Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3

Authors: Calic, Petar P.S., Ashton, Trent D., Mansouri, Mahta, Loi, Katie, Jarman, Kate E., Qiu, Deyun, Lehane, Adele M., Roy, Sayantan, Rao, Gunturu P., Maity, Bikash, Wittlin, Sergio, Crespo, Benigno, Gamo, Franciso-Javier, Deni, Ioanna, Fidock, David A., Chowdury, Mrittika, de Koning-Ward, Tania F., Cowman, Alan F., Jackson, Paul F., Baud, Delphine, Brand, Stephen, Laleu, Benoît, Sleebs, Brad E.

Source: In European Journal of Medicinal Chemistry 5 October 2024 276

Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria

Authors: Lawong, Aloysus, Gahalawat, Suraksha, Ray, Sneha, Ho, Nhi, Han, Yan, Ward, Kurt E., Deng, Xiaoyi, Chen, Zhe, Kumar, Ashwani, Xing, Chao, Hosangadi, Varun, Fairhurst, Kate J., Tashiro, Kyuto, Liszczak, Glen, Shackleford, David M., Katneni, Kasiram, Chen, Gong, Saunders, Jessica, Crighton, Elly, Casas, Arturo, Robinson, Joshua J., Imlay, Leah S., Zhang, Xiaoyu, Lemoff, Andrew, Zhao, Zhiyu, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Wittlin, Sergio, Campbell, Simon F., Fidock, David A., Laleu, Benoît, Charman, Susan A., Ready, Joseph M., Phillips, Margaret A.

Source: In Cell Chemical Biology 15 August 2024 31(8):1503-1517

ATP mimetics targeting prolyl-tRNA synthetases as a new avenue for antimalarial drug development

Authors: Mishra, Siddhartha ^{1, 2, 4}, Malhotra, Nipun ^{1, 5, 6}, Laleu, Benoît ³, Chakraborti, Soumyananda ^{2, 4}, Yogavel, Manickam ¹, Sharma, Amit ^{1, 7, ∗}

Source: In iScience 19 July 2024 27(7)

Replenishing the malaria drug discovery pipeline: Screening and hit evaluation of the MMV Hit Generation Library 1 (HGL1) against asexual blood stage Plasmodium falciparum, using a nano luciferase reporter read-out

Authors: Dechering, Koen J., Timmerman, Martijn, Rensen, Kim, Koolen, Karin M.J., Honarnejad, Saman, Vos, Martijn W., Huijs, Tonnie, Henderson, Rob W.M., Chenu, Elodie, Laleu, Benoît, Montefiore, Bailey C., Segall, Matthew D., Mills, James E.J., Guantai, Eric M., Duffy, James, Duffey, Maëlle

Source: In SLAS Discovery September 2022 27(6):337-348

The Plasmodium falciparum ABC transporter ABCI3 confers parasite strain-dependent pleiotropic antimalarial drug resistance

Authors: Murithi, James M., Deni, Ioanna, Pasaje, Charisse Flerida A., Okombo, John, Bridgford, Jessica L., Gnädig, Nina F., Edwards, Rachel L., Yeo, Tomas, Mok, Sachel, Burkhard, Anna Y., Coburn-Flynn, Olivia, Istvan, Eva S., Sakata-Kato, Tomoyo, Gomez-Lorenzo, Maria G., Cowell, Annie N., Wicht, Kathryn J., Le Manach, Claire, Kalantarov, Gavreel F., Dey, Sumanta, Duffey, Maëlle, Laleu, Benoît, Lukens, Amanda K., Ottilie, Sabine, Vanaerschot, Manu, Trakht, Ilya N., Gamo, Francisco-Javier, Wirth, Dyann F., Goldberg, Daniel E., Odom John, Audrey R., Chibale, Kelly, Winzeler, Elizabeth A., Niles, Jacquin C., Fidock, David A.

Source: In Cell Chemical Biology 19 May 2022 29(5):824-839

Optimisation of 2-(N-phenyl carboxamide) triazolopyrimidine antimalarials with moderate to slow acting erythrocytic stage activity

Authors: Bailey, Brodie L., Nguyen, William, Ngo, Anna, Goodman, Christopher D., Gancheva, Maria R., Favuzza, Paola, Sanz, Laura M., Gamo, Francisco-Javier, Lowes, Kym N., McFadden, Geoffrey I., Wilson, Danny W., Laleu, Benoît, Brand, Stephen, Jackson, Paul F., Cowman, Alan F., Sleebs, Brad E.

