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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

Clinicopathological Features and Outcomes of Granulosa Cell Tumor of the Ovaries - A Retrospective Study

63 views | Sep 22 2023

This retrospective analysis of granulosa cell tumors found that post-menopausal patients, advanced disease at presentation, and various factors related to surgical resection were associated with poorer outcomes, while the median disease-free survival was 60 months and overall survival was 62 months. [Read the Full Post]

Simultaneous quantitation of oxidized and reduced glutathione via LC-MS/MS to study the redox state and drug-mediated modulation in cells, worms and animal tissue

61 views | Sep 22 2023

This study presents an optimized LC-MS/MS method for quantifying GSH and GSSG levels in different biological matrices, offering high sensitivity and throughput for assessing oxidative stress and potential disease progression in toxicological research. [Read the Full Post]

Orthogonal dual reporter-based gain-of-signal assay for probing SARS-CoV-2 3CL protease activity in living cells: inhibitor identification and mutation investigation

78 views | Sep 22 2023

The researchers developed a dual reporter-based assay that measures the activity of the main protease of SARS-CoV-2, overcoming limitations of previous assays and identifying potential inhibitors while assessing the susceptibility of circulating variants. [Read the Full Post]

Metformin protects against retinal ischemia/reperfusion injury through AMPK-mediated mitochondrial fusion

60 views | Sep 22 2023

Metformin exhibits a protective effect against retinal ischemia/reperfusion (I/R) injury by promoting AMPK-mediated mitochondrial fusion and reducing mitochondrial reactive oxygen species (ROS) generation. [Read the Full Post]

Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo

55 views | Sep 22 2023

The study successfully developed Sulfopin, a nanomolar Pin1 inhibitor, which demonstrated potent target engagement, downregulation of c-Myc target genes, and therapeutic benefits in preclinical models of neuroblastoma and pancreatic cancer, highlighting Pin1 as a potential drug target for cancer treatment. [Read the Full Post]

Synergism of PARP inhibitor fluzoparib (HS10160) and MET inhibitor HS10241 in breast and ovarian cancer cells

145 views | Sep 21 2023

The study validated the synergistic effect of combining a selective MET inhibitor (HS10241) with a PARP inhibitor (HS10160) in eliminating triple-negative breast cancer (TNBC) and high-grade serous ovarian cancer (HGSOC) cells, suggesting its potential benefit for patients resistant to single-agent PARP inhibitor treatment. [Read the Full Post]

Atomic model for core modifying region of human fatty acid synthase in complex with Denifanstat

52 views | Sep 21 2023

Researchers have developed an engineered full-length human Fatty Acid Synthase (hFASN) protein, enabling the study of specific regions involved in fatty acid modification and providing insights for the design of small molecule inhibitors targeting hFASN in diseases such as diabetes, cancer, fatty liver diseases, and viral infections. [Read the Full Post]

The synthetic oleanane triterpenoid CDDO-2P-Im binds GRP78/BiP to induce unfolded protein response-mediated apoptosis in myeloma

175 views | Sep 21 2023

The study demonstrates that the synthetic oleanane triterpenoid 2P-Im induces apoptosis in multiple myeloma cells through activation of the unfolded protein response (UPR) and direct binding to the endoplasmic reticulum chaperone BiP (GRP78/BiP). [Read the Full Post]

Optimization of CAR-T Cell-Based Therapies Using Small-Molecule-Based Safety Switches

130 views | Sep 21 2023

Cutting-edge investigations are underway to develop small-molecule-based safety switches for CAR-T cells, enabling pharmacological control over their activities and toxicities to improve the safety and efficacy of CAR-T cell therapy for leukemia. [Read the Full Post]

Genome editing HLA alleles for a pilot immunocompatible hESC line in a Chinese hESC bank for cell therapies

113 views | Sep 21 2023

The study successfully customized an immunocompatible human embryonic stem cell (hESC) line based on Chinese HLA typing characteristics, providing a potential basis for establishing a universal HLA-AR bank of hESCs and expediting the clinical application of hESC-based therapies. [Read the Full Post]

Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction

53 views | Sep 20 2023

NHWD-870, a potent BET inhibitor, shows superior efficacy to current clinical stage inhibitors, suppressing tumor growth by downregulating c-MYC, inhibiting tumor cell proliferation, and blocking TAM proliferation through the suppression of CSF1 expression mediated by BRD4 inhibition and its target HIF1α. [Read the Full Post]

A Case of Dulaglutide-Induced Vaginal Bleed

74 views | Sep 20 2023

Severe vaginal bleeding, a rare side effect of Dulaglutide, was observed in a perimenopausal female with type 2 diabetes mellitus, underscoring the importance of post-market surveillance to identify uncommon adverse reactions not seen in clinical trials. [Read the Full Post]

Recent understandings about hypertension management in type 2 diabetes: What are the roles of SGLT2 inhibitor, GLP-1 receptor agonist, and finerenone?

66 views | Sep 20 2023

Managing blood pressure in patients with diabetes is crucial for preventing cardiovascular complications, and emerging drugs like GLP-1RA, SGLT2i, and finerenone have shown potential in both lowering blood pressure and providing cardio-renal protection. [Read the Full Post]

Discovery of the allosteric inhibitor from actinomyces metabolites to target EGFRCSTMLR mutant protein: molecular modeling and free energy approach

62 views | Sep 20 2023

The study identified compound C_42 as a potential drug candidate with strong binding affinity, favorable structural characteristics, and promising potential as an EGFR inhibitor for cancer treatment. [Read the Full Post]

Guidance on the management of adverse reactions induced by poly(ADP-ribose) polymerase inhibitors

155 views | Sep 20 2023

The common adverse reactions of PARP inhibitors, including hematological toxicity, gastrointestinal toxicity, and fatigue, can be managed through measures such as regular blood tests, referral to specialists, symptomatic treatment, and monitoring for potential complications. [Read the Full Post]

Development and Therapeutic Implications of Tyrosine Kinase 2 Inhibitors

114 views | Sep 19 2023

Selective TYK2 inhibitors, such as deucravacitinib and ropsacitinib, offer a promising approach for treating inflammatory and autoimmune diseases with improved efficacy and safety profiles compared to broad JAK inhibitors. [Read the Full Post]

Sono-Driven Sting Activation Using Semiconducting Polymeric Nanoagonists For Precision Sono-Immunotherapy of Head And Neck Squamous Cell Carcinoma

49 views | Sep 19 2023

This study presents a novel approach utilizing a semiconducting polymeric nanoagonist activated by ultrasound to trigger immunogenic cell death, release a STING agonist, and promote antitumor immunity for precise and effective treatment of head and neck squamous cell carcinoma. [Read the Full Post]

Mining the transcriptome of target tissues of autoimmune and degenerative pancreatic β-cell and brain diseases to discover therapies

43 views | Sep 19 2023

The study identified shared inflammatory gene signatures between pancreatic β-cells in diabetes and neuronal tissue in multiple sclerosis and Alzheimer's disease, and demonstrated the potential of bromodomain inhibitors as therapeutic candidates to revert these transcriptional signatures. [Read the Full Post]

FOXM1 augments sorafenib resistance and promotes progression of hepatocellular carcinoma by epigenetically activating KIF23 expression

53 views | Sep 19 2023

The study revealed that upregulation of FOXM1 in hepatocellular carcinoma (HCC) cells contributes to sorafenib resistance and HCC progression by increasing the expression of KIF23, and targeting FOXM1 could be an effective treatment strategy for HCC. [Read the Full Post]

Phospholipase D2 targeted by miR-5132-5p alleviates cerulein-induced acute pancreatitis via the Nrf2/NFκB pathway

130 views | Sep 19 2023

The study revealed that phospholipase D2 (PLD2), targeted by microRNA-5132-5p (miR-5132-5p), can attenuate cerulein-induced acute pancreatitis in AR42J cells by modulating the Nrf2/NFκB pathway, highlighting its potential as a therapeutic target for AP. [Read the Full Post]