A5057292937- Synthesis and biological activity
- Computational Drug Discovery Methods
- Cancer therapeutics and mechanisms
- Antibiotic Resistance in Bacteria
- Crop Yield and Soil Fertility
- Bacterial Genetics and Biotechnology
- Photosynthetic Processes and Mechanisms
- Andrographolide Research and Applications
- Natural Antidiabetic Agents Studies
- Pharmacological Effects of Natural Compounds
- Microtubule and mitosis dynamics
- DNA and Nucleic Acid Chemistry
- Plant biochemistry and biosynthesis
- Malaria Research and Control
- Tuberculosis Research and Epidemiology
- Vibrio bacteria research studies
- RNA and protein synthesis mechanisms
- Endoplasmic Reticulum Stress and Disease
- Essential Oils and Antimicrobial Activity
- CRISPR and Genetic Engineering
- Insect and Pesticide Research
- Moringa oleifera research and applications
- Agricultural Science and Fertilization
- Allelopathy and phytotoxic interactions
- Botany, Ecology, and Taxonomy Studies
Swami Keshwanand Rajasthan Agricultural University
2021-2024
Maharishi Markandeshwar University, Mullana
2018-2024
Sri Karan Narendra Agriculture University, Jobner
2024
Guru Nanak Dev University
2024
Academy of Scientific and Innovative Research
2022
University of America
2022
Catholic University of America
2022
Institute of Genomics and Integrative Biology
2021-2022
National Institute of Pharmaceutical Education and Research
2022
University of Jammu
2022
Abstract The essential mitotic kinase Aurora A (AURKA) is controlled during cell cycle progression via two distinct mechanisms. Following activation loop autophosphorylation early in mitosis when it localizes to centrosomes, AURKA allosterically activated on the spindle binding microtubule-associated protein, TPX2. Here, we report discovery of AurkinA, a novel chemical inhibitor AURKA-TPX2 interaction, which acts an unexpected structural mechanism inhibit activity and localization. In...
Mycobacterium tuberculosis (Mtb) endures a combination of metal scarcity and toxicity throughout the human infection cycle, contributing to complex clinical manifestations. Pathogens counteract this paradoxical dysmetallostasis by producing specialized trafficking systems. Capture extracellular siderophores is widely accepted mode iron acquisition, Mtb iron-chelating siderophores, mycobactin, have been known since 1965. Currently, it not whether produces zinc scavenging molecules. Here, we...
Abstract The thiol‐disulfide oxidoreductase enzyme DsbA catalyzes the formation of disulfide bonds in periplasm Gram‐negative bacteria. substrates include proteins involved bacterial virulence. In absence DsbA, many these do not fold correctly, which renders bacteria avirulent. Thus is a critical mediator virulence and inhibitors may act as antivirulence agents. Biophysical screening has been employed to identify fragments that bind from Escherichia coli . Elaboration one produced compounds...
Chitin is a major structural polysaccharide after cellulose and exists as the most abundant polymer in nature. nitrogen-containing homopolymer of β-(1,4) linked N-Acetylglucosamine. It key cell wall component fungi, also found wide range organisms, including viruses, plants, animals, insect exoskeletons, crustacean shells. This review focused on recent developments applications chitin, chitinases, chitin derivatives biomedicinal, agricultural environmental perspectives for sustainable...
Oxidative protein folding in Gram-negative bacteria results the formation of disulfide bonds between pairs cysteine residues. This is a multistep process which dithiol-disulfide oxidoreductase enzyme, DsbA, plays central role. The structure DsbA comprises an all helical domain unknown function and thioredoxin domain, where active site cysteines shuttle oxidized, substrate-bound, reduced form DsbB-bound form, DsbB membrane that reoxidizes DsbA. Most enzymes interact with wide variety...
The contributions of phenotypic plasticity to photosynthetic performance in winter (cv Musketeer, cv Norstar) and spring SR4A, Katepwa) rye (Secale cereale) wheat (Triticum aestivum) cultivars grown at either 20°C [non-acclimated (NA)] or 5°C [cold acclimated (CA)] were assessed. 22-40% increase light-saturated rates CO₂ assimilation CA vs NA cereals accounted for by as indicated the dwarf phenotype increased specific leaf weight. However, could not account (1) differential temperature...
