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Xiaoyi Deng
Researcher at University of Texas Southwestern Medical Center
Publications - 20
Citations - 1614
Xiaoyi Deng is an academic researcher from University of Texas Southwestern Medical Center. The author has contributed to research in topics: Dihydroorotate dehydrogenase & Plasmodium falciparum. The author has an hindex of 15, co-authored 19 publications receiving 1405 citations. Previous affiliations of Xiaoyi Deng include University of Texas at Austin & University of Texas at Dallas.
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Journal ArticleDOI
A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria
Margaret A. Phillips,Julie Lotharius,Kennan C. Marsh,John H. White,Anthony Dayan,Karen L. White,Jacqueline W. Njoroge,Farah El Mazouni,Yanbin Lao,Sreekanth Kokkonda,Diana R. Tomchick,Xiaoyi Deng,Trevor Laird,Sangeeta N. Bhatia,Sandra March,Caroline L. Ng,David A. Fidock,Sergio Wittlin,Sergio Wittlin,Maria J. Lafuente-Monasterio,Francisco Javier Gamo Benito,Laura Maria Sanz Alonso,María Santos Martínez,María Belén Jiménez-Díaz,Santiago Ferrer Bazaga,Iñigo Angulo-Barturen,John N. Haselden,James B. Louttit,Yi Cui,Arun Sridhar,Anna Marie Zeeman,Clemens H. M. Kocken,Robert W. Sauerwein,Koen J. Dechering,Vicky M. Avery,Sandra Duffy,Michael J. Delves,Robert E. Sinden,Andrea Ruecker,Kristina S. Wickham,Rosemary Rochford,Janet Gahagen,Lalitha V. Iyer,Ed Riccio,Jon C. Mirsalis,Ian Bathhurst,Thomas Rueckle,Xavier C. Ding,Brice Campo,Didier Leroy,M. John Rogers,Pradipsinh K. Rathod,Jeremy N. Burrows,Susan A. Charman +53 more
TL;DR: DSM265, a triazolopyrimidine-based inhibitor of the pyrimidine biosynthetic enzyme dihydroorotate dehydrogenase (DHODH), is the first DHODH inhibitor to reach clinical development for treatment of malaria as discussed by the authors.
Journal ArticleDOI
Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential
Jose M. Coteron,Maria L. Marco,Jorge Esquivias,Xiaoyi Deng,Karen L. White,John H. White,Maria Koltun,Farah El Mazouni,Sreekanth Kokkonda,Kasiram Katneni,Ravi K. Bhamidipati,David M. Shackleford,Iñigo Angulo-Barturen,Santiago Ferrer,María Belén Jiménez-Díaz,Francisco-Javier Gamo,Elizabeth J. Goldsmith,William N. Charman,Ian Bathurst,David M. Floyd,David Matthews,Jeremy N. Burrows,Pradipsinh K. Rathod,Susan A. Charman,Margaret A. Phillips +24 more
TL;DR: These studies have identified the first candidate in the triazolopyrimidine series to meet previously established progression criteria for efficacy and ADME properties, justifying further development of this compound toward clinical candidate status.
A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria
Margaret A. Phillips,Julie Lotharius,Kennan C. Marsh,John H. White,A. Dayan,Karen L. White,Jacqueline W. Njoroge,F. El Mazouni,Y. Lao,Sreekanth Kokkonda,Diana R. Tomchick,Xiaoyi Deng,T. Laird,Caroline L. Ng,David A. Fidock,Sergio Wittlin,Maria Jose Lafuente-Monasterio,Francisco Javier Gamo Benito,L. M. S. Alonso,María Santos Martínez,María-Belén Jiménez-Díaz,Santiago Ferrer Bazaga,Iñigo Angulo-Barturen,John N. Haselden,James B. Louttit,Yi Cui,Arun Sridhar,Anne-Marie Zeeman,Clemens H. M. Kocken,Robert W. Sauerwein,Koen J. Dechering,Vicky M. Avery,Sandra Duffy,Michael J. Delves,Robert E. Sinden,Andrea Ruecker,Kristina S. Wickham,Rosemary Rochford,Janet Gahagen,Lalitha V. Iyer,Ed Riccio,Jon C. Mirsalis,I. Bathhurst,Thomas Rueckle,Xavier C. Ding,Brice Campo,Didier Leroy,M. J. Rogers,Pradipsinh K. Rathod,Jeremy N. Burrows,Susan A. Charman,Sangeeta N. Bhatia,Sandra March-Riera +52 more
TL;DR: The excellent safety profile, blood- and liver-stage activity, and predicted long half-life in humans position DSM265 as a new potential drug combination partner for either single-dose treatment or once-weekly chemoprevention of malaria.
Journal ArticleDOI
Lead-optimization of aryl and aralkyl amine based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice
Ramesh Gujjar,Farah El Mazouni,Karen L. White,John H. White,Sharon A. Creason,David M. Shackleford,Xiaoyi Deng,William N. Charman,Ian Bathurst,Jeremy N. Burrows,David M. Floyd,David Matthews,Frederick S. Buckner,Susan A. Charman,Margaret A. Phillips,Pradipsinh K. Rathod +15 more
TL;DR: Systematic efforts to optimize the aromatic functionality with the goal of improving potency and in vivo properties of compounds from the triazolopyrimidine-based Plasmodium falciparum dihydroorotate dehydrogenase-based series led to the identification of two new substituted aniline moieties.
Journal ArticleDOI
Novel Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Anti-malarial Activity in the Mouse Model
Michael Booker,Cecilia M. Bastos,Martin Kramer,Robert H. Barker,Renato Skerlj,Amar Bir Singh Sidhu,Xiaoyi Deng,Cassandra Celatka,Joseph F. Cortese,Jose E. Guerrero Bravo,Keila N. Crespo Llado,Adelfa E. Serrano,Iñigo Angulo-Barturen,María Belén Jiménez-Díaz,Sara Viera,Helen Garuti,Sergio Wittlin,Sergio Wittlin,Petros Papastogiannidis,Petros Papastogiannidis,Jing-wen Lin,Chris J. Janse,Shahid M. Khan,Manoj T. Duraisingh,Bradley I. Coleman,Elizabeth J. Goldsmith,Margaret A. Phillips,Benito Munoz,Dyann F. Wirth,Jeffrey D. Klinger,Roger C. Wiegand,Edmund Sybertz +31 more
TL;DR: A series of N-alkyl-5-(1H-benzimidazol-1-yl)thiophene-2-carboxamides with low nanomolar in vitro potency against DHODH demonstrated good tolerability and oral exposure in the mouse, and ED50 values in the 4-day murine P. berghei efficacy model resulted in sterile cure.