Comparative studies on the human serum albumin binding of the clinically approved EGFR inhibitors gefitinib, erlotinib, afatinib, osimertinib and the investigational …

O Dömötör, K Pelivan, A Borics, BK Keppler… - … of Pharmaceutical and …, 2018 - Elsevier
Binding interactions between human serum albumin (HSA) and four approved epidermal
growth factor receptor (EGFR) inhibitors gefitinib (GEF), erlotinib (ERL), afatinib (AFA) …

Interaction of an anticancer drug, gefitinib with human serum albumin: insights from fluorescence spectroscopy and computational modeling analysis

MZ Kabir, WV Tee, SB Mohamad, Z Alias, S Tayyab - RSC advances, 2016 - pubs.rsc.org
Binding of gefitinib (GEF), a promising anticancer drug to human serum albumin (HSA), the
major transport protein in blood circulation was investigated using fluorescence, UV-vis …

Probing the combination of erlotinib hydrochloride, an anticancer drug, and human serum albumin: Spectroscopic, molecular docking, and molecular dynamic …

S Shahraki, Z Razmara, HS Delarami… - …, 2023 - Wiley Online Library
Human serum albumin (HSA) is a globular and monomeric protein in plasma that transports
many drugs and compounds. Binding of some drugs to HSA can lead to changes in its …

[HTML][HTML] In vitro biodistribution studies on clinically approved FGFR inhibitors ponatinib, nintedanib, erlotinib and the investigational inhibitor KP2692

O Dömötör, M Mathuber, CR Kowol - European Journal of Pharmaceutical …, 2024 - Elsevier
Binding towards human serum albumin (HSA) and α1-acid glycoprotein (AGP) of three
approved fibroblast growth factor receptor (FGFR) inhibitors ponatinib (PON), nintedanib …

A spectroscopic study on the interaction between the anticancer drug erlotinib and human serum albumin

Z Ye, Y Ying, X Yang, Z Zheng, J Shi, Y Sun… - Journal of Inclusion …, 2014 - Springer
The interaction between erlotinib and human serum albumin (HSA) in simulated
physiological conditions was investigated by spectroscopic methods. The results revealed …

[HTML][HTML] Spectroscopic studies on the interaction between erlotinib hydrochloride and bovine serum albumin

F Rasoulzadeh, D Asgari, A Naseri… - DARU Journal of …, 2010 - ncbi.nlm.nih.gov
Methods The BSA solution (0.1 mM) was prepared daily in Tris buffer (0.05 mol l-1, pH= 7.4)
and treated at final concentration of 1.67× 10-5 M with different amounts of erlotinib …

[HTML][HTML] Biophysical and docking study on the interaction of anticancer drugs encorafenib and binimetinib with human serum albumin

G Cavalieri, G Cilurzo, L Pettorosso, A Mansueto… - European Journal of …, 2023 - Elsevier
The utilization of BRAF and MEK inhibitors in combination therapy has demonstrated
superior outcomes in the treatment of melanoma as compared to monotherapy. In the …

Binding of gefitinib, an inhibitor of epidermal growth factor receptor-tyrosine kinase, to plasma proteins and blood cells: in vitro and in cancer patients

J Li, J Brahmer, W Messersmith, M Hidalgo… - Investigational new …, 2006 - Springer
Gefitinib exhibits wide inter-subject pharmacokinetic variability which may contribute to
differences in treatment outcome. Unbound drug concentrations are believed to be more …

[HTML][HTML] A spectroscopic approach to investigate the molecular interactions between the newly approved irreversible ErbB blocker" Afatinib" and bovine serum …

AM Alanazi, AS Abdelhameed - PLoS One, 2016 - journals.plos.org
The interaction of afatinib (AFB) with bovine serum albumin (BSA) was examined via
fluorescence and UV-Vis spectroscopy. Spectrofluorimetric measurements revealed that …

Binding mechanism of kinase inhibitors to EGFR and T790M, L858R and L858R/T790M mutants through structural and energetic analysis

M Bello - International journal of biological macromolecules, 2018 - Elsevier
Experimental studies have demonstrated that L858R mutation in the EGF receptor (EGFR)
confers tumor sensitivity whereas T790M and L858R/T790M mutations cause resistance to …