The RET gene is frequently mutated in papillary thyroid carcinoma and in medullary thyroid carcinoma. We have identified three different anti-RET drugs: two pyrazolo-pyrimidines, PP1 and PP2 and an anilinoquinazoline, ZD6474 (AstraZeneca). These compounds are able to inhibit RET kinase activity in vitro (IC50 dose 100 nM) and in vivo and they can prevent RET mediated transformation. Finally, mutation of RET V804 to methionine or leucine, found in MTC patients, induces resistance to the three drugs.
Identification of RET kinase inhibitors as potential new treatment for sporadic and inherited thyroid cancer / Carlomagno, Francesca; Santoro, Massimo. - In: JOURNAL OF CHEMOTHERAPY. - ISSN 1973-9478. - STAMPA. - 16 Suppl 4:(2004), pp. 49-51.
Identification of RET kinase inhibitors as potential new treatment for sporadic and inherited thyroid cancer.
CARLOMAGNO, Francesca;SANTORO, MASSIMO
2004
Abstract
The RET gene is frequently mutated in papillary thyroid carcinoma and in medullary thyroid carcinoma. We have identified three different anti-RET drugs: two pyrazolo-pyrimidines, PP1 and PP2 and an anilinoquinazoline, ZD6474 (AstraZeneca). These compounds are able to inhibit RET kinase activity in vitro (IC50 dose 100 nM) and in vivo and they can prevent RET mediated transformation. Finally, mutation of RET V804 to methionine or leucine, found in MTC patients, induces resistance to the three drugs.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
