國家衛生研究院 NHRI:Item 3990099045/11080
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    題名: Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors
    作者: La Pietra, V;Sartini, S;Botta, L;Antonelli, A;Ferrari, SM;Fallahi, P;Moriconi, A;Coviello, V;Quattrini, L;Ke, YY;Hsing-Pang, H;Da Settimo, F;Novellino, E;La Motta, C;Marinelli, L
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: It is now known that “gain of function” mutations of RET (REarranged during Transfection) kinase are specific and key oncogenic events in the onset of thyroid gland cancers such as the Medullary Thyroid Carcinoma (MTC). Although a number of RET inhibitors exist and are capable of inhibiting RET variants, in which mutations are outside the enzyme active site, the majority becomes dramatically ineffective when mutations are within the protein active site (V804L and V804M). Pursuing a receptor-based virtual screening against the kinase domain of RET, we found that compound 5 is able to inhibit efficiently both wild type and V804L mutant RET. Compound 5 was able to significantly reduce proliferation of both commercially available TT cell lines and surgical thyroid tissues obtained from patients with MTC and displayed a suitable drug-like profile, thus standing out as a promising candidate for further development towards the treatment of clinically unresponsive MTC.
    日期: 2018-04-25
    關聯: European Journal of Medicinal Chemistry. 2018 Apr 25;150:491-505.
    Link to: http://dx.doi.org/10.1016/j.ejmech.2018.02.080
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0223-5234&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000430891400033
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85043520960
    顯示於類別:[謝興邦] 期刊論文

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