Polyfluorinated salicylic acid analogs do not interfere with siderophore biosynthesis

Authors: Hegde, Pooja, Orimoloye, Moyosore O., Sharma, Sachin, Engelhart, Curtis A., Schnappinger, Dirk, Aldrich, Courtney C.

Source: In Tuberculosis May 2023 140

Identification of a Series Containing a Pentafluorophenyl Moiety That Targets Pks13 to Inhibit Growth of Mycobacterium tuberculosis.

Authors: Green, Simon R., Harrison, Justin R., Thompson, Stephen, Murugesan, Dinakaran, Libardo, M. Daben J., Engelhart, Curtis A., Meshanni, Jaclynn, Fletcher, Daniel, Scullion, Paul, Edwards, Darren, Epemolu, Ola, Mutter, Nicole, Shishikura, Yoko, Riley, Jennifer, Ioerger, Thomas R., Roca Guillén, Jose Juan, López, Laura Guijarro, Read, Kevin D., Barry III, Clifton E., Schnappinger, Dirk

Source: ACS Infectious Diseases; 3/14/2025, Vol. 11 Issue 3, p715-726, 12p

Metabolically Stable Adenylation Inhibitors of Biotin Protein Ligase as Antibacterial Agents.

Authors: Liu, Qiang, Engelhart, Curtis A., Wallach, Joshua B., Tiwari, Divya, Ge, Peng, Manna, Adhar, Panda, Subhankar, McCue, William M., Wong, Tsung-Yun, Sharma, Sachin, Jayasinghe, Yahani P., Fuller, Jessica, Ronning, Donald R., Bockman, Matthew R., Cheung, Ambrose, Dartois, Véronique, Zimmerman, Matthew D., Schnappinger, Dirk, Aldrich, Courtney C.

Source: Journal of Medicinal Chemistry; 2/13/2025, Vol. 68 Issue 3, p3065-3087, 23p

Genome-wide gene expression tuning reveals diverse vulnerabilities of M. tuberculosis

Authors: Bosch, Barbara, DeJesus, Michael A., Poulton, Nicholas C., Zhang, Wenzhu, Engelhart, Curtis A., Zaveri, Anisha, Lavalette, Sophie, Ruecker, Nadine, Trujillo, Carolina, Wallach, Joshua B., Li, Shuqi, Ehrt, Sabine, Chait, Brian T., Schnappinger, Dirk, Rock, Jeremy M.

Source: In Cell 19 August 2021 184(17):4579-4592

Rediscovery of PF-3845 as a new chemical scaffold inhibiting phenylalanyl-tRNA synthetase in Mycobacterium tuberculosis

Authors: Wang, Heng, Xu, Min, Engelhart, Curtis A., Zhang, Xi, Yan, Baohua, Pan, Miaomiao, Xu, Yuanyuan, Fan, Shilong, Liu, Renhe, Xu, Lan, Hua, Lan, Schnappinger, Dirk, Chen, Shawn

Source: In Journal of Biological Chemistry January-June 2021 296

Opposing reactions in coenzyme A metabolism sensitize Mycobacterium tuberculosis to enzyme inhibition

Authors: Ballinger, Elaine, Mosior, John, Hartman, Travis, Burns-Huang, Kristin, Gold, Ben, Morris, Roxanne, Goullieux, Laurent, Blanc, Isabelle, Vaubourgeix, Julien, Lagrange, Sophie, Fraisse, Laurent, Sans, Stéphanie, Couturier, Cedric, Bacqué, Eric, Rhee, Kyu, Scarry, Sarah M., Aubé, Jeffrey, Yang, Guangbin, Ouerfelli, Ouathek, Schnappinger, Dirk, Ioerger, Thomas R., Engelhart, Curtis A., McConnell, Jennifer A., McAulay, Kathrine, Fay, Allison, Roubert, Christine, Sacchettini, James, Nathan, Carl

Source: Science, 2019 Feb 01. 363(6426), 498-498.

