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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

Activating JAK-mutations confer resistance to FLT3 kinase inhibitors in FLT3-ITD positive AML in vitro and in vivo

499 views | Nov 10 2020

Christoph Rummelt et al. characterized a novel mechanism of resistance to FLT3-ITD inhibition and might offer a potential therapy, using dual JAK and FLT3 inhibition. [Read the Full Post]

The CHK1 inhibitor MU380 significantly increases the sensitivity of human docetaxel-resistant prostate cancer cells to gemcitabine through the induction of mitotic catastrophe

226 views | Nov 09 2020

Stanislav Drápela et al. suggested that metabolically robust and selective CHK1 inhibitor MU380 could bypass docetaxel resistance and improve the effectiveness of GEM in DR mCRPC models. [Read the Full Post]

Phosphoproteomics Analysis Reveals a Potential Role of CHK1 in Regulation of Innate Immunity through IRF3

281 views | Nov 09 2020

Zhen Chen et al. indicated that the CHK1-dependent regulation of IRF3 phosphorylation at S173 and S175 might play a role in the induction of innate immune response after replication stress or DNA damage, which suggested a potential function of CHK1 in the innate immune response. [Read the Full Post]

Notoginseng Leaf Triterpenes Ameliorates OGD/R-Induced Neuronal Injury via SIRT1/2/3-Foxo3a-MnSOD/PGC-1 α Signaling Pathways Mediated by the NAMPT-NAD Pathway

424 views | Nov 07 2020

Weijie Xie et al. found that PNGL, as a new drug candidate, had a pivotal role in mitochondrial homeostasis and energy metabolism therapy via NAMPT against OGD-induced SH-SY5Y cell injury. [Read the Full Post]

Dehydrodiconiferyl alcohol, a lignan from Herpetospermum pedunculosum, alleviates cholestasis by activating pathways associated with the farnesoid X receptor

354 views | Nov 07 2020

Xiaodong Wei et al. thought that DA might represent an effective agonist for FXR had significant therapeutic potential for the treatment of cholestatic liver injury. [Read the Full Post]

A Preclinical Model for Studying Herpes Simplex Virus Infection

0 views | Nov 06 2020

Poojabahen Tajpara et al. discovered that both drugs had a comparable efficacy for inhibiting HSV-1 replication, suggesting that pritelivir could be an alternative therapeutic agent for patients infected with acyclovir-resistant strains. [Read the Full Post]

Pre-B cell colony enhancing factor induces Nampt-dependent translocation of the insulin receptor out of lipid microdomains in A549 lung epithelial cells

0 views | Nov 06 2020

Qianyi Peng et al. concluded that PBEF could inhibit insulin signaling through the IR by Nampt-dependent promotion of IR translocation into the nonraft domains of A549 epithelial cells. [Read the Full Post]

Characterisation of Ovarian Cancer Cell Line NIH-OVCAR3 and Implications of Genomic, Transcriptomic, Proteomic and Functional DNA Damage Response Biomarkers for Therapeutic Targeting

358 views | Nov 05 2020

Alice Bradbury et al. thought that NIH-OVCAR3 cells highlighted the complexity of HGSOCs and that genomic or functional characterization alone might not be enough to predict/explain chemotherapy response. [Read the Full Post]

Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: Efficacy of decitabine and valganciclovir alone or in combination

269 views | Nov 05 2020

Côme Thieulent et al. showed that deoxycytidine reverts the antiviral effect of decitabine, thus supporting some competition at the level of nucleoside phosphorylation by deoxycytidine kinase and/or DNA synthesis. [Read the Full Post]

Small molecule inhibitors provide insights into the relevance of LAT1 and LAT2 in materno-foetal amino acid transport

326 views | Nov 04 2020

Jonas Zaugg et al. thought that differential specificity of the applied inhibitors allowed for estimation of the contribution of LAT1 and LAT2 in materno-foetal AA transfer and their potential impact in pregnancy diseases associated with impaired foetal growth. [Read the Full Post]

Target inhibition of caspase-8 alleviates brain damage after subarachnoid hemorrhage

354 views | Nov 04 2020

Da-Qiang Ke et al. suggested that caspase-8 inhibition alleviated subarachnoid hemorrhage-induced brain injuries by suppressing inflammation. [Read the Full Post]

VDAC upregulation and αTAT1‑mediated α‑tubulin acetylation contribute to tanespimycin‑induced apoptosis in Calu‑1 cells

2111 views | Nov 02 2020

Qilin Wang et al. provided evidence for the use of a combination of drugs that target VDAC1 and tubulin to induce tumour cell apoptosis. [Read the Full Post]

Identification of Subtype-Specific Metastasis-Related Genetic Signatures in Sarcoma

785 views | Nov 02 2020

Ya-Ling Li et al. provided new insights into the pathogenesis, diagnosis, treatment, and prognosis of sarcomas and provided new directions for further study of sarcoma. [Read the Full Post]

Selective targeting of the αC and DFG-out pocket in p38 MAPK

527 views | Nov 01 2020

Sandra Röhm et al. provided valuable insights into back-pocket interactions that were not addressed in SR-318 and it provided an alternative chemical tool with good cellular activity targeting also the p38 back pocket. [Read the Full Post]

Targeting of BCR-ABL1 and IRE1α induces synthetic lethality in Philadelphia-positive acute lymphoblastic leukemia

0 views | Nov 01 2020

Margherita Vieri et al. found that the identified combined action of nilotinib and MKC-8866 might represent a successful therapeutic strategy in high-risk Ph + ALL. [Read the Full Post]

To inhibit TrxR1 is to inactivate STAT3-Inhibition of TrxR1 enzymatic function by STAT3 small molecule inhibitors

506 views | Oct 29 2020

Sander Busker et al. suggested that targeting of TrxR1 might be a common feature for many small molecules that inhibited cellular STAT3 function. [Read the Full Post]

Small molecule 2,3-DCPE induces S phase arrest by activating the ATM/ATR-Chk1-Cdc25A signaling pathway in DLD-1 colon cancer cells

674 views | Oct 29 2020

Bingjun Bai et al. suggested that 2,3-DCPE caused DNA damage in colon cancer cells and that 2,3-DCPE-induced S phase arrest was associated with the activation of the ATM/ATR-Chk1-Cdc25A pathway. [Read the Full Post]

Histone deacetylase 6 inhibition mitigates renal fibrosis by suppressing TGFß and EGFR signaling pathways in obstructive nephropathy

503 views | Oct 28 2020

Xingying Chen et al. indicated that HDAC6 inhibition could attenuate development of renal fibrosis by suppression of TGFb1 and EGFR signaling, and suggested that HDAC6 would be a potential therapeutic target for the treatment of renal fibrosis. [Read the Full Post]

EBV encoded miRNA BART8-3p promotes radioresistance in nasopharyngeal carcinoma by regulating ATM/ATR signaling pathway

327 views | Oct 28 2020

Xiaohan Zhou et al. indicated that EBV-miR-BART8-3p promoted radioresistance in NPC by modulating the activity of ATM/ATR signaling pathway. [Read the Full Post]

Cadmium induces apoptosis via generating reactive oxygen species to activate mitochondrial p53 pathway in primary rat osteoblasts

545 views | Oct 27 2020

Jiaming Zheng et al. indicated that Cd could induce apoptosis in osteoblasts by increasing the generation of ROS and activating the mitochondrial p53 signaling pathway, and this mechanism required the transcriptional activation of p53. [Read the Full Post]