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Showing 1-11 of 11 results for "SML3055" within Papers
João M Fernandes Neto et al.
Nature communications, 11(1), 3157-3157 (2020-06-24)
Resistance to targeted cancer drugs is thought to result from selective pressure exerted by a high drug dose. Partial inhibition of multiple components in the same oncogenic signalling pathway may add up to complete pathway inhibition, while decreasing the selective
James R Henry et al.
Journal of medicinal chemistry, 58(10), 4165-4179 (2015-05-13)
The RAS-RAF-MEK-MAPK cascade is an essential signaling pathway, with activation typically mediated through cell surface receptors. The kinase inhibitors vemurafenib and dabrafenib, which target oncogenic BRAF V600E, have shown significant clinical efficacy in melanoma patients harboring this mutation. Because of
Wei-Jun Wei et al.
Theranostics, 7(4), 987-1001 (2017-04-07)
Although the prognosis of differentiated thyroid cancer (DTC) is relatively good, 30-40% of patients with distant metastases develop resistance to radioactive iodine therapy due to tumor dedifferentiation. For DTC patients harboring BRAFV600E mutation, Vemurafenib, a BRAF kinase inhibitor, has dramatically
Eliza Vakana et al.
Oncotarget, 8(6), 9251-9266 (2016-12-22)
Activating mutations in the KRAS and BRAF genes, leading to hyperactivation of the RAS/RAF/MAPK oncogenic signaling cascade, are common in patients with colorectal cancer (CRC). While selective BRAF inhibitors are efficacious in BRAFmut melanoma, they have limited efficacy in BRAFmut
Shih-Hsun Chen et al.
Cancer discovery, 6(3), 300-315 (2016-01-07)
We have identified previously undiscovered BRAF in-frame deletions near the αC-helix region of the kinase domain in pancreatic, lung, ovarian, and thyroid cancers. These deletions are mutually exclusive with KRAS mutations and occur in 4.21% of KRAS wild-type pancreatic cancer.
S-H Chen et al.
Oncogene, 37(6), 821-832 (2017-10-24)
KRAS, NRAS and BRAF mutations are among the most important oncogenic drivers in many major cancer types, such as melanoma, lung, colorectal and pancreatic cancer. There is currently no effective therapy for the treatment of RAS mutant cancers. LY3009120, a
Su-Min Yang et al.
International journal of molecular medicine, 42(6), 3477-3484 (2018-10-03)
Excessive preadipocyte differentiation/adipogenesis is closely linked to the development of obesity. LY3009120 is a pan‑Raf kinase inhibitor and is known for its anticancer activities. In the present study, the effect of LY3009120 on 3T3‑L1 cell adipogenesis was investigated. The differentiation
Sheng-Bin Peng et al.
Cancer cell, 28(3), 384-398 (2015-09-08)
LY3009120 is a pan-RAF and RAF dimer inhibitor that inhibits all RAF isoforms and occupies both protomers in RAF dimers. Biochemical and cellular analyses revealed that LY3009120 inhibits ARAF, BRAF, and CRAF isoforms with similar affinity, while vemurafenib or dabrafenib
Shunsaku Miyauchi et al.
Anticancer research, 40(5), 2667-2673 (2020-05-06)
The therapeutic strategy for patients with non-small-cell lung cancer (NSCLC) harboring the BRAF non-V600E mutation has not been established. LY3009120, a newly discovered pan-RAF inhibitor, has shown strong antitumor effects in cancers with various BRAF genotypes. This study investigated the
Young B Kim et al.
Archives of biochemistry and biophysics, 445(1), 9-18 (2005-12-21)
Dipeptidyl peptidase-IV (DPP-IV) is a serine protease with a signature Asp-His-Ser motif at the active site. Our pH data suggest that Gly-Pro-pNA cleavage catalyzed by DPP-IV is facilitated by an ionization of a residue with a pK of 7.2 +/-
Chong Zhang et al.
Clinical science (London, England : 1979), 133(8), 919-932 (2019-04-05)
A dramatic increase in the incidence of inflammatory bowel disease (IBD) has been observed in the past two decades, mainly in developed countries and also in developing regions. Necroptosis has been found to play an important role in the pathogenesis
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