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ESKM, a novel therapeutic agent for sensitive and resistant PH+ leukemias

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

Blog of Signaling Pathways

FOXK1 Promotes Proliferation and Metastasis of Gallbladder Cancer by Activating AKT/mTOR Signaling Pathway

441 views | May 07 2020

Wencong M et al. suggested that FOXK1 promotes GBC cells progression and represent a novel prognostic biomarker and potential therapeutic target in GBC. [Read the Full Post]

Investigation of lncRNA H19 in prostate cancer cells and secreted exosomes upon androgen stimulation or androgen receptor blockage

396 views | May 06 2020

Ozgur E et al. provided evidence that H19 might be involved in androgen receptor pathway. [Read the Full Post]

A novel flow cytometry-based assay to measure compromised B cell receptor signaling as a prognostic factor in chronic lymphocytic leukemia

507 views | May 06 2020

Heitmann JS et al. supported the role of compromised BCR signaling as an important prognostic marker in CLL and establish a novel diagnostic tool for its assessment in clinical settings. [Read the Full Post]

Effects of nanoparticle-mediated delivery of pitavastatin on atherosclerotic plaques in ApoE-knockout mice and THP-1-derived macrophages

386 views | May 05 2020

Sun Y et al. demonstrated that pitavastatin-NP administration was more effective in attenuating the development of atherosclerotic plaques compared with systemic administration of pitavastatin. [Read the Full Post]

GSK-3 Inhibitors: A Double-Edged Sword? - An Update on Tideglusib

549 views | May 05 2020

Mathuram TL et al. concluded the emergence of GSK-3 inhibitors as a 'double-edged sword' in the treatment against human diseases cautioning researchers about the potential ramifications of off-target pharmacological effects. [Read the Full Post]

RO-3306 prevents postovulatory aging-mediated spontaneous exit from M-II arrest in rat eggs cultured in vitro

304 views | May 04 2020

Prasad S et al. resulted suggest that postovulatory aging destabilizes MPF by modulating specific phosphorylation of Cdk1 and cyclin B1 level. RO-3306 prevented these changes and maintained M-II arrest in rat eggs cultured in vitro. Hence, maintenance of M-II arrest in ovulated eggs using RO-3306 could be beneficial to increase the number of eggs available for various ART programs. [Read the Full Post]

Severe pyrexia from nivolumab-resistant advanced melanoma after successful combined therapy with encorafenib plus binimetinib.

0 views | May 04 2020

Amagai R et al. suggested that pyrexia caused by BRAF/MEK inhibitors may possess a similar pathophysiology as that of AOSD. [Read the Full Post]

Necrostatin-1 protects C2C12 myotubes from CoCl2-induced hypoxia

459 views | May 03 2020

Chen R et al. suggested that Nec‑1 protected C2C12 myotubes under conditions of CoCl2-induced hypoxia. [Read the Full Post]

Inhibiting PI3 kinase-γ in both myeloid and plasma cells remodels the suppressive tumor microenvironment in desmoplastic tumors

670 views | May 03 2020

Zhang X et al. concluded that IPI-549 NP delivery could be a promising method for treating pancreatic cancer and other immune-suppressive tumors. [Read the Full Post]

NVP-LDE-225 (Erismodegib) Inhibits Epithelial-Mesenchymal Transition and Human Prostate Cancer Stem Cell Growth in NOD/SCID IL2Rγ Null Mice by Regulating Bmi-1 and microRNA-128

717 views | Apr 30 2020

R Nanta et al. suggested that inhibition of the Shh signaling pathway could therefore be a novel therapeutic option in treating prostate cancer. [Read the Full Post]

NVP-LDE225, a Potent and Selective SMOOTHENED Antagonist Reduces Melanoma Growth in Vitro and in Vivo

