Discovery of Novel PDEδ Degraders for the Treatment of KRAS Mutant Colorectal Cancer.
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DOI: 10.1021/acs.jmedchem.0c00929
Abstract: KRAS-PDEδ protein-protein interaction represents an appealing target for cancer therapy. However, fast release of high-affinity inhibitors from PDEδ hampered drug binding affinity and antiproliferative activity. To overcome the limitations, the first proteolysis-targeting chimeric (PROTAC) small… read more here.
Keywords: colorectal cancer; pde degraders; pde; kras mutant ... See more keywords
Design and Structural Optimization of Orally Bioavailable SOS1 Inhibitors for the Treatment of KRAS-Driven Carcinoma.
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DOI: 10.1021/acs.jmedchem.2c01517
Abstract: KRAS mutations (G12C, G12D, etc.) are implicated in the oncogenesis and progression of many refractory cancers. Son of sevenless homolog 1 (SOS1) is a key regulator of KRAS to modulate KRAS from inactive to active… read more here.
Keywords: optimization orally; design structural; structural optimization; kras driven ... See more keywords
Genotype‐guided targeted treatment of KRAS‐mutated arteriovenous malformations
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DOI: 10.1111/jdv.18165
Abstract: 1966; 34: 827–857 PMID:5330347. 7 Insee. A Mayotte, pr es d’un habitant sur deux est de nationalit e etrang ere. Montrouge, Paris: Insee Premi ere. 2019;1737 [Internet]. French. https:// www.insee.fr/fr/statistiques/3713016 (last accessed 16 November 2021).… read more here.
Keywords: genotype guided; targeted treatment; kras mutated; guided targeted ... See more keywords
A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib
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DOI: 10.2147/lctt.s383662
Abstract: Abstract KRASG12C is one of the most common oncogenes in non-small cell lung cancer (NSCLC) and is associated with a poor prognosis. Historically, KRAS mutations have been difficult to target due to lack of binding… read more here.
Keywords: mutations nsclc; long overdue; targeted treatment; kras mutations ... See more keywords