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FGFR a promising druggable target in cancer: Molecular biology and new drugs.
Porta, Rut; Borea, Roberto; Coelho, Andreia; Khan, Shahanavaj; Araújo, António; Reclusa, Pablo; Franchina, Tindara; Van Der Steen, Nele; Van Dam, Peter; Ferri, Jose; Sirera, Rafael; Naing, Aung; Hong, David; Rolfo, Christian.
Afiliação
  • Porta R; Department of Medical Oncology, Catalan Institute of Oncology (ICO), Girona, Spain; Girona Biomedical Research Institute (IDIBGi), Girona, Spain; Department of Medical Sciences, School of Medicine, University of Girona, Girona, Spain.
  • Borea R; Phase I-Early Clinical Trials Unit, Oncology Department, Antwerp University Hospital (UZA) and Center for Oncological Research (CORE) Antwerp University, Edegem, Antwerp, Belgium(2).
  • Coelho A; Phase I-Early Clinical Trials Unit, Oncology Department, Antwerp University Hospital (UZA) and Center for Oncological Research (CORE) Antwerp University, Edegem, Antwerp, Belgium(2).
  • Khan S; Nanomedicine and Biotechnology Research Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
  • Araújo A; Department of Medical Oncology, Centro Hospitalar do Porto, Porto, Portugal.
  • Reclusa P; Phase I-Early Clinical Trials Unit, Oncology Department, Antwerp University Hospital (UZA) and Center for Oncological Research (CORE) Antwerp University, Edegem, Antwerp, Belgium(2).
  • Franchina T; Medical Oncology Unit A.O. Papardo & Department of Human Pathology, University of Messina, Messina, Italy.
  • Van Der Steen N; Center for Oncological Research (CORE), University of Antwerp, Wilrijk, Antwerp, Belgium; Department of Pathology, Antwerp University Hospital, Edegem, Antwerp, Belgium.
  • Van Dam P; Phase I-Early Clinical Trials Unit, Oncology Department, Antwerp University Hospital (UZA) and Center for Oncological Research (CORE) Antwerp University, Edegem, Antwerp, Belgium(2).
  • Ferri J; Phase I-Early Clinical Trials Unit, Oncology Department, Antwerp University Hospital (UZA) and Center for Oncological Research (CORE) Antwerp University, Edegem, Antwerp, Belgium(2).
  • Sirera R; Phase I-Early Clinical Trials Unit, Oncology Department, Antwerp University Hospital (UZA) and Center for Oncological Research (CORE) Antwerp University, Edegem, Antwerp, Belgium(2).
  • Naing A; Department of Investigational Cancer Therapeutics, MD Anderson Cancer Center, Houston, TX, USA.
  • Hong D; Department of Investigational Cancer Therapeutics, MD Anderson Cancer Center, Houston, TX, USA.
  • Rolfo C; Phase I-Early Clinical Trials Unit, Oncology Department, Antwerp University Hospital (UZA) and Center for Oncological Research (CORE) Antwerp University, Edegem, Antwerp, Belgium(2). Electronic address: christian.rolfo@uza.be.
Crit Rev Oncol Hematol ; 113: 256-267, 2017 May.
Article em En | MEDLINE | ID: mdl-28427515
ABSTRACT

INTRODUCTION:

The Fibroblast Growth Factor Receptor (FGFR) family consists of Tyrosine Kinase Receptors (TKR) involved in several biological functions. Recently, alterations of FGFR have been reported to be important for progression and development of several cancers. In this setting, different studies are trying to evaluate the efficacy of different therapies targeting FGFR. AREAS COVERED This review summarizes the current status of treatments targeting FGFR, focusing on the trials that are evaluating the FGFR profile as inclusion criteria Multi-Target, Pan-FGFR Inhibitors and anti-FGF (Fibroblast Growth Factor)/FGFR Monoclonal Antibodies. EXPERT OPINION Most of the TKR share intracellular signaling pathways; therefore, cancer cells tend to overcome the inhibition of one tyrosine kinase receptor by activating another. The future of TKI (Tyrosine Kinase Inhibitor) therapy will potentially come from multi-targeted TKIs that target different TKR simultaneously. It is crucial to understand the interaction of the FGF-FGFR axis with other known driver TKRs. Based on this, it is possible to develop therapeutic strategies targeting multiple connected TKRs at once. One correct step in this direction is the reassessment of multi target inhibitors considering the FGFR status of the tumor. Another opportunity arises from assessing the use of FGFR TKI on patients harboring FGFR alterations.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Receptores de Fatores de Crescimento de Fibroblastos / Inibidores de Proteínas Quinases / Neoplasias Limite: Humans Idioma: En Revista: Crit Rev Oncol Hematol Assunto da revista: HEMATOLOGIA / NEOPLASIAS Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Espanha

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Receptores de Fatores de Crescimento de Fibroblastos / Inibidores de Proteínas Quinases / Neoplasias Limite: Humans Idioma: En Revista: Crit Rev Oncol Hematol Assunto da revista: HEMATOLOGIA / NEOPLASIAS Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Espanha