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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

SARS-CoV

An exonuclease-resistant chain-terminating nucleotide analogue targeting the SARS-CoV-2 replicase complex

37 views | Jan 24 2024

The modification of Bemnifosbuvir into the α-thiotriphosphate form, AT-9052-Sp, not only evades viral exonuclease-mediated resistance but also demonstrates a unique mechanism of immediate chain termination against SARS-CoV-2, offering a promising strategy for overcoming viral proofreading mechanisms in antiviral drug development. [Read the Full Post]

Phase II study of bemnifosbuvir in high-risk participants in a hospital setting with moderate COVID-19

38 views | Jan 24 2024

The study on bemnifosbuvir for moderate COVID-19, while not meeting its primary efficacy endpoint, demonstrated well-tolerance, absence of increased mortality, and a potential for reducing viral load, suggesting a promising avenue for further exploration in managing COVID-19 progression. [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]

Senescent immune cells accumulation promotes brown adipose tissue dysfunction during aging

65 views | Oct 11 2023

Bone marrow-derived senescent immune cells expressing S100A8 infiltrate brown adipose tissue during aging, compromising axon networks and thermogenic function, but treatment with an S100A8 inhibitor rejuvenates these functions in aged mice. [Read the Full Post]

Upgrading nirmatrelvir to inhibit SARS-CoV-2 Mpro via DeepFrag and free energy calculations

64 views | Sep 25 2023

The hybrid approach combining machine learning and free energy simulations proposed six modified compounds derived from nirmatrelvir, which exhibited enhanced electrostatic interaction free energy with SARS-CoV-2 Mpro and potentially reduced toxicity compared to the original inhibitor. [Read the Full Post]

Estimation of Intangible Costs for Factors Associated with Oral Antiviral Drugs for COVID-19 Treatment: A Conjoint Analysis in Japan

0 views | Sep 25 2023

This study conducted a conjoint analysis to estimate the intangible costs of factors associated with oral antiviral drugs for COVID-19 among the Japanese population, revealing preferences regarding the company, formulation, size, frequency of administration, infectiousness duration, and out-of-pocket expenses. [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]

Estimation of Intangible Costs for Factors Associated with Oral Antiviral Drugs for COVID-19 Treatment: A Conjoint Analysis in Japan

65 views | Sep 13 2023

This study conducted a conjoint analysis to estimate the intangible costs associated with factors of oral antiviral drugs for COVID-19 in Japan, revealing preferences such as a higher intangible cost for drugs developed by foreign companies and a lower cost for smaller sizes and tablets compared to larger sizes and capsules, respectively. [Read the Full Post]

Predicting the systemic exposure and lung concentration of nafamostat using physiologically-based pharmacokinetic modeling

111 views | Feb 18 2023

This study used a physiologically based pharmacokinetic (PBPK) approach and global sensitivity analysis to predict and evaluate the pharmacokinetic profiles of nafamostat in a virtual healthy population under various dosing regimens and found that the approach is valuable in predicting the PK profile and designing an appropriate dosage regimen for the treatment of COVID-19. [Read the Full Post]

The Novel h DHODH Inhibitor MEDS433 Prevents Influenza Virus Replication by Blocking Pyrimidine Biosynthesis

33 views | Dec 18 2022

Giulia Sibille et al. suggested MEDS433 as a potential HTA candidate to develop novel anti-IV intervention approaches, either as a single agent or in combination regimens with DAAs. [Read the Full Post]