令人惊喜的是，该研究团队几乎同时在CANCER DISCOVERY 发表了另外一篇题为Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers 的报道，带来了另外一款多选择性非共价抑制剂RMC-6236，可抑制典型 RAS 亚型突变型和野生型变体的活性 GTP 结合状态[5]。RMC-7977分子简介 ...
4月8日,Revolution Medicines在Nature上发表了RAS抑制剂RMC-7977的临床前研究,文章标题为“Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy1”。去年8月24日我们就在公众号和大家分享过他们的RMC-4998分子,当时是一篇Sci...
为了解决这一问题，不久前美国抗肿瘤药物研发商Revolution Medicines在《自然》杂志上发表了题为“Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy”的论文，介绍了一种新型可逆性三元复合物RAS抑制剂——RMC-7977，它展现出对突变型及野生型KRAS、NRAS、HRAS变体活性状态的广泛抑制作用，...
RAS INHIBITION INDENYL ACETAMIDE COMPOUND, COMPOSITION, AND USES THEREOFCompounds, for example compounds of formula (I) (Wherein R, R, R~ R, N, X, Y, Y, And E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or...
[1]Matthew Holderfield et al. Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy. Nature(2024) [2]Urszula N. Wasko et al. Tumor-selective activity of RAS-GTP inhibition in pancreatic cancer. Nature(2024) [3]https://ir.revmed.com/news-releases/news-release-details...
besides K69 which was used as a control in the Nano-BRET assays. The dose-dependency of nucleotide exchange inhibition by the 3 selected Affimers was then assessed (Fig.1b). Affimer K3 displayed the greatest inhibition of nucleotide exchange on wild-type KRAS with an IC50of 144 ± 94...
20. Kraus BJ, Weir MR, Bakris GL, et al. Characterization and implications of the initial estimated glomerular filtration rate 'dip' upon sodium‑glucose cotransporter‑2 inhibition with empagliflozin in the EMPA‑REG OUTCOME tri...
RAS inhibition via direct RAS binding — is there a path forward? Bioorg. Med. Chem. Lett. 22, 5766–5776 (2012). Article CAS PubMed Google Scholar Taveras, A. G. et al. RAS oncoprotein inhibitors: the discovery of potent, RAS nucleotide exchange inhibitors and the structural ...
Selective inhibition of oncogenic KRAS output with small molecules targeting the inactive state. Cancer Discov. 2016, 6 (3): 316-329. [2] Matthew R Janes, et al. Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor. Cell. 2018, 172(3): 578-589. >>> 相关产品 K-Ras...
A, Karow A, Seebauer C, Platz Batista da Silva N, Wohlgemuth WA, Oppenheimer A, Kröning P, Niemeyer CM, Schanze D, Zenker M, Eng W, Ahmadian MR, Baumgartner I, Rössler J. Somatic RIT1 delins in arteriovenous malformations hyperactivate RAS-MAPK signaling amenable to MEK inhibition....