Structural and dynamic determinants for highly selective RET kinase inhibition reveal cryptic druggability. [PDF]
, 2022 The structural and dynamic determinants for highly selective RET kinase inhibition are poorly understood. Here we demonstrate by applying an integrated structural, computational and biochemical approach that the druggability landscape of the RET active ...
Contreras, Julia +8 more
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Current Guidelines for Management of Medullary Thyroid Carcinoma [PDF]
Endocrinology and Metabolism, 2021 Medullary thyroid carcinoma (MTC) is a rare neuroendocrine tumor originating from the parafollicular cells. The diagnostic and therapeutic strategies for the condition are different from those used for well-differentiated thyroid cancer.
Mijin Kim, Bo Hyun Kim
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healthbook TIMES. Oncology Hematology, 2021 The RET gene encodes a tyrosine kinase receptor that regulates cell survival and proliferation by triggering key downstream pathways.1 RET gene mutations and RET gene fusions are involved in the pathogenesis of lung, thyroid and other cancers.
Alfredo Addeo, Frank Stenner
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RET-MAP: An International Multicenter Study on Clinicobiologic Features and Treatment Response in Patients With Lung Cancer Harboring a RET Fusion [PDF]
, 2023 Chemotherapy; Non–small cell lung cancer; RET inhibitorsQuimioteràpia; Càncer de pulmó de cèl·lules no petites; Inhibidors de RETQuimioterapia; Cáncer de pulmón de células no pequeñas; Inhibidores de RETIntroduction Nearly 1% to 2% of NSCLCs harbor RET ...
Aldea, Mihaela +7 more
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Thyroid cancers: From surgery to current and future systemic therapies through their molecular identities [PDF]
, 2021 Differentiated thyroid cancers (DTC) are commonly and successfully treated with total thyroidectomy plus/minus radioiodine therapy (RAI). Medullary thyroid cancer (MTC) is only treated with surgery but only intrathyroidal tumors are cured.
Agate L. +13 more
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In Silico Strategies for Prospective Drug Repositionings [PDF]
, 2023 The discovery of new drugs is one of pharmaceutical research's most exciting and challenging tasks. Unfortunately, the conventional drug discovery procedure is chronophagous and seldom successful; furthermore, new drugs are needed to address our clinical
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Non-small-cell lung cancer: how to manage RET-positive disease
Drugs in Context, 2022 Targeted therapy has dramatically changed the history and outcomes of oncogene-addicted non-small-cell lung cancer (NSCLC). RET rearrangements are typically observed in about 1–2% of NSCLC, resulting in constitutive activation of downstream signalling ...
Elisa Andrini +6 more
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LIBRETTO-531: a phase III study of selpercatinib in multikinase inhibitor-naïve RET-mutant medullary thyroid cancer [PDF]
, 2022 Medullary thyroid cancer; Selpercatinib; Targeted therapyCáncer medular de tiroides; Selpercatinib; Terapia dirigidaCàncer medul·lar de tiroide; Selpercatinib; Teràpia dirigidaSelpercatinib is a first-in-class, highly selective and potent, central ...
Brose, Marcia S +5 more
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The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib
npj Precision Oncology, 2021 Recently Food and Drug Administration (FDA)-approved pralsetinib (BLU-667) and selpercatinib (LOXO-292) are RET-selective protein tyrosine kinase inhibitors for treating RET-altered cancers, but whether they have distinct activity was unknown.
Tao Shen +5 more
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Frontiers in Oncology, 2022 We are recently faced with a progressive evolution of the therapeutic paradigm for radioiodine refractory differentiated thyroid cancer (RAI-R DTC), since the advent of tissue agnostic inhibitors.
Margherita Nannini +20 more
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