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Blog of Signaling Pathways

Cases of ROS1-rearranged lung cancer: when to use crizotinib, entrectinib, lorlatinib, and beyond?

555 views | Nov 23 2020

Kartik Sehgal et al. described cases of advanced ROS1-rearranged lung cancer receiving crizotinib, entrectinib, and/or lorlatinib in first and later line treatment settings to dissect the current state of evidence supporting management decisions for these patients. [Read the Full Post]

Co-targeting PIM and PI3K/mTOR using multikinase inhibitor AUM302 and a combination of AZD-1208 and BEZ235 in prostate cancer

561 views | Nov 22 2020

Sabina Luszczak et al. believed that a co-targeting approach was a viable therapeutic strategy that should be developed further in pre-clinical studies. [Read the Full Post]

An essential role for Argonaute 2 in EGFR-KRAS signaling in pancreatic cancer development

669 views | Nov 22 2020

Sunita Shankar et al. supported a biphasic model of pancreatic cancer development: an AGO2-independent early phase of PanIN formation reliant on EGFR-RAS signaling, and an AGO2-dependent phase wherein the mutant KRAS-AGO2 interaction was critical for PDAC progression. [Read the Full Post]

Cost-effectiveness of treatments for HER2-positive metastatic breast cancer and associated metastases: an overview of systematic reviews

359 views | Nov 21 2020

Vakaramoko Diaby et al. examined evidence on the cost-effectiveness of treatments for HER2-positive metastatic breast cancer and associated metastases through a review of systematic reviews on the topic. [Read the Full Post]

Brain exposure of the ATM inhibitor AZD1390 in humans - a positron emission tomography (PET) study

396 views | Nov 21 2020

Aurelija Jucaite et al. found the potential of PET microdosing in predicting and guiding dose range and schedule for subsequent clinical studies. [Read the Full Post]

Preclinical evaluation of antitumor activity of the proteasome inhibitor MLN2238 (ixazomib) in hepatocellular carcinoma cells

0 views | Nov 20 2020

Giuseppa Augello et al. thought that association of A1210477 and MLN2238 determined synergistic antitumor effects in HCC cells. [Read the Full Post]

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity

181 views | Nov 20 2020

Zhi-Fu Tao et al. found that A-1155463 represented an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization. [Read the Full Post]

Direct Activation of BAX by BTSA1 Overcomes Apoptosis Resistance in Acute Myeloid Leukemia

0 views | Nov 19 2020

Denis E Reyna et al. provided proof-of-concept for direct BAX activation as a treatment strategy in AML. [Read the Full Post]

The MET Inhibitor AZD6094 (Savolitinib, HMPL-504) Induces Regression in Papillary Renal Cell Carcinoma Patient-Derived Xenograft Models

211 views | Nov 19 2020

Alwin G Schuller et al. provided the first report testing therapeutics in preclinical in vivo models of PRCC and supported the clinical development of AZD6094 in the indication. [Read the Full Post]

Cucurbitacin E and I target the JAK/STAT pathway and induce apoptosis in Sézary cells

1337 views | Nov 18 2020

Isabella J Brouwer et al. suggested that STAT3 played a preferential role in the mechanism of action of these cucurbitacins. [Read the Full Post]

RIP3 dependent NLRP3 inflammasome activation is implicated in acute lung injury in mice

525 views | Nov 18 2020

Jingxian Chen et al. showed that RIP3 participated in the NLRP3 inflammasome activation in infiltrating macrophages in ALI induced by LPS. [Read the Full Post]

Rapalogues as hCES2A Inhibitors: In Vitro and In Silico Investigations

315 views | Nov 17 2020

Cheng-Cheng Shi et al. demonstrated that several marketed rapalogues were potent and specific hCES2A inhibitors, and these agents could serve as leading compounds for the development of more efficacious hCES2A inhibitors to modulate the pharmacokinetic profiles and toxicity of hCES2A-substrate drugs (such as the anticancer agent irinotecan). [Read the Full Post]

CXCL14 inhibits the growth and promotes apoptosis of hepatocellular carcinoma cells via suppressing Akt/mTOR pathway

351 views | Nov 17 2020

Jianqiang Bi et al. thought that CXCL14 inhibited growth but promoted apoptosis of HCC cells via suppressing Akt/mTOR pathway and CXCL14 might be a potential target for HCC treatment in clinical practice. [Read the Full Post]

Suppressor of Ty 16 promotes lung cancer malignancy and is negatively regulated by miR-1227-5p

335 views | Nov 15 2020

Lu Yang et al. indicated that Spt16 was likely to be an essential regulator for lung cancer malignancy and was negatively regulated by miR-1227-5p. [Read the Full Post]

A phase I trial of temsirolimus and erlotinib in patients with refractory solid tumors

647 views | Nov 15 2020

Haeseong Park et al. found the he combination of temsirolimus and erlotinib at the RP2D was well tolerated, and the regimen resulted in prolonged disease stabilization in selected patients (NCT00770263). [Read the Full Post]

Alectinib-Associated Perforated Duodenal Ulcer

309 views | Nov 14 2020

Maximilian J Hochmair et al. found that later-line lorlatinib treatment could induce sustained responses in patients with advanced ALK- and ROS1-positive lung cancer. [Read the Full Post]

Menin regulates the serine biosynthetic pathway in Ewing sarcoma

0 views | Nov 14 2020

Laurie K Svoboda et al. demonstrated that the SSP was highly active in Ewing sarcoma and that its oncogenic activation was maintained, at least in part, by menin-dependent epigenetic mechanisms involving trithorax complexes. [Read the Full Post]

Defactinib attenuates osteoarthritis by inhibiting positive feedback loop between H-type vessels and MSCs in subchondral bone

460 views | Nov 13 2020

Yanjun Hu et al. demonstrated that defactinib inhibited OA by suppressing the positive feedback loop between H-type vessels and MSCs in subchondral bone. [Read the Full Post]

Dexmedetomidine reduces ventilator-induced lung injury via ERK1/2 pathway activation

446 views | Nov 13 2020

Chun-Hua Zhu et al. found that dexmedetomidine reduced the inflammatory response and epithelial cell death caused by VILI, via the activation of the ERK1/2 signaling pathway. [Read the Full Post]

Identification of Quinazolinone Analogs Targeting CDK5 Kinase Activity and Glioblastoma Cell Proliferation

178 views | Nov 12 2020

Marion Peyressatre et al. found that the quinazolinone derivatives were the first small molecules reported to target CDK5 at a site other than the ATP pocket, thereby constituting attractive leads for glioblastoma therapeutics and providing therapeutic perspectives for neurodegenerative diseases. [Read the Full Post]