Publications

Recent research publications from Lgenia and our collaborators.

2026

Novel RU1968-derived inhibitors of CatSper Ca2+ channels in sperm with improved pharmacological properties

Schierling, Tobias; Mittermair, Teresa; Brenker, Christoph; Potapenko, Anton; Münchow, Jens; Balbach, Melanie; Reining, Sophie; Daniliuc, Constantin; Korsching, Kai; Temme, Louisa; Winneroski, Leonard; Hipskind, Philip; Wünsch, Bernhard; Strünker, Timo

Journal of Medicinal Chemistry (submitted)

Optimization and Characterization of SHIP1 Ligands for Cellular Target Engagement and Activity in Alzheimer’s Disease Models

Jesudason, C. D.; Rangel-Barajas, C.; Beach, C. J.; Beck, D. E.; Caballero-Floran, I. H.; Clayton, W. B.; Da Silva, L.; David, J. C.; Doolen, S.; Faulkner, A. N.; Hamdani, A. K.; Huhe, H.; Huynh, K.; Imhoff, R. D.; Javens-Wolfe, J.; Mason, E. R.; Moussaif, M.; Singhal, K.; Soni, D. M.; van Buuren-Milne, M.; Williams, S. P.; Angus, S. P.; Chu, S.; Dage, J. L.; Hipskind, P. A.; Johnson, T. S.; Kaddurah-Daouk, R.; Lamb, B. T.; Meikle, P. J.; Mesecar, A. D.; Palkowitz, A. D.; Quinney, S. K.; Sukoff Rizzo, S. J.; Oblak, A. L.; Richardson, T. I.

bioRxiv 2026, 2025.12.31.697127DOI: 10.64898/2025.12.31.697127
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Curated Set of Tool Compounds to Probe PYK2 and FAK Signaling in Alzheimer’s Disease

Weerawarna, P. M.; Jesudason, C. D.; Lobb, K. L.; Mason, E. R.; Chu, S.; Richardson, T. I.

Alzheimer’s Dementia 2026 (submitted)

2025

Shared Binding Site but Divergent Resistance Profiles Uncover Novel Resistance Mechanisms in Plasmodium HSP90 Inhibitors

Ko, F.-H.; Lukens, A. K.; de Souza, M. L.; Foy, A.; Hsiao, J.; Ndiaye, T.; Okombo, J.; Yeo, T.; Park, H.; Uhlemann, A.-C.; Boonyalai, N.; Kumpornsin, K.; Girling, G.; Pasaje, C.; Godoy, L.; Ottilie, S.; Durst, G. L.; Chatterjee, A.; Niles, J.; Lee, M.; Fidock, D. A.; Wirth, D. F.; Winzeler, E. A.

bioRxiv 2025, 1–46DOI: 10.1101/2025.10.30.684657
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Fungal-Derived Methyldeoxaphomins Target Plasmodium falciparum Segregation through the Inhibition of PfActin1

Jiang, T.; Lee, J. W.; Collins, J. E.; Schaefer, S.; Chen, D.; Nardella, F.; Wendt, K.; Peramuna, T. G.; Paes, R.; McLellan, J. L.; Bhasin, J.; Durst, G. L.; Hanson, K. K.; Chakrabarti, D.; Cichewicz, R. H.; Winzeler, E. A.

Proc. Natl. Acad. Sci. U.S.A. 2025, 122 (8), e2418871122DOI: 10.1073/pnas.2418871122
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Revisiting the Plasmodium falciparum Druggable Genome Using Predicted Structures and Data Mining

Godinez-Macias, K. P.; Chen, D.; Wallis, J. L.; Siegel, M. G.; Adam, A.; Bopp, S.; Carolino, K.; Coulson, L. B.; Durst, G.; Thathy, V.; Esherick, L.; Farringer, M. A.; Flannery, E. L.; Forte, B.; Liu, T.; Godoy Magalhaes, L.; Gupta, A. K.; Istvan, E. S.; Jiang, T.; Kumpornsin, K.; Lobb, K.; McLean, K. J.; Moura, I. M. R.; Okombo, J.; Payne, N. C.; Plater, A.; Rao, S. P. S.; Siqueira-Neto, J. L.; Somsen, B. A.; Summers, R. L.; Zhang, R.; Gilson, M. K.; Gamo, F.-J.; Campo, B.; Baragana, B.; Duffy, J.; Gilbert, I. H.; Lukens, A. K.; Dechering, K. J.; Niles, J. C.; McNamara, C. W.; Cheng, X.; Birkholtz, L.-M.; Bronkhorst, A. W.; Fidock, D. A.; Wirth, D. F.; Goldberg, D. E.; Lee, M. C. S.; Winzeler, E. A.

