C
Cassandra Celatka
Researcher at Genzyme
Publications - 20
Citations - 578
Cassandra Celatka is an academic researcher from Genzyme. The author has contributed to research in topics: Dihydroorotate dehydrogenase & Plasmodium falciparum. The author has an hindex of 11, co-authored 19 publications receiving 547 citations. Previous affiliations of Cassandra Celatka include Massachusetts Institute of Technology.
Papers
More filters
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.
Journal ArticleDOI
Identification and characterization of small molecule inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
Vishal Patel,Michael Booker,Martin Kramer,Leila S. Ross,Cassandra Celatka,Leah M. Kennedy,Jeffrey D. Dvorin,Jeffrey D. Dvorin,Manoj T. Duraisingh,Piotr Sliz,Dyann F. Wirth,Jon Clardy +11 more
TL;DR: Using a target-based high throughput screen, a series of potent, species-specific inhibitors of P. falciparum DHOD are identified and validated as an antimalarial drug target and provide chemical scaffolds with which to begin medicinal chemistry efforts.
Journal ArticleDOI
Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants.
Jian Lin,Hongfeng Deng,Lei Jin,Pramod Pandey,Jesse Quinn,Susan M. Cantin,Michael J. Rynkiewicz,Joan C. Gorga,Frank Bibbins,Cassandra Celatka,Pamela Nagafuji,Thomas D. Bannister,Harold V Meyers,Robert E. Babine,Neil J Hayward,David R. Weaver,Howard Benjamin,Frans L Stassen,Sherin S. Abdel-Meguid,James E. Strickler +19 more
TL;DR: The data suggest that factor XIa plays a significant role in venous thrombosis and may be a suitable target for the development of antithrombotic therapy.
Journal ArticleDOI
Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an alpha-ketothiazole arginine.
Hongfeng Deng,Thomas D. Bannister,Lei Jin,Robert E. Babine,Jesse Quinn,Pamela Nagafuji,Cassandra Celatka,Jian Lin,Tsvetelina I. Lazarova,Michael J. Rynkiewicz,Frank Bibbins,Pramod Pandey,Joan C. Gorga,Harold V Meyers,Sherin S. Abdel-Meguid,James E. Strickler +15 more
TL;DR: Using an alpha-ketothiazole arginine moiety as a key recognition element, a series of small peptidomimetic molecules was designed and synthesized, and their co-crystal structures with factor XIa were studied in an effort to develop smaller, less peptidic inhibitors as antithrombotic agents.
Journal ArticleDOI
Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria.
Renato Skerlj,Cecilia M. Bastos,Michael Booker,Martin Kramer,Robert H. Barker,Cassandra Celatka,Thomas O'Shea,Benito Munoz,Amar Bir Singh Sidhu,Joseph F. Cortese,Sergio Wittlin,Sergio Wittlin,Petros Papastogiannidis,Petros Papastogiannidis,Iñigo Angulo-Barturen,María Belén Jiménez-Díaz,Edmund Sybertz +16 more
TL;DR: The synthesis and structure-activity relationship of a series of 5-(2-methylbenzimidazol-1-yl)-N-alkylthiophene-2-carboxamides that are potent inhibitors against PfDHODH but do not inhibit the human enzyme are reported.