Blog of Signaling Pathways

Evolution of kinase polypharmacology across HSP90 drug discovery

1051 views | Oct 13 2021

Albert A Antolin et al. found that the resorcinol clinical candidates ganetespib and, to a lesser extent, luminespib, displayed unique off-target kinase pharmacology as compared with other HSP90 inhibitors. [Read the Full Post]

Synthesis and evaluation of FAK inhibitors with a 5-fluoro-7H-pyrrolo[2,3-d]pyrimidine scaffold as anti-hepatocellular carcinoma agents

803 views | Oct 12 2021

Hanyi Tan et al. suggested that 16c inhibited the malignant proliferation of hepatocellular carcinoma (HCC) cells through decreasing the phosphorylation in the FAK cascade. [Read the Full Post]

Histone deacetylase inhibitor givinostat attenuates nonalcoholic steatohepatitis and liver fibrosis

609 views | Oct 12 2021

He-Ming Huang et al. found that givinostat was efficacious in reversing diet-induced NASH, and might serve as a therapeutic agent for the treatment of human NASH. [Read the Full Post]

In silico evaluation of the downstream effect of mutated glucagon is consistent with higher blood glucose homeostasis in Galliformes and Strigiformes

353 views | Oct 11 2021

Karim Mahnam et al. suggested this mutation, which leaded to stronger binding affinity of mutated glucagon to its receptor, might be a driving force for higher blood glucose homeostasis in the related birds. [Read the Full Post]

"Petal-like" size-tunable gold wrapped immunoliposome to enhance tumor deep penetration for multimodal guided two-step strategy

383 views | Oct 11 2021

Yanan Li et al. provided a synergistic treatment strategy that could broaden the conventional treatment alone. [Read the Full Post]

rhKGF-2 Attenuates Smoke Inhalation Lung Injury of Rats via Activating PI3K/Akt/Nrf2 and Repressing FoxO1-NLRP3 Inflammasome

413 views | Oct 10 2021

Zhonghua Fu et al. found that rhKGF-2 mitigated SILI by regulating the PI3K/Akt/Nrf2 pathway and the FoxO1-NLRP3 axis, which provided new reference in treating SILI. [Read the Full Post]

Development of LM98, a Small-Molecule TEAD Inhibitor Derived from Flufenamic Acid

421 views | Oct 10 2021

Léa Mélin et al. found that LM98 reduced the expression of CTGF and Cyr61, inhibited MDA-MB-231 breast cancer cell migration and arrested cell cycling in the S phase during cell division. [Read the Full Post]

Genetic Prioritization, Therapeutic Repositioning and Cross-Disease Comparisons Reveal Inflammatory Targets Tractable for Kidney Stone Disease

374 views | Oct 09 2021

Hai Fang et al. provided the rich information of how to target innate immune pathways, with the potential of advancing immunotherapeutic strategies for nephrolithiasis. [Read the Full Post]

GSK2126458 has the potential to inhibit the proliferation of pancreatic cancer uncovered by bioinformatics analysis and pharmacological experiments

349 views | Oct 09 2021

Yueqin Feng et al. found that the PI3K-Akt signaling pathway may be a key pathway for pancreatic cancer, our study uncovered the potential therapeutic potential of GSK2126458, a specific mTOR inhibitor, for pancreatic cancer. [Read the Full Post]

FSH stimulated bovine granulosa cell steroidogenesis involves both canonical and noncanonical WNT signaling

363 views | Oct 08 2021

M Ashry et al. found that both canonical and noncanonical WNT pathways activation was linked to FSH stimulation of E2 production by bovine granulosa cells. [Read the Full Post]

Dual Inhibition of Histone Deacetylases and the Mechanistic Target of Rapamycin Promotes Apoptosis in Cell Line Models of Uveal Melanoma

337 views | Oct 08 2021

Ruchi P Patel et al. found that romidepsin in combination with mTOR inhibition could be an effective treatment strategy against uveal melanoma due in part to changes in apoptotic proteins. [Read the Full Post]

Structural basis of the selective activation of enzyme isoforms: Allosteric response to activators of β1- and β2-containing AMPK complexes

894 views | Oct 06 2021

Elnaz Aledavood et al. found the design of activators tailored for improving the therapeutic treatment of tissue-specific metabolic disorders. [Read the Full Post]

Aspiration Is Associated with Poor Treatment Response in Pediatric Pulmonary Vein Stenosis

1037 views | Oct 06 2021

Maria Niccum et al. found that potentially modifiable risk factor for poor treatment response in pediatric multi-vessel intraluminal pulmonary vein stenosis in patients with 2-ventricle physiology. [Read the Full Post]

Regulation and function of AP-1 in insulinoma cells and pancreatic β-cells

818 views | Oct 05 2021

Tobias M Backes et al. found that AP-1 controls an important function of pancreatic β-cells in vivo, the regulation of glucose homeostasis. [Read the Full Post]

Successful treatment of hepatosplenic T-cell lymphoma with fludarabine, high-dose cytarabine and subsequent unrelated umbilical cord blood transplantation

721 views | Oct 04 2021

Takaya Honda et al. found a heterozygous nonsense c.2961C>G (p.Tyr987Ter) variant of the KMT2C gene. [Read the Full Post]

Epigenetic targeting of Waldenström macroglobulinemia cells with BET inhibitors synergizes with BCL2 or histone deacetylase inhibition

286 views | Oct 04 2021

Stephan J Matissek et al. identified BET inhibitors as effective therapy for WM, and these inhibitors could be enhanced in combination with BCL2 or histone deacetylase inhibition. [Read the Full Post]

The imbalance of Th17/Treg via STAT3 activation modulates cognitive impairment in P. gingivalis LPS-induced periodontitis mice

425 views | Oct 03 2021

Xu Zhang et al. thought that the STAT3 signaling pathway might have immunoregulatory effects on the mouth-to-brain axis. [Read the Full Post]

A [3Fe-4S] cluster and tRNA-dependent aminoacyltransferase BlsK in the biosynthesis of Blasticidin S

674 views | Oct 03 2021

Xiankun Wang et al. provided an example of an iron-sulfur protein that catalyzed an aminoacyl-tRNA (aa-tRNA)-dependent amide bond formation in a natural product biosynthetic pathway. [Read the Full Post]

Nintedanib Regulates GRK2 and CXCR2 to Reduce Neutrophil Recruitment in Endotoxin-Induced Lung Injury

660 views | Oct 02 2021

Vincent Yi-Fong Su et al. found that the inhibition of adhesion molecules via the activation of GRK2 and the inhibition of p38 MAPK and CXCR2. [Read the Full Post]

Drugs repurposed for COVID-19 by virtual screening of 6,218 drugs and cell-based assay

358 views | Oct 01 2021

Woo Dae Jang et al. found that three drug combinations, omipalisib/remdesivir, tipifarnib/omipalisib, and tipifarnib/remdesivir, showed strong synergistic effects in inhibiting SARS-CoV-2. [Read the Full Post]

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