Looking for new inhibitors for the Epidermial Growth Factor Receptor.

Looking for new inhibitors for the Epidermial Growth Factor Receptor.

Curr Top Med Chem. 2018 Mar 29;:

Authors: Concu R, Cordeiro MND

Abstract
Epidermial growth factor receptor (EGFR) is still the main target of the head and neck squamous cell cancer (HNSCC) because its overexpression has been detected in more than 90% of this type of cancer. This overexpression is usually linked with more aggressive disease, increased resistance to chemotherapy and radiotherapy, increased metastasis, inhibition of apoptosis, promotion of neoplastic angiogenesis, and, finally, poor prognosis and decreased survival. Due to this, is the main target in the search of new drugs and inhibitors candidates able to downturn this overexpression. Quantitative structure activity relationship (QSAR) is one of the most and widely used approach while looking for new and more active inhibitors drugs. In this contest, a lot of authors used this technique, combined with others, to find new drugs or enhance the activity of well-known inhibitors. In this paper, on one hand we will review the most important QSAR approaches developed in the last fifteen years, spacing from classical 1D approaches until more sophisticated 3D; the first paper is dated 2003 while the last one is from the 2017. On the other hand, we will present a completely new QSAR approach aimed at the prediction of new EGFR inhibitors drugs. The here presented model has been developed over a dataset consisting of more than 1000 compounds using various molecular descriptors calculated with the DRAGON 7.0© software.

PMID: 29595111 [PubMed - as supplied by publisher]

https://ift.tt/2J8KvBM