Development of Liposome Systems for Enhancing the PK Properties of Bivalent PROTACs

Autor: Ponien Kou, Elizabeth S. Levy, An D. Nguyen, Donglu Zhang, Shu Chen, Yusi Cui, Xing Zhang, Fabio Broccatelli, Jennifer Pizzano, Jennifer Cantley, Elizabeth Bortolon, Emma Rousseau, Michael Berlin, Peter Dragovich, Vijay Sethuraman

Publikováno v: Pharmaceutics, Vol 15, Iss 8, p 2098 (2023)

Proteolysis-Targeting Chimeras (PROTACs) are a promising new technology in drug development. They have rapidly evolved in recent years, with several of them in clinical trials. While most of these advances have been associated with monovalent protein

Externí odkaz: https://doaj.org/article/8e4f9f68f9ea427e99c4b7d4b7e93010

Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria

Autor: David McKenney, Louis E. Metzger, Dirksen E. Bussiere, Sylvia Ma, Ashish Patel, Bhavesh Dhumale, Upendra Kulkarni, Jay Parthiban Lakshman, Sean King, Duncan Armstrong, Kyuto Tashiro, Lauren Kossy, Tushar Patel, Lauren M. Holder, Jogitha Selvarajah, Sarah Williams, Satya Yendluri, Colin Osborne, Jason Vo, Mangesh Fulsunder, Xiaolan Ling, Laura Wedel, Gianfranco De Pascale, Jennifer A. Leeds, Cody Cepura, Heinz E. Moser, Alexey Rivkin, Sunil Namballa, Colin K. Skepper, Bhavin Kantariya, Mina Mostafavi, Bhautik Savani, Anatoli Lvov, Guillaume Lapointe, Cornelia Bellamacina, Bhavesh Vora, Daryl L. Richie, Helen Chan, Wosenu Mergo, Jianwei Bian, Wei Shu, Keshav Mhaske, Aregahegn Yifru, Mark R. Sanderson, Swapnil Malekar, Johanne Blais, Qin Yue, Yong Zhang, Katherine V. Thompson, Julie Kim, Charles R. Dean, Vijay Sethuraman, Trixie Wagner, L. Mark Fisher, Dennis A. Veselkov, Darshit Patel, Folkert Reck, Jonas Noeske, Krishniah Vaarla, Lakhan Vala, Shailesh Satasia, Krunal Prajapati, Philippe Piechon, Valery Polyakov, Katherine R Prosen

Publikováno v: Lapointe, G, Skepper, C K, Holder, L M, Armstrong, D, Bellamacina, C, Blais, J, Bussiere, D, Bian, J, Cepura, C, Chan, H, Dean, C R, De Pascale, G, Dhumale, B, Fisher, L M, Fulsunder, M, Kantariya, B, Kim, J, King, S, Kossy, L, Kulkarni, U, Lakshman, J, Leeds, J A, Ling, X, Lvov, A, Ma, S, Malekar, S, McKenney, D, Mergo, W, Metzger, L, Mhaske, K, Moser, H E, Mostafavi, M, Namballa, S, Noeske, J, Osborne, C, Patel, A, Patel, D, Patel, T, Piechon, P, Polyakov, V, Prajapati, K, Prosen, K R, Reck, F, Richie, D L, Sanderson, M R, Satasia, S, Savani, B, Selvarajah, J, Sethuraman, V, Shu, W, Tashiro, K, Thompson, K V, Vaarla, K, Vala, L, Veselkov, D A, Vo, J, Vora, B, Wagner, T, Wedel, L, Williams, S L, Yendluri, S, Yue, Q, Yifru, A, Zhang, Y & Rivkin, A 2021, ' Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria ', Journal of Medicinal Chemistry, vol. 64, no. 9, pp. 6329-6357 . https://doi.org/10.1021/acs.jmedchem.1c00375

Herein, we describe the discovery and optimization of a novel series that inhibits bacterial DNA gyrase and topoisomerase IV via binding to, and stabilization of, DNA cleavage complexes. Optimization of this series led to the identification of compou

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56db96726415696056387173baa99222
https://kclpure.kcl.ac.uk/en/publications/675d57ab-71d9-4244-886c-019cc57306cd

Co-crystal formation based on structural matching

Autor: Vijay Sethuraman, Riccardo Panicucci, Liping Zhou, Stephanie Kay Dodd, Christina Capacci-Daniel, Sudhakar Garad

Publikováno v: European Journal of Pharmaceutical Sciences. 88:191-201

A co-crystal is defined as a single crystalline structure composed of two or more components with no proton transfer which are solid at room temperature. Our group has come up with the following rationale selection of co-formers for initial co-crysta

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::889a109f358aa03f20606807cdb862a2
https://doi.org/10.1016/j.ejps.2016.02.017

Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers

Autor: Yan Lou, Sharadha Subramanian, Yingyun Wang, Lifeng Wan, John Tellew, Laura Tandeske, Benjamin R. Taft, Kalyani Gampa, Jacob R. Haling, Gisele Nishiguchi, Lina Setti, Alice Rico, Sylvia Ma, Payman Amiri, Mallika Singh, Huw Tanner, Brent A. Appleton, Robert J. Aversa, Sepideh Vaziri, Shenlin Huang, Johanna M. Jansen, Anne Van Abbema, Jing Yuan, Vesselina G. Cooke, Hanne Merritt, Aaron Smith, Wenlin Shao, Valery Polyakov, Fei Feng, Savithri Ramurthy, Matthew Burger, Mulugeta Mamo, Lesley A. Mathews Griner, Vijay Sethuraman, Victoriano Tamez, Michael Patrick Dillon, Emma Lees, Ina Dix, Paul A. Barsanti, Richard Zang, Darrin Stuart, Mohammad Hekmat-Nejad

Publikováno v: Journal of medicinal chemistry. 60(12)

RAS oncogenes have been implicated in30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant tumors has been established in genetically engineered mouse models and human tumor cells. To d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2623e531b4911ee04267b3f1e132c67
https://pubmed.ncbi.nlm.nih.gov/28557458

Measurement of Mechanical Properties and Stress-Potential Coupling in Lithiated Silicon

Autor: Vijay Sethuraman, Michael Chon, Pradeep Guduru

Publikováno v: ECS Meeting Abstracts. :456-456

not Available.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::600c4fccee63e79df173e5decd237c4e
https://doi.org/10.1149/ma2011-01/10/456