日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

The ATM Kinase Inhibitor AZD0156 Is a Potent Inhibitor of Plasmodium Phosphatidylinositol 4-Kinase (PI4Kβ) and Is an Attractive Candidate for Medicinal Chemistry Optimization Against Malaria

ATM激酶抑制剂AZD0156是疟原虫磷脂酰肌醇4-激酶(PI4Kβ)的强效抑制剂,是抗疟药物化学优化的理想候选药物。

Woodland, John G; Coertzen, Dina; Wicht, Kathryn J; Hidalgo, Virginia Franco; Pasaje, Charisse Flerida A; Godoy, Luiz C; Qahash, Tarrick; Mmonwa, Mmakwena M; Dziwornu, Godwin A; Wambua, Lynn; Harries, Sarah; Korkor, Constance M; Njoroge, Mathew; Krugmann, Liezl; Taylor, Dale; Leshabane, Meta; Langeveld, Henrico; Rabie, Tayla; Reader, Janette; van der Watt, Mariëtte; Venter, Nelius; Erlank, Erica; Aswat, Ayesha S; Koekemoer, Lizette L; Yeo, Tomas; Jeon, Jin H; Fidock, David A; Gamo, Francisco Javier; Wittlin, Sergio; Niles, Jacquin C; Llinas, Manuel; Coulson, Lauren B; Birkholtz, Lyn-Marié; Chibale, Kelly

Optimization and Characterization of N-Acetamide Indoles as Antimalarials That Target PfATP4

优化和表征靶向 PfATP4 的 N-乙酰胺吲哚类抗疟药

Awalt, Jon Kyle; Ooi, Zi Kang; Ashton, Trent D; Mansouri, Mahta; Calic, Petar P S; Zhou, Qingmiao; Vasanthan, Santhya; Lee, Serena; Loi, Katie; Jarman, Kate E; Penington, Jocelyn S; Qiu, Deyun; Zhang, Xinxin; Lehane, Adele M; Mao, Emma Y; Gancheva, Maria R; Wilson, Danny W; Giannangelo, Carlo; MacRaild, Christopher A; Creek, Darren J; Yeo, Tomas; Sheth, Tanaya; Fidock, David A; Churchyard, Alisje; Baum, Jake; Famodimu, Mufuliat T; Delves, Michael J; Kristan, Mojca; Stewart, Lindsay; Sutherland, Colin J; Coyle, Rachael; Jagoe, Hannah; Lee, Marcus C S; Chowdury, Mrittika; de Koning-Ward, Tania F; Baud, Delphine; Brand, Stephen; Jackson, Paul F; Cowman, Alan F; Dans, Madeline G; Sleebs, Brad E

Optimization and Characterization of the Antimalarial Activity of N-Aryl Acetamides that are Susceptible to Mutations in ROM8 and CSC1

对易受ROM8和CSC1突变影响的N-芳基乙酰胺类化合物的抗疟活性进行优化和表征

Nguyen, William; Boulet, Coralie; Dans, Madeline G; Loi, Katie; Jarman, Kate E; Barnes, Claudia B G; Yeo, Tomas; Sheth, Tanaya; Mukherjee, Partha; Chakraborty, Arnish; Famodimu, Mufuliat T; Delves, Michael J; Pollard, Harry; Sutherland, Colin J; Coyle, Rachael; Sevilleno, Nicole; Boonyalai, Nonlawat; Lee, Marcus C S; Rabie, Tayla; Birkholtz, Lyn-Marié; Baud, Delphine; Brand, Stephen; Chowdury, Mrittika; de Koning-Ward, Tania F; Fidock, David A; Gilson, Paul R; Sleebs, Brad E

Quinoxaline-based anti-schistosomal compounds have potent anti-plasmodial activity.

喹喔啉类抗血吸虫化合物具有很强的抗疟原虫活性

Rawat Mukul, Padalino Gilda, Adika Edem, Okombo John, Yeo Tomas, Brancale Andrea, Fidock David A, Hoffmann Karl F, Lee Marcus C S

Plasmodium falciparum African PfCRT Mutant Isoforms Conducive to Piperaquine Resistance Are Infrequent and Impart a Major Fitness Cost

恶性疟原虫非洲型PfCRT突变异构体虽然罕见,但会导致哌喹耐药性,且会造成严重的适应性损失。

Hagenah, Laura M; Yeo, Tomas; Schindler, Kyra A; Jeon, Jin H; Bloxham, Talia S; Small-Saunders, Jennifer L; Mok, Sachel; Fidock, David A

Collateral hypersensitivity between ZY19489 and piperaquine neutralizes PfCRT-mediated drug efflux and Plasmodium falciparum resistance

ZY19489 与哌喹之间的协同超敏反应可中和 PfCRT 介导的药物外排和恶性疟原虫耐药性。

Okombo, John; Ndiaye, Tolla; Qahash, Tarrick; Moura, Igor M R; Gil-Iturbe, Eva; Hagenah, Laura M; Bridgford, Jessica L; Bonatto, Vinicius; Ward, Kurt E; Yeo, Tomas; Narwal, Sunil K; Orta, Lily V; Anderson, Isla; Dhingra, Satish K; Pasaje, Charisse Flerida A; Park, Heekuk; Kim, Jonathan; Guido, Rafael V C; Angulo-Barturen, Iñigo; Niles, Jacquin C; Mancia, Filippo; Uhlemann, Anne-Catrin; Mok, Sachel; Quick, Matthias; Winzeler, Elizabeth A; Leroy, Didier; Llinás, Manuel; Thathy, Vandana; Fidock, David A

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

疟原虫HSP90抑制剂的共同结合位点和不同的耐药谱揭示了新的耐药机制

Ko, Fu-Hsuan; Lukens, Amanda K; de Souza, Mariana Laureano; Foy, Alex; Hsiao, Jason; Ndiaye, Tolla; Okombo, John; Yeo, Tomas; Park, Heekuk; Uhlemann, Anne-Catrin; Boonyalai, Nonlawat; Kumpornsin, Krittikorn; Girling, Gareth; Pasaje, Charisse; Godoy, Luiz; Ottilie, Sabine; Durst, Gregory L; Chatterjee, Arnab; Niles, Jacquin; Lee, Marcus; Fidock, David A; Wirth, Dyann F; Winzeler, Elizabeth A

Systematic in vitro evolution in Plasmodium falciparum reveals key determinants of drug resistance.

恶性疟原虫体外系统进化揭示了耐药性的关键决定因素

Luth Madeline R, Godinez-Macias Karla P, Chen Daisy, Okombo John, Thathy Vandana, Cheng Xiu, Daggupati Sindhu, Davies Heledd, Dhingra Satish K, Economy Jan M, Edgar Rebecca C S, Gomez-Lorenzo Maria G, Istvan Eva S, Jado Juan Carlos, LaMonte Gregory M, Melillo Bruno, Mok Sachel, Narwal Sunil K, Ndiaye Tolla, Ottilie Sabine, Palomo Diaz Sara, Park Heekuk, Peña Stella, Rocamora Frances, Sakata-Kato Tomoyo, Small-Saunders Jennifer L, Summers Robert L, