Article (Scientific journals)
Tyrosine Kinase Inhibitors in Cancer: Breakthrough and Challenges of Targeted Therapy.
POTTIER, Charles; Fresnais, Margaux; Gilon, Marie et al.
2020In Cancers
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Keywords :
cancer; oncology; pharmacology; tyrosine kinase inhibitors
Abstract :
[en] Receptor tyrosine kinases (RTKs) are key regulatory signaling proteins governing cancer cell growth and metastasis. During the last two decades, several molecules targeting RTKs were used in oncology as a first or second line therapy in different types of cancer. However, their effectiveness is limited by the appearance of resistance or adverse effects. In this review, we summarize the main features of RTKs and their inhibitors (RTKIs), their current use in oncology, and mechanisms of resistance. We also describe the technological advances of artificial intelligence, chemoproteomics, and microfluidics in elaborating powerful strategies that could be used in providing more efficient and selective small molecules inhibitors of RTKs. Finally, we discuss the interest of therapeutic combination of different RTKIs or with other molecules for personalized treatments, and the challenge for effective combination with less toxic and off-target effects.
Disciplines :
Oncology
Author, co-author :
POTTIER, Charles ;  Centre Hospitalier Universitaire de Liège - CHU > Département de médecine interne > Service des maladies infectieuses - médecine interne
Fresnais, Margaux;  University Hospital of Heidelberg > Department of Clinical Pharmacology and Pharmacoepidemiology
Gilon, Marie ;  Université de Liège - ULiège > Master méd. (180 crédits)
JERUSALEM, Guy  ;  Centre Hospitalier Universitaire de Liège - CHU > Département de médecine interne > Service d'oncologie médicale
Longuespée, Rémi  ;  Université de Liège - ULiège > Département de chimie (sciences) > Chimie analytique inorganique
Sounni, Nor Eddine   ;  Université de Liège - ULiège > Cancer-Tumours and development biology
 These authors have contributed equally to this work.
Language :
English
Title :
Tyrosine Kinase Inhibitors in Cancer: Breakthrough and Challenges of Targeted Therapy.
Alternative titles :
[en] Inhibiteurs tyrosine kinase dans le cancer: percée et défis de la thérapie ciblée.
Publication date :
20 March 2020
Journal title :
Cancers
eISSN :
2072-6694
Publisher :
Multidisciplinary Digital Publishing Institute (MDPI), Switzerland
Special issue title :
Non-Canonical Kinases and Substrates in Cancer Progression
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
F.R.S.-FNRS - Fonds de la Recherche Scientifique [BE]
Available on ORBi :
since 14 June 2020

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