Brayton, Samantha R Toles, Zachary E A Sanchez, Christian A Michaud, Marina E Thierer, Laura M Keller, Taylor M Risener, Caitlin J Quave, Cassandra L Wuest, William M Minbiole, Kevin P C
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Published in
ACS infectious diseases
Quaternary ammonium compounds (QACs) serve as a first line of defense against infectious pathogens. As resistance to QACs emerges in the environment, the development of next-generation disinfectants is of utmost priority for human health. Balancing antibacterial potency with environmental considerations is required to effectively counter the develo...
Ghimire, Jenisha Hart, Robert J Soldano, Anabel Chen, Charles H Guha, Shantanu Hoffmann, Joseph P Hall, Kalen M Sun, Leisheng Nelson, Benjamin J Lu, Timothy K
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Published in
ACS infectious diseases
Here, we describe the continued synthetic molecular evolution of a lineage of host-compatible antimicrobial peptides (AMP) intended for the treatment of wounds infected with drug-resistant, biofilm-forming bacteria. The peptides tested are variants of an evolved AMP called d-amino acid CONsensus with Glycine Absent (d-CONGA), which has excellent an...
Luo, Shu Y. Moussa, Eman W. Lopez-Orozco, Joaquin Felix-Lopez, Alberto Ishida, Ray Fayad, Nawell Gomez-Cardona, Erik Wang, Henry Wilson, Joyce A. Kumar, Anil
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Published in
ACS Infectious Diseases
The recent emergence of SARS-CoV-2 in the human population has caused a global pandemic. The virus encodes two proteases, Mpro and PLpro, that are thought to play key roles in the suppression of host protein synthesis and immune response evasion during infection. To identify the specific host cell substrates of these proteases, active recombinant S...
Al Ayed, Karol Zamarbide Losada, Denise Machushynets, Nataliia V. Terlouw, Barbara Elsayed, Somayah S. Schill, Julian Trebosc, Vincent Pieren, Michel Medema, Marnix H. van Wezel, Gilles P.
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Published in
ACS Infectious Diseases
The unabated rise of antibiotic resistance has raised the specter of a post-antibiotic era and underscored the importance of developing new classes of antibiotics. The relacidines are a recently discovered group of nonribosomal lipopeptide antibiotics that show promising activity against Gram-negative pathogens and share structural similarities wit...
Attram, Henrietta D. Korkor, Constance M. Taylor, Dale Njoroge, Mathew Chibale, Kelly
Published in
ACS Infectious Diseases
We previously identified a novel class of antimalarial benzimidazoles incorporating an intramolecular hydrogen bonding motif. The frontrunner of the series, analogue A , showed nanomolar activity against the chloroquine-sensitive NF54 and multi-drug-resistant K1 strains of Plasmodium falciparum ( Pf NF54 IC50 = 0.079 μM; Pf K1 IC50 = 0.335 μM). Her...
Neugent, Michael L. Hulyalkar, Neha V. Kumar, Ashwani Xing, Chao Zimmern, Philippe E. Shulaev, Vladimir De Nisco, Nicole J.
Published in
ACS Infectious Diseases
Glycosaminoglycans (GAGs) are linear, negatively charged polysaccharides composed of repeating disaccharide units of uronic acid and amino sugars. The luminal surface of the bladder epithelium is coated with a GAG layer. These urothelial GAGs are thought to provide a protective barrier and serve as a potential interaction site with the urinary micr...
Cha, Hyeon-Min Kim, Uk-Il Ahn, Soo Bin Lee, Myoung Kyu Lee, Haemi Bang, Hyungtae Jang, Yejin Kim, Seong Soon Bae, Myung Ae Kim, Kyungjin
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Published in
ACS Infectious Diseases
Gemcitabine is a nucleoside analogue of deoxycytidine and has been reported to be a broad-spectrum antiviral agent against both DNA and RNA viruses. Screening of a nucleos(t)ide analogue-focused library identified gemcitabine and its derivatives (compounds 1 , 2a , and 3a ) blocking influenza virus infection. To improve their antiviral selectivity ...
Nguyen, William Dans, Madeline G Currie, Iain Awalt, Jon Kyle Bailey, Brodie L Lumb, Chris Ngo, Anna Favuzza, Paola Palandri, Josephine Ramesh, Saishyam
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Published in
ACS infectious diseases
The development of new antimalarials is required because of the threat of resistance to current antimalarial therapies. To discover new antimalarial chemotypes, we screened the Janssen Jumpstarter library against the P. falciparum asexual parasite and identified the 7-N-substituted-3-oxadiazole quinolone hit class. We established the structure-acti...
Rota, Paola La Rocca, Paolo Bonfante, Francesco Pagliari, Matteo Piccoli, Marco Cirillo, Federica Ghiroldi, Andrea Franco, Valentina Pappone, Carlo Allevi, Pietro
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Published in
ACS infectious diseases
Global infections with viruses belonging to the Paramyxoviridae, such as Newcastle disease virus (NDV) or human parainfluenza viruses (hPIVs), pose a serious threat to animal and human health. NDV-HN and hPIVs-HN (HN hemagglutinin-neuraminidase) share a high degree of similarity in catalytic site structures; therefore, the development of an efficie...
Stewart, Louisa J. Hong, YoungJin Holmes, Isabel R. Firth, Samantha J. Ahmed, Yasmin Quinn, Janet Santos, Yazmin Cobb, Steven L. Jakubovics, Nicholas S. Djoko, Karrera Y.
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Published in
ACS Infectious Diseases
Histatin-5 (Hst5) is a member of the histatin superfamily of cationic, His-rich, Zn(II)-binding peptides in human saliva. Hst5 displays antimicrobial activity against fungal and bacterial pathogens, often in a Zn(II)-dependent manner. In contrast, here we showed that under in vitro conditions that are characteristic of human saliva, Hst5 does not k...
