Looking for New Inhibitors for the Epidermal Growth Factor Receptor

• Tipo: Outra Publicação em Revista Científica Internacional
• Data: 2018

Autores

Riccardo Concu (Autor) FCUP; Natalia N D S Cordeiro (Autor) FCUP

Revista

Título: Current Topics in Medicinal Chemistry

Vol. 18

Páginas: 219-232

ISSN: 1568-0266

Editora: Bentham

Indexação

ISI Web of Knowledge - 7 Citações

Scopus - 7 Citações

Outras Informações

ID Authenticus: P-00Q-D6W

DOI: 10.2174/1568026618666180329123023

Abstract (EN): Epidermal 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 reason, the main target in the search of new drugs and inhibitors candidates is to downturn this overexpression. Quantitative Structure-Activity Relationship (QSAR) is one of the most widely used approaches 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 2017. On the other hand, we will present a completely new QSAR approach aimed at the prediction of new EGFR inhibitors drugs. The model presented here has been developed over a dataset consisting of more than 1000 compounds using various molecular descriptors calculated with the DRAGON 7.0 (c) software.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 14