Výsledky vyhledávání - "Dirksen E Bussiere"

Akademický článek

A polyomavirus peptide binds to the capsid VP1 pore and has potent antiviral activity against BK and JC polyomaviruses

Autor: Joshua R Kane, Susan Fong, Jacob Shaul, Alexandra Frommlet, Andreas O Frank, Mark Knapp, Dirksen E Bussiere, Peter Kim, Elizabeth Ornelas, Carlos Cuellar, Anastasia Hyrina, Johanna R Abend, Charles A Wartchow

Publikováno v: eLife, Vol 9 (2020)

In pursuit of therapeutics for human polyomaviruses, we identified a peptide derived from the BK polyomavirus (BKV) minor structural proteins VP2/3 that is a potent inhibitor of BKV infection with no observable cellular toxicity. The thirteen-residue

Externí odkaz: https://doaj.org/article/2b17b8ea557f438fa77b7135beaff218

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Akademický článek

Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED.

Publikováno v: PLoS ONE, Vol 12, Iss 1, p e0169855 (2017)

Polycomb repressive complex 2 (PRC2), a histone H3 lysine 27 methyltransferase, plays a key role in gene regulation and is a known epigenetics drug target for cancer therapy. The WD40 domain-containing protein EED is the regulatory subunit of PRC2. I

Externí odkaz: https://doaj.org/article/09dc29db6d614ee7832a57cab569330c

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Akademický článek

Structural basis for therapeutic inhibition of influenza A polymerase PB2 subunit

Autor: Xiaolei Ma, Lili Xie, Charles Wartchow, Robert Warne, Yongjin Xu, Alexey Rivkin, David Tully, Steven Shia, Kyoko Uehara, Dianna M. Baldwin, Gladys Muiru, Weidong Zhong, Isabel Zaror, Dirksen E. Bussiere, Vincent H. J. Leonard

Publikováno v: Scientific Reports, Vol 7, Iss 1, Pp 1-8 (2017)

Abstract Influenza virus uses a unique mechanism to initiate viral transcription named cap-snatching. The PB2 subunit of the viral heterotrimeric RNA polymerase binds the cap structure of cellular pre-mRNA to promote its cleavage by the PA subunit. T

Externí odkaz: https://doaj.org/article/0e992cb2a2914995a1aae7e6664172d2

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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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