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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

Solute carrier-related signature for assessing prognosis and immunity in patients with clear-cell renal cell carcinoma

65 views | Oct 16 2023

The study identified a predictive signature consisting of eight SLC-related genes that have prognostic value in clear-cell renal cell carcinoma (ccRCC) and influence the immune microenvironment, highlighting potential treatment targets and providing insights into metabolic reprogramming in ccRCC. [Read the Full Post]

Synthesis, Anticancer, Antimicrobial and Antioxidant Potential of Novel 4-(Substituted phenyl-1,3,4-oxadiazol/thiadiazol-2-yl)-4-(4-substituted phenyl) Azetidin-2-One Derivatives

60 views | Oct 16 2023

The synthesized 4-substitutedphenyl-1,3,4-oxadiazol/Thiadiazol-2-yl)-4-(4-substitutedphenyl) azetidin-2-one derivatives demonstrated high efficacy against MCF-7 cancer cell lines, significant antimicrobial potential, and potent antioxidant activity, suggesting their potential for further research and development as therapeutic agents. [Read the Full Post]

Inhibition of ErbB3 and Associated Regulatory Pathways Potently Impairs Malignant Peripheral Nerve Sheath Tumor Proliferation and Survival

107 views | Oct 16 2023

The study identified erbB3, calmodulin, PIM kinases, and Src family members as potential therapeutic targets in MPNSTs and demonstrated that combinatorial therapies targeting these pathways are more effective in reducing proliferation and survival. [Read the Full Post]

Bioactive components and molecular mechanisms of Salvia miltiorrhiza Bunge in promoting blood circulation to remove blood stasis

177 views | Oct 16 2023

Salvia miltiorrhiza Bunge (SM) contains phenolic acids and tanshinones that synergistically target multiple signaling pathways to enhance blood circulation and alleviate blood stasis, making it an effective herbal medicine for the treatment of blood stasis syndrome. [Read the Full Post]

Coordination-Driven Self-Assembly of Biomedicine to Enhance Photodynamic Therapy by Inhibiting Proteasome and Bcl-2

75 views | Oct 16 2023

BSC, a self-delivery biomedicine formed through the coordination-driven self-assembly of BTZ, Sab, and Ce6, combines proteasome and Bcl-2 inhibitions with photodynamic therapy, exhibiting superior efficacy in tumor treatment and controlled drug release in the acidic tumor microenvironment. [Read the Full Post]

Novel targets and inhibitors of the Mycobacterium tuberculosis cytochrome bd oxidase to foster anti-tuberculosis drug discovery

47 views | Oct 15 2023

This review provides an overview of the structural, mechanistic, and inhibitory aspects of Mycobacterium tuberculosis cytochrome bd oxidase (cyt-bd), highlighting its potential as a target for the development of novel tuberculosis treatments. [Read the Full Post]

Knockdown screening of chromatin binding and regulatory proteins in zebrafish identified Suz12b as a regulator of tfpia and an antithrombotic drug target

141 views | Oct 15 2023

This study identified novel epigenetic regulators of the tfpia gene and demonstrated the potential of UNC6852 as an antithrombotic drug by enhancing tfpia mRNA levels and prolonging the time to occlude the caudal vessel after laser injury in zebrafish larvae and adults. [Read the Full Post]

BMP9-ID1 Signaling Activates HIF-1α and VEGFA Expression to Promote Tumor Angiogenesis in Hepatocellular Carcinoma

101 views | Oct 15 2023

The study indicates that targeting BMP9-ID1 signaling may serve as a promising therapeutic strategy for advanced hepatocellular carcinoma (HCC) by inhibiting angiogenesis. [Read the Full Post]

Mussel-inspired multifunctional surface through promoting osteogenesis and inhibiting osteoclastogenesis to facilitate bone regeneration

50 views | Oct 15 2023

This study developed a multifunctional bone repair scaffold coated with LYN and HA, which exhibited dual effects of promoting osteogenesis and inhibiting osteoclastogenesis, resulting in accelerated bone regeneration in both in vitro and in vivo experiments. [Read the Full Post]

Novel Allosteric Effectors Targeting Human Transcription Factor TEAD

93 views | Oct 15 2023

Chemical modifications of inhibitors targeting the palmitate-binding pocket in TEAD1-4 proteins have led to the discovery of allosteric inhibitors that enhance communication between TEAD4 and YAP1 domains, offering potential therapeutic strategies for solid tumors. [Read the Full Post]

