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311.
Chandrabose Karthikeyan Pramod Jharia Digambar Kumar Waiker Amy Catherine Nusbaum Haneen Amawi Erin Marie Kirwen Ryann Christman Sri Krishna Chaitanya Arudra Laurent Meijer Amit K. Tiwari Piyush Trivedi 《Bioorganic & medicinal chemistry letters》2017,27(12):2663-2667
Described herein is the design, synthesis and biological evaluation of a series of N-(1H-pyrazol-3-yl)quinazolin-4-amines against a panel of eight disease relevant protein kinases. The kinase inhibition results indicated that two compounds inhibited casein kinase 1δ/ε (CK1δ/ε) with some selectivity over related kinases, namely CDK5/p25, GSK-3α/β, and DYRK1A. Docking studies with 3c and 3d revealed the key interactions with desired amino acids in the ATP binding site of CK1δ. Furthermore, compound 3c also elicited selective cytotoxic activity against the pancreas ductal adenocarcinoma (PANC-1) cell line. Taken together, the results of this study establish N-(1H-pyrazol-3-yl)quinazolin-4-amines especially 3c and 3d as valuable lead molecules with great potential for CK1δ/ε inhibitor development targeting neurodegenerative disorders and cancer. 相似文献
312.
We have cloned the cDNA coding the beta-tropomyosin of human muscle in an expression vector whose expression depends upon a promotor that can be induced by isopropyl-beta-thiogalactopyranoside. We show that a new protein was synthesized by bacteria containing the engineered plasmid. This protein was heat stable and reacted with antibodies against tropomyosin. We have purified this protein and further identified it by determining its amino acid composition and sequencing the NH2 terminal. Unlike the native muscle tropomyosin, the NH2 terminal is not acetylated and contains a methionine. The circular dichroism spectrum is compatible with 100% alpha-helices. These results show that the protein synthesized in E. coli possesses a native structure. 相似文献
313.
Sri Devi Sukumaran Shah Bakhtiar Nasir Jia Ti Tee Michael J. C. Buckle Rozana Othman Noorsaadah Abd. Rahman Vannajan Sanghiran Lee Syed Nasir Abbas Bukhari Chin Fei Chee 《Journal of enzyme inhibition and medicinal chemistry》2021,36(1):130
A series of C4-substituted tertiary nitrogen-bearing 2′-hydroxychalcones were designed and synthesised based on a previous mixed type acetylcholinesterase inhibitor. Majority of the 2′-hydroxychalcone analogues displayed a better inhibition against acetylcholinesterase (AChE) than butyrylcholinesterase (BuChE). Among them, compound 4c was identified as the most potent AChE inhibitor (IC50: 3.3 µM) and showed the highest selectivity for AChE over BuChE (ratio >30:1). Molecular docking studies suggested that compound 4c interacts with both the peripheral anionic site (PAS) and catalytic anionic site (CAS) regions of AChE. ADMET analysis confirmed the therapeutic potential of compound 4c based on its blood–brain barrier penetrating. Overall, the results suggest that this 2′-hydroxychalcone deserves further investigation into the therapeutic lead for Alzheimer’s disease (AD). 相似文献
314.
Issac Praveen Kumar Guru Ajay Chandrakumar Sri Snehaa Lite Christy Saraswathi N. T. Arasu Mariadhas Valan Al-Dhabi Naif Abdullah Arshad Aziz Arockiaraj Jesu 《Molecular biology reports》2020,47(9):6727-6740
Molecular Biology Reports - Understanding the mechanism by which the exogenous biomolecule modulates the GLUT-4 signalling cascade along with the information on glucose metabolism is essential for... 相似文献
315.
Stefania Pagliari Vladimir Vinarsky Fabiana Martino Ana Rubina Perestrelo Jorge Oliver De La Cruz Guido Caluori Jan Vrbsky Pamela Mozetic Antonio Pompeiano Andrea Zancla Sri Ganji Ranjani Petr Skladal Dan Kytyr Zbynk Zdrhal Gabriele Grassi Maurilio Sampaolesi Alberto Rainer Giancarlo Forte 《Cell death and differentiation》2021,28(4):1193
316.
Background
Sequence similarity between proteins is usually considered a reliable indicator of homology. Pyruvate-ferredoxin oxidoreductase and quinol-fumarate reductase contain ferredoxin domains that bind [Fe-S] clusters and are involved in electron transport. Profile-based methods for sequence comparison, such as PSI-BLAST and HMMer, suggest statistically significant similarity between these domains. 相似文献317.
D. Ballerini D. Parlouar M. Lapeyronnie K. Sri 《Applied microbiology and biotechnology》1977,4(1):1-9
Summary A mixed culture of bacteria MS1 capable of growth on methanol as its sole carbon-energy source was isolated by continuous culture with a minimum mineral salts medium and without asepsis. This bacterial association is composed of four Gram-negative bacterial strains which we identified. The respective numerical proportions of each microorganism are stable in time. The properties, and specially the stability of the continuous culture process have been studied with respect to substrate yield, biomass and productivity. 相似文献