Source: In Bioorganic Chemistry October 2021 115

Structure-Based Discovery and Development of Highly Potent Dihydroorotate Dehydrogenase Inhibitors for Malaria Chemoprevention

Authors: Nie, Zhe, Bonnert, Roger, Tsien, Jet, Deng, Xiaoyi, Higgs, Christopher, El Mazouni, Farah, Zhang, Xiaoyu, Li, Renzhe, Ho, Nhi, Feher, Victoria, Paulsen, Janet, Shackleford, David M., Katneni, Kasiram, Chen, Gong, Ng, Alice C. F., McInerney, Mitchell, Wang, Wen, Saunders, Jessica, Collins, Daniel, Yan, Dandan, Li, Peng, Campbell, Michael, Patil, Rahul, Ghoshal, Atanu, Mondal, Pallab, Kundu, Abhijit, Chittimalla, Rajesh, Mahadeva, Muralikumar, Kokkonda, Sreekanth, White, John, Das, Rishi, Mukherjee, Partha, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Malmstrom, Robert, Lawrenz, Morgan, Rodriguez-Granillo, Agustina, Rathod, Pradipsinh K., Tomchick, Diana R., Palmer, Michael J., Laleu, Benoît, Qin, Tian, Charman, Susan A., Phillips, Margaret A.

Source: Journal of Medicinal Chemistry; January 2025, Vol. 68 Issue: 1 p590-637, 48p

Global Health Priority BoxProactive Pandemic Preparedness.

Authors: Adam, Anna, Besson, Dominique, Bryant, Rob, Rees, Sarah, Willis, Paul A., Burrows, Jeremy N., Hooft van Huisjduijnen, Rob, Laleu, Benoît, Norton, Larry, Canan, Stacie, Hawryluk, Natalie, Robinson, Dale, Palmer, Mike, Samby, Kirandeep Kaur

Source: ACS Infectious Diseases; 12/13/2024, Vol. 10 Issue 12, p4030-4039, 10p

Assessing the interplay between off-target promiscuity, cytotoxicity, and tolerability in rodents to improve the safety profile of novel anti-malarial plasmepsin X inhibitors.

Authors: Gerets, Helga H J, Delaunois, Annie, Cardenas, Alvaro, Class, Reiner, Fleurance, Renaud, Haro, Teresa de, Laleu, Benoît, Lowe, Martin A, Rosseels, Marie-Luce, Valentin, Jean-Pierre

Source: Toxicological Sciences; Oct2024, Vol. 201 Issue 2, p311-320, 10p

Subject Terms: MUSCARINIC acetylcholine receptors, CYTOTOXINS, GUINEA pigs, DRUG development, PROMISCUITY, OPIOID receptors

Exploring a Tetrahydroquinoline Antimalarial Hit from the Medicines for Malaria Pathogen Box and Identification of its Mode of Resistance as PfeEF2

Authors: Laleu, Benoît, Rubiano, Kelly, Yeo, Tomas, Hallyburton, Irene, Anderson, Mark, Crespo‐Fernandez, Benigno, Gamo, Francisco‐Javier, Antonova‐Koch, Yevgeniya, Orjuela‐Sanchez, Pamela, Wittlin, Sergio, Jana, Gouranga P., Maity, Bikash C., Chenu, Elodie, Duffy, James, Sjö, Peter, Waterson, David, Winzeler, Elizabeth, Guantai, Eric, Fidock, David A., Hansson, Thomas G.

Source: ChemMedChem. 17(22)

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100191266664.0x000001&indx=1&recIds=ETOCvdc_100191266664.0x000001

In vitro screening of the open source Pathogen Box identifies novel compounds with profound activities against Neospora caninum

Authors: Müller, Joachim, Aguado, Adriana, Laleu, Benoît, Balmer, Vreni, Ritler, Dominic, Hemphill, Andrew

Source: In International Journal for Parasitology October 2017 47(12):801-809

Novel Compound MMV1804559 from the Global Health Priority Box Exhibits In Vitro and In Vivo Activity against Madurella mycetomatis.

Authors: Ma, Jingyi, Eadie, Kimberly, Schippers, Marij, Fahal, Ahmed, Laleu, Benoît, Verbon, Annelies, van de Sande, Wendy W. J.

