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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

Radiation induces IRAK1 expression to promote radioresistance by suppressing autophagic cell death via decreasing the ubiquitination of PRDX1 in glioma cells

119 views | Jun 06 2023

The study found that overexpression of IRAK1 in glioma patients is associated with a poor prognosis, and that IRAK1 knockdown inhibits malignancy and enhances radiosensitivity by targeting the IRAK1-PRDX1 axis. [Read the Full Post]

Characterization of a Novel Milk-Clotting Aspartic Protease from Penicillium sp. and Structural Explanation for its High Milk-Clotting Index

138 views | Jun 06 2023

PsMCE is a novel milk-clotting enzyme with specific hydrolysis activity on κ-casein proteins and potential applications in cheese making due to its thermolability and high milk-clotting index value. [Read the Full Post]

Potential drug discovery for COVID-19 treatment targeting Cathepsin L using a deep learning-based strategy

40 views | Jun 06 2023

The study suggests that CTSL could be a promising therapeutic target for COVID-19, and the researchers used Chemprop to identify small molecules and FDA-approved drugs that can block CTSL activity, finding five molecules and drugs that can inhibit the activity of CTSL and inhibit the infection of both pseudotype and live SARS-CoV-2, including daptomycin. [Read the Full Post]

Protective Effect of Calpain Inhibition During Cold Ischemia on Ischemia-reperfusion Injury After Lung Transplantation

59 views | Jun 06 2023

The study showed that the administration of ALLN during cold ischemia improves IR lung injury in a lung transplant animal model by suppressing necroptosis. [Read the Full Post]

Canine distemper virus N protein induces autophagy to facilitate viral replication

93 views | Jun 06 2023

This study revealed that CDV N protein induces complete autophagy to facilitate viral replication, providing new insights into the interaction between CDV and the host autophagy machinery. [Read the Full Post]

Vascular lipid droplets formed in response to TNF, hypoxia, or OA: biochemical composition and prostacyclin generation

122 views | Jun 05 2023

The study investigates the role of lipid droplets (LDs) and adipose triglyceride lipase (ATGL)-dependent prostacyclin (PGI2) generation in the response of endothelial cells to proinflammatory stimuli, demonstrating that LDs formation and ATGL-mediated PGI2 generation represent a universal response to vascular proinflammatory insult. [Read the Full Post]

AdipoRon Engages Microglia to Antinociception through the AdipoR1/AMPK Pathway in SNI Mice

129 views | Jun 05 2023

AdipoRon may alleviate neuropathic pain by inhibiting microglia-derived TNF-α expression through the AdipoR1/AMPK pathway. [Read the Full Post]

Alpha-tocopherol enhances spermatogonial stem cell proliferation and restores mouse spermatogenesis by up-regulating BMI1

100 views | Jun 05 2023

This study investigates the role of BMI1 in spermatogonial stem cell proliferation and male reproduction, and demonstrates the potential modulatory effect of alpha-tocopherol on BMI1 both in vitro and in vivo. [Read the Full Post]

Identification of Embryonic Chicken Proteases Activating Newcastle Disease Virus and Their Roles in the Pathogenicity of Virus Used as In Ovo Vaccine

51 views | Jun 05 2023

The study identified five trypsin-like proteases that activate NDV in chicken embryos and found that the F protein with a 3B-FCS was crucial for the attenuation of NDV, providing a potential target for the rational design of safe in ovo ND vaccines. [Read the Full Post]

Phytochemical characterization, antioxidant activity and antihypertensive evaluation of Ocimum basilicum L. in l-NAME induced hypertensive rats and its correlation analysis

171 views | Jun 05 2023

The study found that Ocimum basilicum Linn. leaves extracts have potential as antihypertensive drugs due to their bioactive metabolites, with phenolic compounds playing a role in inhibiting l-Name induced hypertension and flavonoids contributing to antioxidant activities. [Read the Full Post]

The Class IIA Histone Deacetylase (HDAC) Inhibitor TMP269 Downregulates Ribosomal Proteins and Has Anti-Proliferative and Pro-Apoptotic Effects on AML Cells