Drug Discovery 2025, 2, 3DOI: 10.1038/s44386-025-00006-5
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2024

An Arylsulfonamide that Targets Cell Wall Biosynthesis in Mycobacterium tuberculosis

Allen, R.; Ames, L.; Baldin, V. P.; Butts, A.; Henry, K. J.; Durst, G.; Quach, D.; Sugie, J.; Pogliano, J.; Parish, T.

Antimicrob. Agents Chemother. 2024, 68 (11), 1–6DOI: 10.1128/aac.01037-24
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2023

SHIP1 Therapeutic Target Enablement: Identification and Evaluation of Inhibitors for the Treatment of Late-Onset Alzheimer’s Disease

Jesudason, C. D.; Mason, E. R.; Chu, S.; Oblak, A. L.; Javens-Wolfe, J.; Moussaif, M.; Durst, G.; Hipskind, P.; Beck, D. E.; Dong, J.; Amarasinghe, O.; Zhang, Z.-Y.; Hamdani, A. K.; Singhal, K.; Mesecar, A. D.; Souza, S.; Jacobson, M.; Di Salvo, J.; Soni, D. M.; Kandasamy, M.; Masters, A. R.; Quinney, S. K.; Doolen, S.; Huhe, H.; Sukoff Rizzo, S. J.; Lamb, B. T.; Palkowitz, A. D.; Richardson, T. I.

Alzheimer’s Dementia (N. Y.) 2023, 9, e12429DOI: 10.1002/trc2.12429
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Inhibition of SHIP1 as a Therapeutic Strategy for the Treatment of Alzheimer’s Disease

Richardson, T. I.; Jesudason, C. D.; Clayton, B. W.

PCT Patent Application 2023 (Filed July 11, 2023)

2022

Identification of β-Lactams Active against Mycobacterium tuberculosis by a Consortium of Pharmaceutical Companies and Academic Institutions

Gold, B.; Zhang, J.; Lopez Quezada, L.; Roberts, J.; Ling, Y.; Wood, M.; Shinwari, W.; Goullieux, L.; Roubert, C.; Fraisse, L.; Bacqué, E.; Lagrange, S.; Filoche-Rommé, B.; Vieth, M.; Hipskind, P. A.; Jungheim, L. N.; Aubé, J.; Scarry, S. M.; McDonald, S. L.; Li, K.; Perkowski, A.; Nguyen, Q.; Dartois, V.; Zimmerman, M.; Olsen, D. B.; Young, K.; Bonnett, S.; Joerss, D.; Parish, T.; Arora, K.; Barry, C. E., III; Guijarro, L.; Anca, S.; Rullas, J.; Rodríguez-Salguero, B.; Martínez-Martínez, M. S.; Porras-De Francisco, E.; Cacho, M.; Barros-Aguirre, D.; Smith, P.; Berthel, S. J.; Nathan, C.; Bates, R. H.

ACS Infect. Dis. 2022, 8 (3), 557–573DOI: 10.1021/acsinfecdis.1c00570
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2021

Prioritization of Molecular Targets for Antimalarial Drug Discovery

Forte, B.; Ottilie, S.; Plater, A.; Campo, B.; Dechering, K. J.; Gamo, F. J.; Goldberg, D. E.; Istvan, E. S.; Lee, M.; Lukens, A. K.; McNamara, C. W.; Niles, J. C.; Okombo, J.; Pasaje, C. F. A.; Siegel, M. G.; Wirth, D.; Wyllie, S.; Fidock, D. A.; Baragana, B.; Winzeler, E. A.; Gilbert, I. H.

