Blog of Signaling Pathways

Structural Biology Insight for the Design of Sub-type Selective Aurora Kinase Inhibitors

464 views | Mar 12 2021

Sailu Sarvagalla et al. found that a possible means to develop sub-type selective inhibitor was by targeting Aurora A specific residues (Leu215, Thr217 and Arg220) or Aurora B specific residues (Arg159, Glu161 and Lys164), near the solvent exposed region of the protein. [Read the Full Post]

Sirtuin 1 and Sirtuin 3 in Granulosa Cell Tumors

408 views | Mar 12 2021

Nina Schmid et al. found that several SIRTs were expressed by GCTs, and SIRT1 and SIRT3 were involved in the growth regulation of KGN. [Read the Full Post]

Hypoxic targeting and activating TH-302 loaded transcatheter arterial embolization microsphere

380 views | Mar 11 2021

Pengkai Ma et al. found that TH-302 microspheres showed to be feasible and effective for TACE and hold promise in the clinical for HCC chemoembolization therapy. [Read the Full Post]

A screening-based approach identifies cell cycle regulators AURKA, CHK1 and PLK1 as targetable regulators of chondrosarcoma cell survival

394 views | Mar 11 2021

Yvonne de Jong et al. thought that AURKA, CHK1 and PLK1 were identified as important survival genes in chondrosarcoma cell lines. [Read the Full Post]

The effect of ivermectin alone and in combination with cobicistat or elacridar in experimental Schistosoma mansoni infection in mice

377 views | Mar 10 2021

Belén Vicente et al. thought that even in the presence of pharmacological inhibition of P-glycoprotein or cytochrome P450 3A, did not result in effective prophylaxis for S. mansoni infection in an experimental murine model. [Read the Full Post]

Hypoxia-induced CREB cooperates MMSET to modify chromatin and promote DKK1 expression in multiple myeloma

314 views | Mar 10 2021

Yinyin Xu et al. found that hypoxia and a cytogenetic abnormality regulated DKK1 expression in myeloma cells, and provided an additional rationale for the development of therapeutic strategies that interrupted DKK1 to cure MM. [Read the Full Post]

4-hydroxytamoxifen does not deteriorate cardiac function in cardiomyocyte-specific MerCreMer transgenic mice

497 views | Mar 09 2021

Andre Heinen et al. investigated potential adverse effects of DNA editing by the αMHC-MerCreMer/loxP system in combination with a low-dose treatment protocol with the tamoxifen metabolite 4-hydroxytamoxifen (OH-Txf). [Read the Full Post]

Optimization of dose and route of administration of the P-glycoprotein inhibitor, valspodar (PSC-833) and the P-glycoprotein and breast cancer resistance protein dual-inhibitor, elacridar (GF120918) as dual infusion in rats

389 views | Mar 09 2021

Christopher Rowbottom rt al. demonstrated that doses greater than 0.9 mg/hr/kg valspodar and 8.9 mg/hr/kg elacridar were sufficient to inhibit P-gp- and BCRP-mediated efflux at the blood-brain barrier in rats without any tolerability issues. [Read the Full Post]

Sublethal irradiation promotes the metastatic potential of hepatocellular carcinoma cells

354 views | Mar 08 2021

Yulin Cao et al. indicated that MMP-8 secreted by irradiated NPCs enhanced the migration and invasion of HCC by regulating AMPK/mTOR signaling, revealing a novel mechanism mediating sublethal irradiation-induced HCC metastasis at the level of the tumor microenvironment. [Read the Full Post]

Effect of Eriocalyxin B on prostatic inflammation and pelvic pain in a mouse model of experimental autoimmune prostatitis

615 views | Mar 08 2021

Li-Gang Zhang et al. suggested that EriB could alleviate the severity of prostatic inflammation and pelvic pain in an EAP mouse model. [Read the Full Post]

Differential Outcomes in Codon 12/13 and Codon 61 NRAS-Mutated Cancers in the Phase 2 NCI-MATCH Trial of Binimetinib in Patients with NRAS-Mutated Tumors

525 views | Mar 07 2021

James M Cleary et al. thought that the observation of increased OS and PFS in codon 61 NRAS-mutated colorectal cancer patients merited further investigation. [Read the Full Post]

Mnk inhibitors: a patent review

1276 views | Mar 07 2021

Ahmed M Abdelaziz et al. provided a succinct review of the current state of development of pyridone-aminal-derived Mnk inhibitors through the analysis of relevant patent applications filed in the last 5 years. [Read the Full Post]

Kinesin-7 CENP-E regulates the formation and structural maintenance of the acrosome

496 views | Mar 06 2021

Zhen-Yu She et al. found that light on the molecular mechanisms involved in vesicle trafficking and architecture maintenance of the acrosome. [Read the Full Post]

Immediate Effect of Baricitinib on Arthritis and Biological Disease-Modifying Antirheumatic Drug-Induced Psoriasis-Like Skin Lesions in Two Patients with Rheumatoid Arthritis

805 views | Mar 05 2021

Yoshifumi Tada et al. found that baricitinib was initiated because of RA flare and resulted in immediate beneficial effects on arthritis as well as skin lesions. [Read the Full Post]

Comparison of Treatment Effect and Tolerance of the Topical Application of Mizoribine and Cyclosporine A in a Mouse Dry Eye Model

710 views | Mar 05 2021

Xiang Lin et al. found that MZR (0.05% in PBS) could be a good competitive product for Restasis because of the comparable treatment effect in dry eye diseases and better ocular tolerability in ocular itch and pain. [Read the Full Post]

PLK1 inhibition sensitizes breast cancer cells to radiation via suppressing autophagy

330 views | Mar 04 2021

Baiyao Wang et al. indicated that PLK1 inhibition enhanced the radiosensitivity of breast cancer cells in a manner associated with the suppression of radiation-induced autophagy. [Read the Full Post]

In-vitro evaluation of the immunomodulatory effects of baricitinib: implication for COVID-19 therapy

835 views | Mar 04 2021

Linda Petrone et al. found that exogenous addition of baricitinib decreased the in-vitro SARS-CoV-2-specific response in COVID-19 patients using a whole-blood platform. [Read the Full Post]

Oncogenic activation of JAK3-STAT signaling confers clinical sensitivity to PRN371, a novel selective and potent JAK3 inhibitor, in natural killer/T-cell lymphoma

331 views | Mar 03 2021

M -L Nairismägi found that the activity of PRN371 had a more durable inhibition on JAK3 compared to tofacitinib in vitro, leading to significant tumor growth inhibition in a NKTL xenograft model harboring JAK3 activating mutation. [Read the Full Post]

Manipulating bovine granulosa cell energy metabolism limits inflammation

703 views | Mar 03 2021

Anthony D Horlock et al. implied that energy stress compromised ovarian follicle immune defences. [Read the Full Post]

CBP Bromodomain Inhibition Rescues Mice From Lethal Sepsis Through Blocking HMGB1-Mediated Inflammatory Responses

358 views | Mar 02 2021

Xiaowen Bi et al. suggested that CBP bromodomain could serve as a candidate therapeutic target for the treatment of lethal sepsis via inhibiting LPS-induced expression and release of HMGB1 and suppressing the pro-inflammatory activity of HMGB1. [Read the Full Post]