Targeting transcription factors in cancer—from undruggable to reality

JH Bushweller - Nature Reviews Cancer, 2019 - nature.com
Mutated or dysregulated transcription factors represent a unique class of drug targets that
mediate aberrant gene expression, including blockade of differentiation and cell death gene …

Tailor‐made amino acids and fluorinated motifs as prominent traits in modern pharmaceuticals

H Mei, J Han, S White, DJ Graham… - … A European Journal, 2020 - Wiley Online Library
Structural analysis of modern pharmaceutical practices allows for the identification of two
rapidly growing trends: the introduction of tailor‐made amino acids and the exploitation of …

Acquired resistance to the mutant-selective EGFR inhibitor AZD9291 is associated with increased dependence on RAS signaling in preclinical models

CA Eberlein, D Stetson, AA Markovets, KJ Al-Kadhimi… - Cancer research, 2015 - AACR
Resistance to targeted EGFR inhibitors is likely to develop in EGFR-mutant lung cancers.
Early identification of innate or acquired resistance mechanisms to these agents is essential …

Curcumin overcome primary gefitinib resistance in non-small-cell lung cancer cells through inducing autophagy-related cell death

P Chen, HP Huang, Y Wang, J Jin, WG Long… - Journal of Experimental …, 2019 - Springer
Background Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are
being wildly used as target therapy in non-small-cell lung cancer (NSCLC). However …

Application of single-cell RNA sequencing in optimizing a combinatorial therapeutic strategy in metastatic renal cell carcinoma

KT Kim, HW Lee, HO Lee, HJ Song, DE Jeong, S Shin… - Genome biology, 2016 - Springer
Background Intratumoral heterogeneity hampers the success of marker-based anticancer
treatment because the targeted therapy may eliminate a specific subpopulation of tumor …

Targeted therapies for treatment of non‐small cell lung cancer—recent advances and future perspectives

J Minguet, KH Smith, P Bramlage - International journal of …, 2016 - Wiley Online Library
Non‐small cell lung cancer (NSCLC) is one of the most deadly cancers worldwide, with poor
prognosis once the disease has progressed past the point at which surgery is a viable …

A review of HER4 (ErbB4) kinase, its impact on cancer, and its inhibitors

MI El-Gamal, NH Mewafi, NE Abdelmotteleb… - Molecules, 2021 - mdpi.com
HER4 is a receptor tyrosine kinase that is required for the evolution of normal body systems
such as cardiovascular, nervous, and endocrine systems, especially the mammary glands. It …

FDA- and EMA-Approved Tyrosine Kinase Inhibitors in Advanced EGFR-Mutated Non-Small Cell Lung Cancer: Safety, Tolerability, Plasma Concentration Monitoring …

I Solassol, F Pinguet, X Quantin - Biomolecules, 2019 - mdpi.com
Non-small-cell lung cancer (NSCLC) is the most common form of primary lung cancer. The
discovery of several oncogenic driver mutations in patients with NSCLC has allowed the …

Kinetics and thermodynamics of reversible thiol additions to mono-and diactivated Michael acceptors: implications for the design of drugs that bind covalently to …

EH Krenske, RC Petter, KN Houk - The Journal of Organic …, 2016 - ACS Publications
Additions of cysteine thiols to Michael acceptors underpin the mechanism of action of
several covalent drugs (eg, afatinib, osimertinib, ibrutinib, neratinib, and CC-292) …

Current and future molecular testing in NSCLC, what can we expect from new sequencing technologies?

S Garinet, P Laurent-Puig, H Blons… - Journal of clinical …, 2018 - mdpi.com
Recent changes in lung cancer care, including new approvals in first line and the
introduction of high-throughput molecular technologies in routine testing led us to question …