Publications by authors named "Nirmal Jana"
Article Synopsis
- The PI3K pathway is essential for B-cell survival and is linked to B-cell cancers like DLBCL, with the overactivation of PI3Kδ being a significant factor.
- Small molecule inhibitors targeting PI3Kδγ, like LL-00084282, show promise in fighting DLBCL by demonstrating high potency and selectivity against this isoform while outperforming selective PI3Kδ inhibitors in cancer cell lines.
- LL-00084282 has shown effective results in vivo and exhibits good pharmacokinetic properties, indicating potential for future clinical trials in DLBCL patients and possible benefits in treating immunoinflammatory conditions.
PI3Kδ plays a critical role in adaptive immune cell activation and function. Suppression of PI3Kδ has been shown to counter excessive triggering of immune responses which has led to delineating the role of this isoform in the pathophysiology of autoimmune disorders. In the current study, we have described preclinical characterization of PI3Kδ specific inhibitor LL-00071210 in various rheumatoid arthritis models.
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- PI3Kδ inhibitors are used to treat B-cell malignancies, but existing options have limitations in potency, selectivity, and pharmacokinetics.
- Researchers developed a new inhibitor by improving the structure of an existing compound, transitioning from a "three-blade propeller" to a "four-blade propeller" design.
- The new compound shows superior effectiveness, selectivity, and stability, making it a promising candidate for treatment in various B-cell cancers, either alone or with other drugs.
[reaction: see text] In cases where both reactants in a phase-vanishing reaction are less dense than the fluorous phase, an alternative to the U-tube method is to employ a solvent with greater density than the fluorous phase, such as 1,2-dibromoethane. This modification has been successfully applied to the methylation of a phenol derivative with dimethyl sulfate and to the m-CPBA-induced epoxidation of alkenes, N-oxide formation from nitrogen-containing compounds, and S-oxide or sulfone formation from organic sulfides.
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