Access URL: https://www.jstor.org/stable/26588396

Plasticity of the Mycobacterium tuberculosis respiratory chain and its impact on tuberculosis drug development

Authors: Beites, Tiago, O'Brien, Kathryn, Tiwari, Divya, Engelhart, Curtis, Walters, Shaun, Andrews, Jenna, Yang, Hee-Jeong, Sutphen, Michelle, Weiner, Danielle, Dayao, Emmanuel, Zimmerman, Matthew, Prideaux, Brendan, Desai, Prashant, Masquelin, Thierry, Via, Laura, Dartois, Véronique, Boshoff, Helena, Barry, Clifton, Ehrt, Sabine, Schnappinger, Dirk

Source: Nature communications. 10(1):1-12

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100190885009.0x000001&indx=1&recIds=ETOCvdc_100190885009.0x000001

Two‐way regulation of protein expression for identification and validation of on‐target inhibitors of Mycobacterium tuberculosis

Authors: Grover, Shipra, Engelhart, Curtis A., Perez‐Herran, Esther, Tiwari, Divya, Li, Wei, Abrahams, Katherine A., Papavinasasundaram, Kadamba, Bean, James M., Sassetti, Christopher M., Mendoza‐Losana, Alfonso, Besra, Gurdyal S., Jackson, Mary, Aldrich, Courtney, Schnappinger, Dirk

Source: FASEB journal. 36

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100196447424.0x000001&indx=1&recIds=ETOCvdc_100196447424.0x000001

Dual inhibition of the terminal oxidases eradicates antibiotic‐tolerant Mycobacterium tuberculosis

Authors: Lee, Bei Shi, Hards, Kiel, Engelhart, Curtis A, Hasenoehrl, Erik J, Kalia, Nitin P, Mackenzie, Jared S, Sviriaeva, Ekaterina, Chong, Shi Min Sherilyn, Manimekalai, Malathy Sony S, Koh, Vanessa H, Chan, John, Xu, Jiayong, Alonso, Sylvie, Miller, Marvin J, Steyn, Adrie J C, Grüber, Gerhard, Schnappinger, Dirk, Berney, Michael, Cook, Gregory M, Moraski, Garrett C, Pethe, Kevin

Source: EMBO molecular medicine. 13(1)

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100115875569.0x000001&indx=1&recIds=ETOCvdc_100115875569.0x000001

Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity.

Authors: Green, Simon R., Wilson, Caroline, Eadsforth, Thomas C., Punekar, Avinash S., Tamaki, Fabio K., Wood, Gavin, Caldwell, Nicola, Forte, Barbara, Norcross, Neil R., Kiczun, Michael, Post, John M., Lopez-Román, Eva Maria, Engelhart, Curtis A., Lukac, Iva, Zuccotto, Fabio, Epemolu, Ola, Boshoff, Helena I. M., Schnappinger, Dirk, Walpole, Chris, Gilbert, Ian H.

Source: Journal of Medicinal Chemistry; 11/23/2023, Vol. 66 Issue 22, p15380-15408, 29p

Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs.

Authors: Green, Simon R., Davis, Susan H., Damerow, Sebastian, Engelhart, Curtis A., Mathieson, Michael, Baragaña, Beatriz, Robinson, David A., Tamjar, Jevgenia, Dawson, Alice, Tamaki, Fabio K., Buchanan, Kirsteen I., Post, John, Dowers, Karen, Shepherd, Sharon M., Jansen, Chimed, Zuccotto, Fabio, Gilbert, Ian H., Epemolu, Ola, Riley, Jennifer, Stojanovski, Laste

Source: Nature Communications; 10/11/2022, Vol. 13 Issue 1, p1-12, 12p

Subject Terms: TUBERCULOSIS, MYCOBACTERIUM tuberculosis, MIDDLE-income countries, LABORATORY mice, DRUGS

Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.

