A5003455919- Peptidase Inhibition and Analysis
- Histone Deacetylase Inhibitors Research
- Chemical Synthesis and Analysis
- Alzheimer's disease research and treatments
- Catalytic Alkyne Reactions
- RNA Interference and Gene Delivery
- Telomeres, Telomerase, and Senescence
- Click Chemistry and Applications
- Advanced biosensing and bioanalysis techniques
- Parasites and Host Interactions
- Supramolecular Self-Assembly in Materials
- Catalytic C–H Functionalization Methods
- Protein Hydrolysis and Bioactive Peptides
- Pneumocystis jirovecii pneumonia detection and treatment
- Helminth infection and control
- Antimicrobial Peptides and Activities
- Drug Transport and Resistance Mechanisms
- Advanced Drug Delivery Systems
- Cholinesterase and Neurodegenerative Diseases
- Protein Degradation and Inhibitors
- Metal complexes synthesis and properties
- Signaling Pathways in Disease
- Parkinson's Disease Mechanisms and Treatments
- Synthesis and biological activity
- Catalytic Cross-Coupling Reactions
University of Siena
2019-2022
Purdue University West Lafayette
2022
National Institute of Pharmaceutical Education and Research
2016-2017
Indian Institute of Chemical Technology
2017
University of Hyderabad
2016-2017
Epigenetic regulation orchestrates many cellular processes and greatly influences key disease mechanisms. Histone deacetylase (HDAC) enzymes play a crucial role either as biomarkers or therapeutic targets owing to their involvement in specific pathophysiological pathways. Beyond well-characterized histone modifiers, HDACs also interact with several nonhistone substrates increased expression has been highlighted diseases. The HDAC6 isoform, due its unique cytoplasmic localization, modulates...
Idiopathic pulmonary fibrosis (IPF) is an interstitial lung disease characterized by a progressive-fibrosing phenotype. IPF has been associated with aberrant HDAC activities confirmed our immunohistochemistry studies on HDAC6 overexpression in tissues. We herein developed series of novel hHDAC6 inhibitors, having low inhibitory potency over hHDAC1 and hHDAC8, as potential pharmacological tools for treatment. Their was combined vitro vivo toxicity. Structural analysis 6h structure–activity...
AgSbF<sub>6</sub>-catalyzed domino aza-annulation/Diels–Alder/aromatization cascade for the construction of carbazoles, dihydrocarbazoles, tetrahydrocarbazoles and 3-indolyl-substituted was achieved.
Histone deacetylase inhibitors (HDACi) have emerged as promising therapeutics for the treatment of neurodegeneration, cancer, and rare disorders. Herein, we report development a series spiroindoline-based HDAC6 isoform-selective based on X-ray crystal studies hit 6a. We identified compound 6j most potent selective hHDAC6 inhibitor series. Biological investigation compounds 6b, 6h, demonstrated their antiproliferative activity against several cancer cell lines. Western blotting indicated that...
Schistosomiasis (also known as bilharzia) is a neglected tropical disease caused by platyhelminths of the genus Schistosoma. The endemic in and subtropical areas world where water infested intermediate parasite host, snail. More than 800 million people live more 200 are infected require treatment. Praziquantel (PZQ) drug choice for schistosomiasis treatment transmission control being safe very effective against adult worms all clinically relevant Schistosoma species. Unfortunately, it...
Pin1 catalyzes the cis-trans isomerization of pThr-Pro or pSer-Pro amide bonds various proteins involved in several physio/pathological processes. In this framework, recent research activity is directed toward identification new selective inhibitors. Here, we developed a set peptide-based Direct-binding experiments allowed inhibitor 5 k (methylacetyl-l-alanyl-l-histidyl-l-prolyl-l-phenylalaninate) as potent ligand Pin1. Notably, binds with higher affinity than Pin4. The comparative analysis...
Abstract The domino aza‐annulation/Diels—Alder cyclization of 2‐ene‐yne anilines (I) with acetylenedicarboxylate leads to desired carbazoles (III).
Type 2 Diabetes Treatment In article 2101301, Fortin and co-workers study transmission electron microscopy images of mature human islet amyloid polypeptide (IAPP) fibrils. Dense intertwined fibrils resulted from the incubation synthetic IAPP at a concentration 10 μM in mM phosphate buffered saline (control). was co-incubated room temperature for 12 h with or without resveratrol compound-to-protein ratio 10:1. Resveratrol reduced fibril formation.