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Published in Valerio Voliani, Nanomaterials and Neoplasms, 2021
Eun-Kyung Lim, Taekhoon Kim, Soonmyung Paik, Seungjoo Haam, Yong-Min Huh, Kwangyeol Lee
Since then, other targeting agents, including mAbs and the new tyrosine kinase inhibitors (TKI), were then developed using recombinant technology to avoid immune rejection and directly target molecular abnormalities on certain types of cancer, instead of interfering DNA. There has been steady clinical progress with targeted therapies used alone or in combination with conventional therapies, finding new indications in many tumor types, including cancers previously considered untreatable [385]. These targeted therapies aim to further increase the anticancer drugs while reducing their toxicity. The extracellular domain of cell surface receptors plays an important role in the physiological regulation, i.e., proliferation, differentiation, and survival of epithelial cells [386, 387]. The relevance of these receptors in the oncogenesis of epithelial cancers is significant, and hence, they are ideal targets for antibody therapies [202, 206, 388, 389]. On the other hand, the intracellular kinase domain can be targeted by small-molecule drugs.
Metal-free domino amination-Knoevenagel condensation approach to access new coumarins as potent nanomolar inhibitors of VEGFR-2 and EGFR
Published in Green Chemistry Letters and Reviews, 2021
Essam M. Eliwa, Marcel Frese, Ahmed H. Halawa, Maha M. Soltan, Larissa V. Ponomareva, Jon S. Thorson, Khaled A. Shaaban, Mohamed Shaaban, Ahmed M. El-Agrody, Norbert Sewald
Cancer remains one of the most daunting diseases to treat, thus, the development of new antitumor agents is still a very critical research domain. Amongst the attractive therapeutic targets for cancer, protein tyrosine kinases (PTKs) that regulate the biological potency of proteins by phosphorylation process that play a crucial role in signal transduction mechanisms by which inter-cellular signals regulate significance intra-cellular functions such as ion transport, cellular proliferation, differentiation, angiogenesis, and hormone responses. Among them, the epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR) are receptor protein tyrosine kinases (RPTKs) that overexpressed or mutated in several tumors due to a mutation of a normal gene to an oncogene [1]. EGFR (a dimer of HER-1 and HER-2) and VEGFR-2 (KDR, a type of VEGFRs) are pro-angiogenic growth factor receptors that induce angiogenesis process in order to establish new blood vessels that have an important role in tumor growth and metastasis; therefore, they are attractive therapy targets and dominant strategy for the treatment of cancer [1-6].
How combination therapies shape drug resistance in heterogeneous tumoral populations
Published in Letters in Biomathematics, 2018
E. Piretto, M. Delitala, M. Ferraro
This type of cancer shows resistance to several therapies. One of the most clinically effective treatment involves the use of a small-molecule tyrosine kinase inhibitor (TKIs) Erlotinib (Pao et al., 2004). Erlotinib is an orally active selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (Shepherd et al., 2005), whose mutation appears in 70% of patients with NSCLC. This drug is part of the more general class of molecular target therapies.