Source: International Journal of Molecular Sciences; Jun2024, Vol. 25 Issue 11, p6227, 14p

Subject Terms: ANTIFUNGAL agents, CHEMICAL libraries, WORLD health, DRUG discovery, NEGLECTED diseases, GREATER wax moth

Screening a repurposing library, the Medicines for Malaria Venture Stasis Box, against Schistosoma mansoni

Authors: Pasche, Valérian, Laleu, Benoît, Keiser, Jennifer

Source: Parasites & vectors. 11(1):1-8

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100165398900.0x000001&indx=1&recIds=ETOCvdc_100165398900.0x000001

Screening of the ‘Pathogen Box’ identifies an approved pesticide with major anthelmintic activity against the barber's pole worm

Authors: Preston, Sarah, Jiao, Yaqing, Jabbar, Abdul, McGee, Sean L., Laleu, Benoît, Willis, Paul, Wells, Timothy N.C., Gasser, Robin B.

Source: In International Journal for Parasitology: Drugs and Drug Resistance December 2016 6(3):329-334

Targeting prolyl-tRNA synthetase via a series of ATP-mimetics to accelerate drug discovery against toxoplasmosis.

Authors: Yogavel, Manickam¹, Bougdour, Alexandre², Mishra, Siddhartha^1,3,4, Malhotra, Nipun¹, Chhibber-Goel, Jyoti¹, Bellini, Valeria², Harlos, Karl⁵, Laleu, Benoît⁶, Hakimi, Mohamed-Ali², mohamed-ali.hakimi@univ-grenoble-alpes.fr, Sharma, Amit^1,3,4, mohamed-ali.hakimi@univ-grenoble-alpes.fr

Source: PLoS Pathogens; 2/28/2023, Vol. 18 Issue 2, p1-22, 22p

Screening of the 'Stasis Box' identifies two kinase inhibitors under pharmaceutical development with activity against Haemonchus contortus

Authors: Jiao, Yaqing, Preston, Sarah, Koehler, Anson, Stroehlein, Andreas, Chang, Bill, Simpson, Kaylene, Cowley, Karla, Palmer, Michael, Laleu, Benoît, Wells, Timothy, Jabbar, Abdul, Gasser, Robin

Source: Parasites & vectors. 10(1):1-7

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100136216493.0x000001&indx=1&recIds=ETOCvdc_100136216493.0x000001

Assessing the anthelmintic activity of pyrazole-5-carboxamide derivatives against Haemonchus contortus

Authors: Jiao, Yaqing, Preston, Sarah, Song, Hongjian, Jabbar, Abdul, Liu, Yuxiu, Baell, Jonathan, Hofmann, Andreas, Hutchinson, Dana, Wang, Tao, Koehler, Anson, Fisher, Gillian, Andrews, Katherine, Laleu, Benoît, Palmer, Michael, Burrows, Jeremy, Wells, Timothy, Wang, Qingmin, Gasser, Robin

Source: Parasites & vectors. 10(1):1-7

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100133576183.0x000001&indx=1&recIds=ETOCvdc_100133576183.0x000001

MAIP: An Open-Source Tool to Enrich High-Throughput Screening Output and Identify Novel, Druglike Molecules with Antimalarial Activity.

Authors: Bosc, Nicolas, Felix, Eloy, Gardner, J. Mark F., Mills, James, Timmerman, Martijn, Asveld, Dennis, Rensen, Kim, Mukherjee, Partha, Das, Rishi, Chenu, Elodie, Besson, Dominique, Burrows, Jeremy N., Duffy, James, Laleu, Benoît, Guantai, Eric M., Leach, Andrew R.

Source: ACS Medicinal Chemistry Letters; 12/14/2023, Vol. 14 Issue 12, p1733-1741, 9p

Design of Novel Series of Antimalarial PMX Inhibitors with Increased Half-Life via Molecular Property Optimization.

Authors: Sakata, Komei, Lowe, Martin A., Xuan, Mengyang, Bruffaerts, Jeffrey, Stasi, Luigi P., Lallemand, Bénédicte, Cardenas, Alvaro, Taylor, Richard D., Vidler, Lewis R., King, Lloyd, Valentin, Jean-Pierre, Laleu, Benoît, de Haro, Teresa

Source: ACS Medicinal Chemistry Letters; 11/9/2023, Vol. 14 Issue 11, p1582-1588, 7p

Double drugging of prolyl-tRNA synthetase provides a new paradigm for anti-infective drug development.

Authors: Manickam, Yogavel¹, Malhotra, Nipun¹, Mishra, Siddhartha^1,2,3, Babbar, Palak¹, Dusane, Abhishek¹, Laleu, Benoît⁴, Bellini, Valeria⁵, Hakimi, Mohamed-Ali⁵, Bougdour, Alexandre⁵, alexandre.bougdour@univ-grenoble-alpes.fr, Sharma, Amit^1,2,3, alexandre.bougdour@univ-grenoble-alpes.fr

Source: PLoS Pathogens; 3/25/2022, Vol. 18 Issue 3, p1-17, 17p