A-type lamins encoded by LMNA form a structural fibrillar meshwork within the mammalian nucleus. How this nuclear organization may influence execution of biological processes involving DNA transactions remains unclear. Here, we characterize changes in dynamics and biochemical interactions lamin A/C after damage. We find that breakage reduces mobility nucleoplasmic GFP-lamin A throughout nucleus as measured dynamic fluorescence imaging spectroscopy living cells, suggestive incorporation into...
DsbA catalyzes disulfide bond formation in secreted and outer membrane proteins bacteria. In pathogens, is a major facilitator of virulence constituting target for antivirulence antimicrobial development. However, many pathogens encode multiple diverse enzymes factor folding during infection. The aim this study was to determine whether our recently identified inhibitors Escherichia coli K-12 can inhibit the found two important human attenuate their virulence.DsbA from chemical classes...
Capsazepine, an antagonist of capsaicin, is discovered by the structure and activity relationship. In previous studies it has been found that capsazepine potency for immunomodulation anti-inflammatory emerging as a favourable target in quest efficacious safe drug. Thus, 2D quantitative structural relationship (QSAR) model against tumor necrosis factor-α (TNF-α) was developed using multiple linear regression method (MLR) with good internal prediction (r2 = 0.8779) external (r2pred 0.5865)...
To screen the active antimalarial novel artemisinin derivatives, a QSAR modeling approach was used. model showed high correlation (r(2)= 0.83 and rCV(2)= 0.81) indicated that Connectivity Index (order 1, standard), 2, Dipole Moment (debye), Vector X (debye) LUMO Energy (eV) well correlate with activity. High binding likeness on target plasmepsin detected through molecular docking. Active derivatives significant activity compliance standard parameters of oral bioavailability ADMET. The...
Naringenin is a powerful antioxidant and anti-inflammatory flavonoid which has been widely used as therapeutic agent in various toxic models. However, few studies have clearly discussed the neuromodulatory effects of naringenin against different neurodegenerative disorders.We investigated neuroprotective efficacy 3-nitropropionic acid (3-NP)-induced neurobehavioral, biochemical histopathological alterations rats.Albino Wistar rats were randomly divided into three experimental groups. Group...
As part of our drug discovery program for anti-filarial agents from Indian medicinal plants, leaves Eucalyptus tereticornis were chemically investigated, which resulted in the isolation and characterization an agent, ursolic acid (UA) as a major constituent. Antifilarial activity UA against human lymphatic filarial parasite Brugia malayi using vitro vivo assays, silico docking search on glutathione-s-transferase (GST) parasitic enzyme carried out. The was lethal to microfilariae (mf; LC100:...
The enzyme TcpG is a periplasmic protein produced by the Gram-negative pathogen Vibrio cholerae. essential for production of ToxR-regulated proteins, including virulence-factor pilus proteins and cholera toxin, therefore target development new class anti-virulence drugs. Here, 1.2 Å resolution crystal structure reported using cryocooled crystal. This compared with previous determined at 2.1 from data measured room temperature. first DsbA to be solved sufficiently high allow inclusion refined...
A series of new andrographolide‐1,2,3‐triazole derivatives, 3a , 3b 3c 3d 3e 3f 3g 3h 3i 3j 3k were synthesized from a natural bioactive labdane type diterpenoid, andrographolide. All the derivatives screened against human cancer cell lines MCF7, MDA‐MB‐231, COLO205, HepG2, K562, Hela, and HEK293 to evaluate their cytotoxic activity. compounds showed anticancer activity selectively K562 line, with IC 50 values ranging 8.00 17.11 µ M are inactive rest lines. Compounds significant cytotoxicity...
C-Jun N-terminal kinase (JNK) is a therapeutic target for inhibitors which may provide clinical benefit in the pathogenesis of rheumatoid arthritis (RA) as well various apoptosis-related disorders. The benzothiazol-2-yl acetonitrile derivatives, recently reported by Pascale et al. (J. Med. Chem. 2005, 48, 4596−4607), are first generation JNK this class. To understand inhibitory mechanisms and elucidate pharmacophoric properties these derivatives molecular docking 3D-QSAR studies were...