Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - Signal transduction and …, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

Protein tyrosine kinase inhibitor resistance in malignant tumors: molecular mechanisms and future perspective

Y Yang, S Li, Y Wang, Y Zhao, Q Li - Signal transduction and targeted …, 2022 - nature.com
Protein tyrosine kinases (PTKs) are a class of proteins with tyrosine kinase activity that
phosphorylate tyrosine residues of critical molecules in signaling pathways. Their basal …

Poziotinib for EGFR exon 20-mutant NSCLC: Clinical efficacy, resistance mechanisms, and impact of insertion location on drug sensitivity

YY Elamin, JP Robichaux, BW Carter, M Altan, H Tran… - Cancer Cell, 2022 - cell.com
We report a phase II study of 50 advanced non-small cell lung cancer (NSCLC) patients with
point mutations or insertions in EGFR exon 20 treated with poziotinib (NCT03066206). The …

Structure and dynamics of the EGFR/HER2 heterodimer

X Bai, P Sun, X Wang, C Long, S Liao, S Dang… - Cell Discovery, 2023 - nature.com
HER2 belongs to the human epidermal growth factor receptor tyrosine kinase family. Its
overexpression or hyperactivation is a leading cause for multiple types of cancers. HER2 …

Diverse rescue potencies of p53 mutations to ATO are predetermined by intrinsic mutational properties

H Song, J Wu, Y Tang, Y Dai, X Xiang, Y Li… - Science Translational …, 2023 - science.org
Tumor suppressor p53 is inactivated by thousands of heterogeneous mutations in cancer,
but their individual druggability remains largely elusive. Here, we evaluated 800 common …

[HTML][HTML] UNcommon EGFR mutations: international case series on efficacy of osimertinib in real-life practice in first-LiNe setting (UNICORN)

J Bar, N Peled, S Schokrpur, M Wolner, O Rotem… - Journal of thoracic …, 2023 - Elsevier
Introduction Approximately 10% of EGFR mutations (EGFRmuts) are uncommon
(ucEGFRmuts). We aimed to collect real-world data about osimertinib for patients with …

[HTML][HTML] Treatment outcome of atypical EGFR mutations in the German national network genomic medicine lung cancer (nNGM)

M Janning, J Süptitz, C Albers-Leischner, P Delpy… - Annals of oncology, 2022 - Elsevier
Background Atypical EGFR mutations occur in 10%-30% of non-small-cell lung cancer
(NSCLC) patients with EGFR mutations and their sensitivity to classical epidermal growth …

[HTML][HTML] Predicting gene mutation status via artificial intelligence technologies based on multimodal integration (MMI) to advance precision oncology

J Shao, J Ma, Q Zhang, W Li, C Wang - Seminars in cancer biology, 2023 - Elsevier
Personalized treatment strategies for cancer frequently rely on the detection of genetic
alterations which are determined by molecular biology assays. Historically, these processes …

MoDAFold: a strategy for predicting the structure of missense mutant protein based on AlphaFold2 and molecular dynamics

L Zheng, S Shi, X Sun, M Lu, Y Liao… - Briefings in …, 2024 - academic.oup.com
Protein structure prediction is a longstanding issue crucial for identifying new drug targets
and providing a mechanistic understanding of protein functions. To enhance the progress in …

Omics-based deep learning approaches for lung cancer decision-making and therapeutics development

TO Tran, TH Vo, NQK Le - Briefings in Functional Genomics, 2024 - academic.oup.com
Lung cancer has been the most common and the leading cause of cancer deaths globally.
Besides clinicopathological observations and traditional molecular tests, the advent of …