500 views | Apr 30 2020

Ahmad Jalili et al. concluded that inhibition of SHH-GLI signaling pathway in human melanoma by the specific smoothened inhibitor NVP-LDE225 could have potential therapeutic application in human melanoma even in the absence of BRAF(V600E) mutation and warrants further investigations. [Read the Full Post]

Caspase-3 Inhibitor Z-DEVD-FMK Enhances Retinal Ganglion Cell Survival and Vision Restoration After Rabbit Traumatic Optic Nerve Injury

589 views | Apr 28 2020

Yuanyuan Liu et al. showed the caspase-3 inhibitor Z-DEVD-FMK is neuroprotective by inhibiting RGCs apoptosis when injected 30 min after optic nerve damage and significantly promotes restoration of vision. A controlled clinical trial is now needed to evaluate the efficacy and safety of Z-DEVD-FMK in humans. [Read the Full Post]

Ricolinostat, the First Selective Histone Deacetylase 6 Inhibitor, in Combination With Bortezomib and Dexamethasone for Relapsed or Refractory Multiple Myeloma

542 views | Apr 27 2020

Dan T Vogl et al. showed that at the recommended phase II dose of ricolinostat of 160 mg daily, the combination with bortezomib and dexamethasone is safe, well-tolerated, and active, suggesting that selective inhibition of HDAC6 is a promising approach to multiple myeloma therapy. [Read the Full Post]

Covalent CDK7 Inhibitor THZ1 Inhibits Myogenic Differentiation

333 views | Apr 27 2020

Xinqi Ma et al. indicated that THZ1 inhibits myogenic differentiation, suggesting that therapies based on THZ1 might have potential side effects on muscle functions. [Read the Full Post]

A First-in-Human Phase I Study of the Oral p38 MAPK Inhibitor, Ralimetinib (LY2228820 Dimesylate), in Patients With Advanced Cancer

375 views | Apr 26 2020

Amita Patnaik et al. demonstrated acceptable safety, tolerability, and pharmacokinetics for patients with advanced cancer. [Read the Full Post]

Characterization of LY2228820 Dimesylate, a Potent and Selective Inhibitor of p38 MAPK With Antitumor Activity

320 views | Apr 26 2020

Robert M Campbell et al. showed that LY2228820 is a p38 MAPK inhibitor, which has been optimized for potency, selectivity, drug-like properties (such as oral bioavailability), and efficacy in animal models of human cancer. [Read the Full Post]

YH25448, an Irreversible EGFR-TKI With Potent Intracranial Activity in EGFR Mutant Non-Small Cell Lung Cancer

1148 views | Apr 23 2020

Jiyeon Yun et al. suggested that YH25448 is a promising third-generation EGFR inhibitor, which may be more effective and better tolerated than the currently approved osimertinib. [Read the Full Post]

Safety and Antitumor Activity of Apalutamide (ARN-509) in Metastatic Castration-Resistant Prostate Cancer With and Without Prior Abiraterone Acetate and Prednisone

328 views | Apr 23 2020

Dana E Rathkopf et al. indicated that apalutamide was safe, well tolerated, and demonstrated clinical activity in mCRPC, with 80% of AAP-naïve and 43% of post-AAP patients, remaining on treatment for 6 months or longer. [Read the Full Post]

Design, Synthesis and Biological Evaluation of 2-amino-4-(1,2,4-triazol)pyridine Derivatives as Potent EGFR Inhibitors to Overcome TKI-resistance

542 views | Apr 22 2020

Haikui Yang et al. provided 2-amino-4-(1,2,4-triazol)pyridines as a new scaffold for EGFRT790M and/or EGFRvⅢ inhibitor. [Read the Full Post]

The Syk Inhibitor R406 Is a Modulator of P-glycoprotein (ABCB1)-mediated Multidrug Resistance

542 views | Apr 21 2020

George E Duran et al. indicated that the chemo-sensitizing effect of R406 in taxane-resistant cells previously reported was not associated with Syk but resulted from the modulation of P-gp-mediated MDR. [Read the Full Post]