase in human cancer biology

B Hallberg, RH Palmer - Nature Reviews Cancer, 2013 - nature.com
The burgeoning field of anaplastic lymphoma kinase (ALK) in cancer encompasses many
cancer types, from very rare cancers to the more prevalent non-small-cell lung cancer …

Structural mechanism of a drug-binding process involving a large conformational change of the protein target

P Ayaz, A Lyczek, YT Paung, VR Mingione… - Nature …, 2023 - nature.com
Proteins often undergo large conformational changes when binding small molecules, but
atomic-level descriptions of such events have been elusive. Here, we report unguided …

Conformational states dynamically populated by a kinase determine its function

T Xie, T Saleh, P Rossi, CG Kalodimos - Science, 2020 - science.org
INTRODUCTION Protein kinases mediate many cell signaling processes. Central to their
physiological function is the regulation of their binding and enzymatic activities, which is …

Mechanisms of acquired crizotinib resistance in ALK-rearranged lung cancers

R Katayama, AT Shaw, TM Khan… - Science translational …, 2012 - science.org
Most anaplastic lymphoma kinase (ALK)–positive non–small cell lung cancers (NSCLCs)
are highly responsive to treatment with ALK tyrosine kinase inhibitors (TKIs). However …

Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia

CC Smith, Q Wang, CS Chin, S Salerno, LE Damon… - Nature, 2012 - nature.com
Effective targeted cancer therapeutic development depends upon distinguishing disease-
associated 'driver'mutations, which have causative roles in malignancy pathogenesis, from …

Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling

N Wagle, C Emery, MF Berger, MJ Davis… - Journal of clinical …, 2011 - ascopubs.org
A detailed understanding of the mechanisms by which tumors acquire resistance to targeted
anticancer agents should speed the development of treatment strategies with lasting clinical …

[HTML][HTML] EGFR Mutation and Resistance of Non–Small-Cell Lung Cancer to Gefitinib

S Kobayashi, TJ Boggon, T Dayaram… - … England Journal of …, 2005 - Mass Medical Soc
Mutations of the epidermal growth factor receptor (EGFR) gene have been identified in
specimens from patients with non–small-cell lung cancer who have a response to …

Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF

PTC Wan, MJ Garnett, SM Roe, S Lee… - Cell, 2004 - cell.com
Over 30 mutations of the B-RAF gene associated with human cancers have been identified,
the majority of which are located within the kinase domain. Here we show that of 22 B-RAF …

Chronic myeloid leukemia: an update of concepts and management recommendations of European LeukemiaNet

M Baccarani, J Cortes, F Pane… - Journal of clinical …, 2009 - ascopubs.org
Purpose To review and update the European LeukemiaNet (ELN) recommendations for the
management of chronic myeloid leukemia with imatinib and second-generation tyrosine …