VPS34-IN1 induces apoptosis of ER+ breast cancer cells via activating PERK/ATF4/CHOP pathway

151 views | Oct 14 2023

VPS34-IN1, a selective inhibitor of Class III Phosphatidylinositol 3-kinase (PI3K), exhibits an antitumor effect in estrogen receptor positive (ER+) breast cancer by activating the PERK/ATF4/CHOP pathway of endoplasmic reticulum (ER) stress to induce apoptosis in breast cancer cells. [Read the Full Post]

A phase 1b study of the allosteric extracellular FGFR2 inhibitor alofanib in patients with pretreated advanced gastric cancer

73 views | Oct 14 2023

Alofanib, a small-molecule allosteric extracellular FGFR2 inhibitor, showed acceptable tolerability and preliminary signs of clinical activity in heavily pretreated patients with advanced gastric cancer, with a recommended phase 2 dose of 350 mg/m2 administered 5 days on and 2 days off. [Read the Full Post]

PTK2B regulates immune responses of neutrophils and protects mucosal inflammation in ulcerative colitis

130 views | Oct 14 2023

Proline-rich tyrosine kinase 2B (PTK2B) plays a role in the pathogenesis of ulcerative colitis (UC) by promoting neutrophil migration and inhibiting mucosal inflammation, making it a potential therapeutic target for UC treatment. [Read the Full Post]

Capturing Differences in the Regulation of LRRK2 Dynamics and Conformational States by Small Molecule Kinase Inhibitors

71 views | Oct 14 2023

This study combines enhanced sampling simulations with HDX-MS to investigate the effects of type I and type II kinase inhibitors on the conformational dynamics and allosteric communications within the C-terminal domains of LRRK2, providing insights for the design of allosteric modulators that can regulate LRRK2 conformations and its interactions with other proteins. [Read the Full Post]

Potential New Therapeutic Approaches for Cisplatin-Resistant Testicular Germ Cell Tumors

98 views | Oct 14 2023

The proteasome inhibitor MG-132 shows promise as a potential new drug for treating cisplatin-resistant testicular germ cell tumors (TGCTs), enhancing sensitivity to cisplatin and inducing apoptosis in both parental and resistant cell lines. [Read the Full Post]

Inhibition of PIKFYVE kinase interferes ESCRT pathway to suppress RNA virus replication

67 views | Oct 13 2023

The inhibition of PIKFYVE kinase by YM201636 disrupts the ESCRT pathway and endosomal transport, leading to the repression of replication for various RNA viruses, offering potential antiviral therapy against RNA virus infections. [Read the Full Post]

ABCB1 and ABCG2 Overexpression Mediates Resistance to the Phosphatidylinositol 3-Kinase Inhibitor HS-173 in Cancer Cell Lines

71 views | Oct 13 2023

The study demonstrated that HS-173, a potent PI3K inhibitor, is susceptible to efflux mediated by ABCB1 and ABCG2 transporters, leading to decreased intracellular drug concentration and suggesting potential implications for its clinical use in multidrug-resistant cancers. [Read the Full Post]

Atypical Anti-Glomerular Basement Membrane Nephritis After the First Dose of the Severe Acute Respiratory Syndrome Coronavirus 2 mRNA Vaccine

100 views | Oct 13 2023

Atypical anti-GBM nephritis, which can occur after the administration of the SARS-CoV-2 mRNA vaccine, is characterized by linear IgG deposition in the glomerular basement membrane without circulating anti-GBM antibodies or lung involvement, and its response to immunosuppressive therapy is uncertain. [Read the Full Post]

Olverembatinib Treatment in Pediatric Patients With Relapsed Philadelphia-Chromosome-Positive Acute Lymphoblastic Leukemia

155 views | Oct 13 2023

In this study, olverembatinib demonstrated both safety and efficacy in children with relapsed Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL), including some achieving complete remission as a single agent. [Read the Full Post]

The Novel Cardiac Myosin Activator Danicamtiv Improves Cardiac Systolic Function at the Expense of Diastolic Dysfunction In Vitro and In Vivo: Implications for Clinical Applications

68 views | Oct 13 2023

Danicamtiv, a direct myosin activator, has demonstrated positive effects on cardiac systolic function but may impair diastolic performance, particularly at higher concentrations, indicating a need for cautious dosing and monitoring. [Read the Full Post]