77 views | Jun 04 2023

The study found that HDAC genes are overexpressed in AML patients and cell lines, and that TMP269, a class IIA HDAC inhibitor, has anti-leukemic activity when combined with venetoclax and may be a potential therapeutic drug for AML. [Read the Full Post]

A covalent inhibitor of K-Ras(G12C) induces MHC class I presentation of haptenated peptide neoepitopes targetable by immunotherapy

127 views | Jun 04 2023

The study demonstrates that covalent drugs that alkylate mutated residues on oncoproteins can generate unique MHC-I-restricted neoantigens, which can be targeted with a bispecific T cell engager construct to elicit a cytotoxic T cell response against cancer cells, including those resistant to direct inhibition. [Read the Full Post]

Blockade of STAT3/IL-4 overcomes EGFR T790M-cis-L792F-induced resistance to osimertinib via suppressing M2 macrophages polarization

62 views | Jun 04 2023

The study suggests that targeting the EGFR T790M-cis-L792F/STAT3 Tyr705/IL-4 pathway could be a potential strategy to suppress osimertinib resistance in NSCLC. [Read the Full Post]

From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors

142 views | Jun 04 2023

The passage describes the discovery of a potent BET inhibitor called 1q (SJ1461) through a CLICK chemistry-based approach, which shows improved profiles compared to existing BET inhibitors and has promising potential for further development as a cancer therapy. [Read the Full Post]

Inhibitor of Apoptosis Proteins Antagonist Induces T-cell Proliferation after Cross-Presentation by Dendritic Cells

60 views | Jun 04 2023

Researchers have identified AZD5582 as a compound that enhances dendritic cell cross-presentation of tumor antigens, leading to an increased frequency of systemic tumor antigen-specific CD8+ T cells, which could improve the clinical benefit of immune checkpoint blockade in patients who are unlikely to respond. [Read the Full Post]

Jmjd4 Facilitates Pkm2 Degradation in Cardiomyocytes and Is Protective Against Dilated Cardiomyopathy

92 views | Jun 03 2023

The study found that Jmjd4 plays a critical role in maintaining metabolic homeostasis in adult cardiomyocytes by degrading Pkm2 and its deficiency may lead to DCM, which suggests that targeting Jmjd4 and Pkm2 may be a potential therapeutic strategy for DCM and other cardiac diseases with metabolic dysfunction. [Read the Full Post]

PKM2/PDK1 dual-targeted shikonin derivatives restore the sensitivity of EGFR-mutated NSCLC cells to gefitinib by remodeling glucose metabolism

66 views | Jun 03 2023

The authors proposed a "two-step approach" to target both PKM2 and PDK1 simultaneously, and designed a novel PKM2/PDK1 dual-target agent E5, which showed promising anti-tumor activity and restored the sensitivity of EGFR-TKIs resistant NSCLC cells to gefitinib. [Read the Full Post]

KDELC2 Upregulates Glioblastoma Angiogenesis via Reactive Oxygen Species Activation and Tumor-Associated Macrophage Proliferation

134 views | Jun 03 2023

This study demonstrates that KDELC2 promotes glioblastoma angiogenesis via the activation of multiple pathways, including NLRP3 inflammasome, autophagy, ER stress, and TAM polarization. [Read the Full Post]

NDUFS3 knockout cancer cells and molecular docking reveal specificity and mode of action of anti-cancer respiratory complex I inhibitors

218 views | Jun 03 2023

This study highlights the need for cautious evaluation and dosage optimization of inhibitors targeting respiratory complex I in cancer treatment. [Read the Full Post]

Smad7 Is Highly Expressed in Human Degenerative Discs and Participates in IL-1 β-Induced Apoptosis of Rat AF Cells via the Mitochondria Pathway

64 views | Jun 03 2023

Smad7 participates in IL-1β-induced apoptosis of rat annulus fibrosus cells via the mitochondria pathway and may be a potential target for the prevention and treatment of degenerative disc disease. [Read the Full Post]