ACS Infect. Dis. 2021, 7 (10), 2764–2776DOI: 10.1021/acsinfecdis.1c00322
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The Tuberculosis Drug Accelerator at Year 10: What Have We Learned?

Aldridge, B. B.; Barros-Aguirre, D.; Barry, C. E., III; Bates, R. H.; Berthel, S. J.; Boshoff, H. I.; Chibale, K.; Chu, X.-J.; Cooper, C. B.; Dartois, V.; Duncan, K.; Fotouhi, N.; Gusovsky, F.; Hipskind, P. A.; Kempf, D. J.; Lelièvre, J.; Lenaerts, A. J.; McNamara, C. W.; Mizrahi, V.; Nathan, C.; Olsen, D. B.; Parish, T.; Petrassi, H. M.; Pym, A.; Yuan, Y.; et al.

Nat. Med. 2021, 27, 1333–1337DOI: 10.1038/s41591-021-01442-2
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Novel Trifluoromethyl Pyrimidinone Compounds With Activity Against Mycobacterium tuberculosis

Hembre, E.; Early, J. V.; Odingo, J.; Shelton, C.; Anoshchenko, O.; Guzman, J.; Flint, L.; Dennison, D.; McNeil, M. B.; Korkegian, A.; Ovechkina, Y.; Ornstein, P.; Masquelin, T.; Hipskind, P. A.; Parish, T.

Front. Chem. 2021, 9, 613349DOI: 10.3389/fchem.2021.613349
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Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth

Ray, P. C.; Huggett, M.; Turner, P. A.; Taylor, M.; Cleghorn, L. A. T.; Early, J.; Kumar, A.; Bonnett, S. A.; Flint, L.; Joerss, D.; Johnson, J.; Korkegian, A.; Mullen, S.; Moure, A. L.; Davis, S. H.; Murugesan, D.; Mathieson, M.; Caldwell, N.; Engelhart, C. A.; Schnappinger, D.; Epemolu, O.; Zuccotto, F.; Riley, J.; Scullion, P.; Stojanovski, L.; Massoudi, L.; Robertson, G. T.; Lenaerts, A. J.; Freiberg, G.; Kempf, D. J.; Masquelin, T.; Hipskind, P. A.; Odingo, J.; Read, K. D.; Green, S. R.; Wyatt, P. G.; Parish, T.

ACS Omega 2021, 6 (3), 2284–2311DOI: 10.1021/acsomega.0c05589
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2019

Identification of Compounds with pH-Dependent Bactericidal Activity against Mycobacterium tuberculosis

Early, J.; Ollinger, J.; Darby, C.; Alling, T.; Mullen, S.; Casey, A.; Gold, B.; Ochoada, J.; Wiernicki, T.; Masquelin, T.; Nathan, C.; Hipskind, P. A.; Parish, T.

ACS Infect. Dis. 2019, 5 (2), 272–280DOI: 10.1021/acsinfecdis.8b00256
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2018

Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB

Cleghorn, L. A. T.; Ray, P. C.; Odingo, J.; Kumar, A.; Wescott, H.; Korkegian, A.; Masquelin, T.; Lopez Moure, A.; Wilson, C.; Davis, S.; Huggett, M.; Turner, P.; Smith, A.; Epemolu, O.; Zuccotto, F.; Riley, J.; Scullion, P.; Shishikura, Y.; Ferguson, L.; Rullas, J.; Guijarro, L.; Read, K. D.; Green, S. R.; Hipskind, P.; Parish, T.; Wyatt, P. G.

J. Med. Chem. 2018, 61 (15), 6592–6608DOI: 10.1021/acs.jmedchem.8b00511
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Imidazopyridine Compounds Inhibit Mycobacterial Growth by Depleting ATP Levels

O’Malley, T.; Alling, T.; Early, J. V.; Wescott, H. A.; Kumar, A.; Moraski, G. C.; Miller, M. J.; Masquelin, T.; Hipskind, P. A.; Parish, T.

Antimicrob. Agents Chemother. 2018, 62 (6)DOI: 10.1128/AAC.02439-17
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