Targeting KRAS(G12C): From Inhibitory Mechanism to Modulation of Antitumor Effects in Patients
Sign Up to like & getrecommendations! Published in 2020 at "Cell"
DOI: 10.1016/j.cell.2020.09.044
Abstract: KRAS mutations are among the most common genetic alterations in lung, colorectal, and pancreatic cancers. Direct inhibition of KRAS oncoproteins has been a long-standing pursuit in precision oncology, one established shortly after the discovery of… read more here.
Keywords: inhibitory mechanism; g12c inhibitory; targeting kras; mechanism modulation ... See more keywords
KRAS p.G12C mutation occurs in 1% of EGFR-mutated advanced non-small-cell lung cancer patients progressing on a first-line treatment with a tyrosine kinase inhibitor
Sign Up to like & getrecommendations! Published in 2021 at "ESMO Open"
DOI: 10.1016/j.esmoop.2021.100279
Abstract: Background KRAS is mutated in ∼30% of non-small-cell lung cancer (NSCLC) but it has also been identified as one of the mechanisms underlying resistance to tyrosine kinase inhibitors (TKIs) in EGFR-positive NSCLC patients. Novel KRAS… read more here.
Keywords: nsclc; first line; g12c mutation; kras g12c ... See more keywords
Quantifying KRAS G12C Covalent Drug Inhibitor Activity in Mouse Tumors Using Mass Spectrometry.
Sign Up to like & getrecommendations! Published in 2023 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.2c04417
Abstract: The growing opportunities recognized for covalent drug inhibitors, like KRAS G12C inhibitors, are driving the need for mass spectrometry methods that can quickly and robustly measure therapeutic drug activity in vivo for drug discovery research… read more here.
Keywords: mass spectrometry; kras g12c; drug; activity ... See more keywords
Two new agents target KRAS G12C
Sign Up to like & getrecommendations! Published in 2019 at "Nature Reviews Clinical Oncology"
DOI: 10.1038/s41571-019-0304-3
Abstract: Nature reviews | CliniCal OnCOlOgy Attempts to therapeutically target the products of the RAS oncogenes, frequently mutated in cancer, have had disappointing results thus far. The small molecules MRTX849 and AMG 510, from two independent… read more here.
Keywords: kras g12c; treatment; amg 510; oncology ... See more keywords
Multiple initiatives to conquer KRAS G12C inhibitor resistance from the perspective of clinical therapy
Sign Up to like & getrecommendations! Published in 2023 at "Expert Opinion on Investigational Drugs"
DOI: 10.1080/13543784.2023.2178419
Abstract: ABSTRACT Introduction KRAS G12C targeted covalent inhibitors for cancer therapy are revolutionary. However, resistance to KRAS G12C inhibitors in clinical trials is a proven fact. Areas covered The authors focus on providing coverage and emphasizing… read more here.
Keywords: kras g12c; inhibitor resistance; therapy; resistance ... See more keywords
Targeting KRAS G12C mutations in colorectal cancer
Sign Up to like & getrecommendations! Published in 2022 at "Gastroenterology Report"
DOI: 10.1093/gastro/goac083
Abstract: Abstract With the advent of Kirsten rat sarcoma viral oncogene homologue G12C (KRAS G12C) inhibitors, RAS is no longer considered undruggable. For the suppression of RAS, new therapeutic approaches have been suggested. However, current clinical… read more here.
Keywords: targeting kras; kras g12c; colorectal cancer; therapeutic resistance ... See more keywords
Novel natural inhibitors targeting KRAS G12C by computational study
Sign Up to like & getrecommendations! Published in 2022 at "Anti-Cancer Drugs"
DOI: 10.1097/cad.0000000000001317
Abstract: Ideal leading and nominee compounds with inhibiting effects on KRAS G12C were selected from the ZINC database, laying a cornerstone for the progress of anticancer drugs. A variety of computational virtual screening methods were utilized… read more here.
Keywords: kras g12c; inhibitors targeting; zinc000012494057 zinc000003789195; natural inhibitors ... See more keywords
Abstract 1079: Combination of tipifarnib with KRAS G12C inhibitors to prevent adaptive resistance
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-1079
Abstract: Selective KRAS G12C inhibitors, including AMG510 (sotorasib) and MRTX849 (adagrasib), have exhibited clinical activity in patients with non-small cell lung cancer (NSCLC); however, drug resistance and relapse inevitably occur through various mechanisms, which limits the… read more here.
Keywords: kras g12c; g12c inhibitors; adaptive resistance; combination ... See more keywords
Abstract 2137: Clinical utility of circulating tumor DNA in patients with advanced KRAS G12C-mutated NSCLC treated with sotorasib
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-2137
Abstract: Introduction: The CodeBreaK 200 trial showed that in patients (pts) with advanced KRAS G12C mutated (KRAS+) NSCLC sotorasib, a KRAS G12C-specific inhibitor, is superior to docetaxel for progression free survival (PFS) (HR 0.66) with a… read more here.
Keywords: kras g12c; ctdna; keap1; stk11 ... See more keywords
Abstract 2267: HLA-DR-restricted CD4 T cell responses to KRAS G12C in healthy donors linked to bacterial mimotope: lessons for KRAS neoantigen vaccines in cancer patients
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-2267
Abstract: Mutations in the KRAS gene are among the most common driver mutations in cancer. Targeting KRAS G12C mutations has shown some promise in clinical studies, though acquired resistance mutations pose a challenge for small molecule-based… read more here.
Keywords: kras g12c; cell responses; cell; cd4 cell ... See more keywords
Abstract 257: CDX model based genome-scale CRISPR KO screens for modulators of KRAS (G12C) inhibitor sensitivity
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-257
Abstract: KRAS is the most frequently mutated oncogene in human cancers and had long been considered an undruggable target for cancer therapy, until the FDA approval of Sotorasib (AMG 510) for the treatment of patients with… read more here.
Keywords: cell; kras g12c; scale crispr; cancer ... See more keywords