The rearranged during transfection (RET) proto-oncogene was recognized as the multiple endocrine neoplasia type 2 (MEN2) causing gene in 1993. Since then, much effort has been put into a clear understanding of its oncogenic signaling, its biochemical function and ways to block its aberrant activation in MEN2 and related cancers. Several small molecules have been designed, developed or redirected as RET inhibitors for the treatment of MEN2 and sporadic MTC. However, current drugs are mostly active against several other kinases, as they were not originally developed for RET. This limits efficacy and poses safety issues. Therefore, there is still much to do to improve targeted MEN2 treatments. New, more potent and selective molecules, or combinatorial strategies may lead to more effective therapies in the near future. Here, we review the rationale for RET targeting in MEN2, the use of currently available drugs and novel preclinical and clinical RET inhibitor candidates.
Redaelli, S., Plaza-Menacho, I., & Mologni, L. (2018). Novel targeted therapeutics for MEN2. ENDOCRINE-RELATED CANCER, 25(2), T53-T68 [10.1530/ERC-17-0297].
|Citazione:||Redaelli, S., Plaza-Menacho, I., & Mologni, L. (2018). Novel targeted therapeutics for MEN2. ENDOCRINE-RELATED CANCER, 25(2), T53-T68 [10.1530/ERC-17-0297].|
|Tipo:||Articolo in rivista - Review Essay|
|Carattere della pubblicazione:||Scientifica|
|Presenza di un coautore afferente ad Istituzioni straniere:||Si|
|Titolo:||Novel targeted therapeutics for MEN2|
|Autori:||Redaelli, S; Plaza-Menacho, I; Mologni, L|
MOLOGNI, LUCA (Corresponding)
|Data di pubblicazione:||2018|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1530/ERC-17-0297|
|Appare nelle tipologie:||01 - Articolo su rivista|