piroxicam and Inflammation

This review stretches insight about the advancement (2011-2021) of synthesized non-heterocyclic, heterocyclic and natural occurring cyclic molecules for inflammation. While inflammation is very significant in the abolition of pathogens and other causes of soreness, a protracted inflammatory procedure takes to outcomes in chronic disease that might finally affect in organ failure or damage. Thus, restraining the provocative process by the use of anti-inflammatory agents is chief in controlling this damage. It also reveals other pursuit along with their anti-inflammatory activity. Molecular docking studies represent most suitable PDB (Protein Data Bank) ID for the synthesized heterocyclic molecules with their selective inhibitor. It discusses the findings presented in recent research papers and provides understanding to researchers intended for the growth of newer combinations/molecules having littler side things.

Topics: Animals; Anti-Inflammatory Agents; Dose-Response Relationship, Drug; Humans; Inflammation; Molecular Structure; Structure-Activity Relationship

Thienopyrimidine scaffold is a fused heterocyclic ring system that structurally can be considered as adenine, the purine base that is found in both DNA and RNA-bioisosteres. Thienopyrimidines exist in three distinct isomeric forms. The current review discusses thieno[2,3-d]pyrimidine as a one of the opulent heterocycles in drug discovery. Its broad range of medical applications such as anticancer, anti-inflammatory, anti-microbial, and CNS protective agents has inspired us to study its structure-activity relationship (SAR), along with its relevant synthetic strategies. The present review briefly summarizes synthetic approaches for the preparation of thieno[2,3-d]pyrimidine derivatives. In addition, the promising biological activities of this scaffold are also illustrated with explanatory diagrams for their SAR studies.

Topics: Anti-Infective Agents; Anti-Inflammatory Agents, Non-Steroidal; Antineoplastic Agents; Chemistry, Pharmaceutical; Humans; Inflammation; Neoplasms; Pyrimidines; Structure-Activity Relationship

Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease without any effective treatment. Protein TDP-43 is a pathological hallmark of ALS in both sporadic and familiar patients. Post-translational modifications of TDP-43 promote its aggregation in the cytoplasm. Tau-Tubulin kinase (TTBK1) phosphorylates TDP-43 in cellular and animal models; thus, TTBK1 inhibitors emerge as a promising therapeutic strategy for ALS. The design, synthesis, biological evaluation, kinase-ligand complex structure determination, and molecular modeling studies confirmed novel pyrrolopyrimidine derivatives as valuable inhibitors for further development. Moreover, compound

Topics: Amyotrophic Lateral Sclerosis; Animals; Brain; Case-Control Studies; DNA-Binding Proteins; Humans; Inflammation; Macrophages; Male; Mice; Mice, Inbred BALB C; Mice, Transgenic; Phosphorylation; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Rats; Rats, Wistar; Spinal Cord; Tissue Distribution

This protocol describes microsphere-based protease assays for use in flow cytometry and high-throughput screening. This platform measures a loss of fluorescence from the surface of a microsphere due to the cleavage of an attached fluorescent protease substrate by a suitable protease enzyme. The assay format can be adapted to any site or protein-specific protease of interest and results can be measured in both real time and as endpoint fluorescence assays on a flow cytometer. Endpoint assays are easily adapted to microplate format for flow cytometry high-throughput analysis and inhibitor screening.

Topics: Animals; Biotinylation; Flow Cytometry; Fluorescence Resonance Energy Transfer; Green Fluorescent Proteins; High-Throughput Screening Assays; Humans; Inflammation; Kinetics; Microspheres; Peptide Hydrolases; Peptides; Reproducibility of Results; Temperature