Authors: Govender, Preshendren, Müller, Rudolf, Singh, Kawaljit, Reddy, Virsinha, Eyermann, Charles J., Fienberg, Stephen, Ghorpade, Sandeep R., Koekemoer, Lizbé, Myrick, Alissa, Schnappinger, Dirk, Engelhart, Curtis, Meshanni, Jaclynn, Byl, Jo Ann W., Osheroff, Neil, Singh, Vinayak, Chibale, Kelly, Basarab, Gregory S.

Source: Journal of Medicinal Chemistry; 5/12/2022, Vol. 65 Issue 9, p6903-6925, 23p

Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target

Authors: Wilson, Caroline, Ray, Peter, Zuccotto, Fabio, Hernandez, Jorge, Aggarwal, Anup, Mackenzie, Claire, Caldwell, Nicola, Taylor, Malcolm, Huggett, Margaret, Mathieson, Michael, Murugesan, Dinakaran, Smith, Alasdair, Davis, Susan, Cocco, Mattia, Parai, Maloy K., Acharya, Arjun, Tamaki, Fabio, Scullion, Paul, Epemolu, Ola, Riley, Jennifer, Stojanovski, Laste, Lopez-Román, Eva Maria, Torres-Gómez, Pedro Alfonso, Toledo, Ana Maria, Guijarro-Lopez, Laura, Camino, Isabel, Engelhart, Curtis A., Schnappinger, Dirk, Massoudi, Lisa M., Lenaerts, Anne, Robertson, Gregory T., Walpole, Chris, Matthews, David, Floyd, David, Sacchettini, James C., Read, Kevin D., Encinas, Lourdes, Bates, Robert H., Green, Simon R., Wyatt, Paul G.

Source: Journal of Medicinal Chemistry; January 2022, Vol. 65 Issue: 1 p409-423, 15p

Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth.

Authors: Ray, Peter C., Huggett, Margaret, Turner, Penelope A., Taylor, Malcolm, Cleghorn, Laura A. T., Early, Julie, Kumar, Anuradha, Bonnett, Shilah A., Flint, Lindsay, Joerss, Douglas, Johnson, James, Korkegian, Aaron, Mullen, Steven, Moure, Abraham L., Davis, Susan H., Murugesan, Dinakaran, Mathieson, Michael, Caldwell, Nicola, Engelhart, Curtis A., Schnappinger, Dirk

Source: ACS Omega; 1/26/2021, Vol. 6 Issue 3, p2284-2311, 28p

Antitubercular 2‑Pyrazolylpyrimidinones: Structure–Activity Relationship and Mode-of-Action Studies.

Authors: Soares de Melo, Candice, Singh, Vinayak, Myrick, Alissa, Simelane, Sandile B., Taylor, Dale, Brunschwig, Christel, Lawrence, Nina, Schnappinger, Dirk, Engelhart, Curtis A., Kumar, Anuradha, Parish, Tanya, Su, Qin, Myers, Timothy G., Boshoff, Helena I. M., Barry III, Clifton E., Sirgel, Frederick A., van Helden, Paul D., Buchanan, Kirsteen I., Bayliss, Tracy, Green, Simon R.

Source: Journal of Medicinal Chemistry; 1/14/2021, Vol. 64 Issue 1, p719-740, 22p

Two-Way Regulation of MmpL3 Expression Identifies and Validates Inhibitors of MmpL3 Function in Mycobacterium tuberculosis.

Authors: Grover, Shipra, Engelhart, Curtis A., Pérez-Herrán, Esther, Li, Wei, Abrahams, Katherine A., Papavinasasundaram, Kadamba, Bean, James M., Sassetti, Christopher M., Mendoza-Losana, Alfonso, Besra, Gurdyal S., Jackson, Mary, Schnappinger, Dirk

Source: ACS Infectious Diseases; 1/8/2021, Vol. 7 Issue 1, p141-152, 12p

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