Blog of Signaling Pathways

IGF-1R inhibition induces MEK phosphorylation to promote survival in colon carcinomas

455 views | Apr 07 2021

Qing Wang et al. found that the treatment of colon tumor cells with IGF-1R inhibitors stimulated p70S6K1 activity via MEK1/2 to promote survival, providing a new strategy for colorectal cancer therapeutics. [Read the Full Post]

A proprotein convertase subtilisin/kexin type 9 inhibitor provides comparable efficacy with lower detriment than statins on mitochondria of oxidative muscle of obese estrogen-deprived rats

416 views | Apr 06 2021

Chanisa Thonusin et al. showed that 17β-Estradiol exhibited the greatest efficacy on the attenuation of obesity with the least harmful effect on skeletal muscle in a model of menopause with obesity, yet its effect on the treatment of hyperlipidemia was inferior to those of standard lipid-lowering agents. [Read the Full Post]

Melanin Distribution in Human Skin: Influence of Cytoskeletal, Polarity, and Centrosome-Related Machinery of Stratum basale Keratinocytes

1147 views | Apr 06 2021

Irene Castellano-Pellicena et al. explored the role of actin, microtubules, and centrosome-associated machinery in distributing melanin within KCs. [Read the Full Post]

In vivo Pharmacokinetic Drug-Drug Interaction Studies Between Fedratinib and Antifungal Agents Based on a Newly Developed and Validated UPLC/MS-MS Method

928 views | Apr 04 2021

Congrong Tang et al. thought that the toxicity of fedratinib should be avoided when the concurrent use of fedratinib with CYP3A4 inhibitors might occur. [Read the Full Post]

Current Clinical Investigations in Myelofibrosis

1023 views | Apr 04 2021

Sangeetha Venugopal et al. provided insight into the novel therapies under clinical evaluation. [Read the Full Post]

Preclinical Evaluation of the Pan-FGFR Inhibitor LY2874455 in FRS2-Amplified Liposarcoma

481 views | Apr 02 2021

Robert Hanes et al. supported LY2874455 as a better therapy than NVP-BGJ398 for FRS2-amplified liposarcoma, and a clinical trial was warranted. [Read the Full Post]

Protective effects of NAC and salubrinal on apoptosis of retinal pigment epithelial cells induced by all-trans retinoic acid

1095 views | Apr 02 2021

Juan Wu et al. thought that ATRA might play an important role in the prevention, diagnosis and treatment of age-related macular degeneration. [Read the Full Post]

Isoform- and phosphorylation-specific multiplexed quantitative pharmacodynamics of drugs targeting PI3K and MAPK signaling in xenograft models and clinical biopsies

231 views | Apr 01 2021

William G Herrick et al. demonstrated the degree and duration of phosphorylation modulation for three distinct classes of drugs targeting the PI3K/AKT and MAPK pathways. [Read the Full Post]

LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors

325 views | Apr 01 2021

Kelli-Ann Monaco et al. found that LXH254 was a novel RAF inhibitor, which was able to inhibit dimerized BRAF and CRAF, as well as monomeric BRAF, while largely sparing ARAF. [Read the Full Post]

Cardiomyocyte protective effects of thyroid hormone during hypoxia/reoxygenation injury through activating of IGF-1-mediated PI3K/Akt signalling

254 views | Mar 31 2021

Bin Zeng et al. showed that T3 pretreatment protected cardiomyocytes against H/R-induced injury by activating the IGF-1-mediated PI3K/Akt signalling pathway. [Read the Full Post]

BET inhibitor bromosporine enhances 5-FU effect in colorectal cancer cells

208 views | Mar 30 2021

Xueyuan Cheng et al. found that the combination treatment inhibits cell viability, formation of colonies, increased apoptosis and cell cycle arrest at G0-G1. [Read the Full Post]

Nucleotide variation in histone H2BL drives crossalk of histone modification and promotes tumour cell proliferation by upregulating c-Myc

471 views | Mar 30 2021

Lei Zhang et al. revealed that an H2BK5ac-H2BK120ubi crosstalk which regulates gene transcription. [Read the Full Post]

Topical Exposure to Nemopilema nomurai Venom Triggers Oedematogenic Effects: Enzymatic Contribution and Identification of Venom Metalloproteinase

363 views | Mar 29 2021

Yang Yue et al. suggested a considerable contribution of NnNV metalloproteinase-like components to the increased vasopermeability. [Read the Full Post]

Specific Inhibitor of Matrix Metalloproteinase Decreases Tumor Invasiveness After Radiofrequency Ablation in Liver Tumor Animal Model

298 views | Mar 29 2021

An-Na Jiang et al. suggested that targeting the MMP process with the specific inhibition could help to increase overall ablation efficacy. [Read the Full Post]

A high-throughput screen identifies that CDK7 activates glucose consumption in lung cancer cells

362 views | Mar 28 2021

Chiara Ghezzi et al. thought that CDK7 was a key regulator of glucose consumption in cells with an activated PI3K pathway. [Read the Full Post]

Comprehensive analysis of ubiquitin-specific protease 1 reveals its importance in hepatocellular carcinoma

325 views | Mar 28 2021

Yalei Zhao et al. found that USP1 was a promising target for HCC treatment with good prognostic value. [Read the Full Post]

A covalent p97/VCP ATPase inhibitor can overcome resistance to CB-5083 and NMS-873 in colorectal cancer cells

440 views | Mar 26 2021

Gang Zhang et al. identified and characterized PPA as a selective covalent p97 inhibitor, which would allow future exploration to improve the potency of p97 inhibitors with different mechanisms of action. [Read the Full Post]

The role of drug efflux and uptake transporters ABCB1 (P-gp), ABCG2 (BCRP) and OATP1A/1B and of CYP3A4 in the pharmacokinetics of the CDK inhibitor milciclib

292 views | Mar 26 2021

Alejandra Martínez-Chávez found that the low impact of OATP1 and CYP3A could be clinically favorable for milciclib, reducing the risks of unintended drug-drug interactions or interindividual variation in CYP3A4 activity. [Read the Full Post]

CEP131 Abrogates CHK1 Inhibitor-Induced Replication Defects and Is Associated with Unfavorable Outcome in Neuroblastoma

279 views | Mar 25 2021

Kiyohiro Ando et al. revealed that MDM2 was associated with CEP131 protein degradation, whereas overexpression of CEP131 accelerated neuroblastoma cell growth and exhibited resistance to CHK1i-induced replication defects. [Read the Full Post]

Pharmacological inhibition of IKKβ dampens NLRP3 inflammasome activation after priming in the human myeloid cell line THP-1

825 views | Mar 25 2021

Adeline Unterreiner et al. suggested that IκKβ might fulfill a dual role in coupling priming and activation of the NLRP3 inflammasome. [Read the Full Post]

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