Výsledky vyhledávání - "Gianfranco De Pascale"

Akademický článek

A pathway-directed positive growth restoration assay to facilitate the discovery of lipid A and fatty acid biosynthesis inhibitors in Acinetobacter baumannii.

Autor: Daryl L Richie, Lisha Wang, Helen Chan, Gianfranco De Pascale, David A Six, Jun-Rong Wei, Charles R Dean

Publikováno v: PLoS ONE, Vol 13, Iss 3, p e0193851 (2018)

Acinetobacter baumannii ATCC 19606 can grow without lipooligosaccharide (LOS). Lack of LOS can result from disruption of the early lipid A biosynthetic pathway genes lpxA, lpxC or lpxD. Although LOS itself is not essential for growth of A. baumannii

Externí odkaz: https://doaj.org/article/10190c5aac8a410eb37f60e20cfe2614

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Two Distinct Mechanisms of Inhibition of LpxA Acyltransferase Essential for Lipopolysaccharide Biosynthesis

Publikováno v: Journal of the American Chemical Society. 142:4445-4455

The lipopolysaccharide biosynthesis pathway is considered an attractive drug target against the rising threat of multi-drug-resistant Gram-negative bacteria. Here, we report two novel small-molecule inhibitors (compounds 1 and 2) of the acyltransfera

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::35d90e01ff06abb91a53cfa340142eb6
https://doi.org/10.1021/jacs.9b13530

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Akademický článek

Cross‐species discovery of syncretic drug combinations that potentiate the antifungal fluconazole

Autor: Michaela Spitzer, Emma Griffiths, Kim M Blakely, Jan Wildenhain, Linda Ejim, Laura Rossi, Gianfranco De Pascale, Jasna Curak, Eric Brown, Mike Tyers, Gerard D Wright

Publikováno v: Molecular Systems Biology, Vol 7, Iss 1, Pp 1-14 (2011)

Abstract Resistance to widely used fungistatic drugs, particularly to the ergosterol biosynthesis inhibitor fluconazole, threatens millions of immunocompromised patients susceptible to invasive fungal infections. The dense network structure of synthe

Externí odkaz: https://doaj.org/article/823869d3f07548b4a721f5dac6aeaf53

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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

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Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria

Autor: Xiaolin Li, Martin Traebert, David McKenney, Dirksen E. Bussiere, Sylvia Ma, Katherine V. Thompson, Nirav Shah, Douglas C. Bauer, Wosenu Mergo, Duncan Armstrong, Richard Zang, Bhavin Kantariya, Jennifer A. Leeds, Bo Zhou, Ashish Patel, John Fuller, Tushar Patel, Alice Rico, William S. Sawyer, Colin Osborne, Heinz E. Moser, Mangesh Fulsunder, Yongjin Xu, Bret Benton, Swapnil Malekar, Shravanthi Madhavan, Jason Vo, Cheng Hu, Daniel Mutnick, Krunal Prajapati, Michael Wang, Katherine R Prosen, Louis E. Metzger, Carl J. Balibar, Darshit Patel, Jogitha Selvarajah, Sarah Williams, Shailesh Satasia, Peichao Lu, Bhavesh Dhumale, Kartik Shanghavi, Alexey Rivkin, Javier de Vicente, Wei Shu, Jonas Noeske, Anand Vala, Mark R. Sanderson, Cornelia Bellamacina, L. Mark Fisher, Lakhan Vala, Qin Yue, Charles R. Dean, Gianfranco De Pascale, Dennis A. Veselkov, Marcella Widya, Folkert Reck, Lauren M. Holder, Guillaume Lapointe, Colin K. Skepper, Daryl L. Richie, Anatoli Lvov

Publikováno v: Skepper, C K, Armstrong, D, Balibar, C J, Bauer, D, Bellamacina, C, Benton, B M, Bussiere, D, De Pascale, G, De Vicente, J, Dean, C R, Dhumale, B, Fisher, L M, Fuller, J, Fulsunder, M, Holder, L M, Hu, C, Kantariya, B, Lapointe, G, Leeds, J A, Li, X, Lu, P, Lvov, A, Ma, S, Madhavan, S, Malekar, S, Mckenney, D, Mergo, W, Metzger, L, Moser, H E, Mutnick, D, Noeske, J, Osborne, C, Patel, A, Patel, D, Patel, T, Prajapati, K, Prosen, K R, Reck, F, Richie, D L, Rico, A, Sanderson, M R, Satasia, S, Sawyer, W S, Selvarajah, J, Shah, N, Shanghavi, K, Shu, W, Thompson, K V, Veselkov, D A, Williams, S L, Xu, Y, Yue, Q, Zang, R, Zho, B & Rivkin, A 2020, ' Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria ', Journal of Medicinal Chemistry, vol. 63, no. 14, pp. 7773-7816 . https://doi.org/10.1021/acs.jmedchem.0c00347

Since their discovery over 5 decades ago, quinolone antibiotics have found enormous success as broad spectrum agents that exert their activity through dual inhibition of bacterial DNA gyrase and topoisomerase IV. Increasing rates of resistance, drive

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99afdf67109b37c858dc407505690414
https://kclpure.kcl.ac.uk/ws/files/133475695/Topoisomerase_Inhibitors_Addressing_Fluoroquinolone_SKEPPER_Acc16Jun2020E_ub7Jul2020_GREEN_AAM.pdf

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A Common Platform for Antibiotic Dereplication and Adjuvant Discovery

Autor: Andrew C. Pawlowski, Gerard D. Wright, Gianfranco De Pascale, Andrew M. King, Kalinka Koteva, Arthur O. Sieron, Georgina Cox

Publikováno v: Cell Chemical Biology. 24:98-109

Solving the antibiotic resistance crisis requires the discovery of new antimicrobial drugs and the preservation of existing ones. The discovery of inhibitors of antibiotic resistance, antibiotic adjuvants, is a proven example of the latter. A major d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5dfcb5a1233107b1d2a471e1b1e78cf
https://doi.org/10.1016/j.chembiol.2016.11.011

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Biased Complement Diversity Selection for Effective Exploration of Chemical Space in Hit-Finding Campaigns

Autor: Mika Lindvall, Susan Fong, Charles Wartchow, Gianfranco De Pascale, Johanna M. Jansen, Keith B. Pfister, Heinz E. Moser, Bob Warne

Publikováno v: Journal of chemical information and modeling. 59(5)

The success of hit-finding campaigns relies on many factors, including the quality and diversity of the set of compounds that is selected for screening. This paper presents a generalized workflow that guides compound selections from large compound ar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e25cd82bf33b8c6df9e8f56e901670c
https://pubmed.ncbi.nlm.nih.gov/30943027

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