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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

DUB

MitoCur-1 induces ferroptosis to reverse vemurafenib resistance in melanoma through inhibition of USP14

44 views | Jan 16 2024

The discovery of MitoCur-1's ability to inhibit USP14 and induce ferroptosis presents a promising avenue for reversing vemurafenib resistance in melanoma, potentially transforming treatment outcomes for patients. [Read the Full Post]

Inhibition of USP2 Enhances TRAIL-Mediated Cancer Cell Death through Downregulation of Survivin

45 views | Jan 06 2024

The study reveals that targeting Ubiquitin-specific protease 2 (USP2) using the inhibitor ML364 enhances TNF-related apoptosis-inducing ligand (TRAIL)-induced cancer cell death selectively by promoting ubiquitination and degradation of survivin, offering a potential avenue for targeted cancer therapies. [Read the Full Post]

Entropy driven cooperativity effect in multi-site drug optimization targeting SARS-CoV-2 papain-like protease

59 views | Nov 28 2023

The study investigated the enhanced binding affinity between the papain-like protease (PLpro) of SARS-CoV-2 and the existing drug GRL0617, revealing that optimization of specific regions in the drug led to increased cooperativity by stabilizing key residues and reducing entropic loss, providing valuable insights for drug development strategies targeting PLpro. [Read the Full Post]

Ubiquitin-specific protease 20 in human disease: Emerging role and therapeutic implications

49 views | Nov 22 2023

The discovery of USP20's diverse physiological roles, including its involvement in metabolic disorders and neurological diseases, alongside the development of specific inhibitors like GSK2643943A, highlights its potential as a valuable therapeutic target for a wide array of diseases. [Read the Full Post]

Selective USP7 inhibition elicits cancer cell killing through a p53-dependent mechanism

80 views | Oct 10 2023

XL177A, a potent and selective USP7 inhibitor, demonstrates p53-dependent growth suppression and TP53 mutational status as a potential biomarker for response, showing promise as a targeted therapeutic agent in cancer, including pediatric cancers such as Ewing sarcoma and malignant rhabdoid tumor. [Read the Full Post]

Combined inhibition of XIAP and autophagy induces apoptosis and differentiation in acute myeloid leukaemia

97 views | Jul 03 2023

In acute myeloid leukemia (AML), the inhibition of X-linked inhibitor of apoptosis (XIAP) induces autophagy, apoptosis, and differentiation, and combining XIAP inhibition with autophagy inhibition shows promise as a therapeutic strategy for AML. [Read the Full Post]

USP1 promotes the aerobic glycolysis and progression of T-cell acute lymphoblastic leukemia via PLK1/LDHA axis

57 views | Jun 13 2023

The study demonstrated that the upregulation of deubiquitinase USP1 in pediatric T-ALL correlated with poor prognosis, and its inhibition attenuated glycolytic metabolism and cellular proliferation, suggesting USP1 as a promising therapeutic target. [Read the Full Post]

Patients with infective endocarditis undergoing cardiac surgery have distinct ROTEM profiles and more bleeding complications compared to patients without infective endocarditis

155 views | May 24 2023

This exploratory investigation found significantly altered coagulation profiles in patients with infective endocarditis, with concomitant hyper- and hypocoagulability, leading to increased bleeding complications and transfusion requirements, and suggests the need for adjustments to existing coagulation management algorithms in these high-risk patients. [Read the Full Post]

Administration of USP7 inhibitor P22077 inhibited cardiac hypertrophy and remodeling in Ang II-induced hypertensive mice

50 views | May 24 2023

USP7 may be a new therapeutic target for hypertrophic remodeling and heart failure due to its involvement in multiple signaling pathways that contribute to cardiac hypertrophy and remodeling. [Read the Full Post]

Ubiquitin-Specific Proteases as Potential Therapeutic Targets in Bladder Cancer-In Vitro Evaluation of Degrasyn and PR-619 Activity Using Human and Canine Models

84 views | May 23 2023

The study found that Degrasyn showed greater anti-cancer activity against bladder cancer cell lines compared to the non-selective DUB inhibitor PR-619, inducing caspase-dependent apoptosis and triggering DNA damage. [Read the Full Post]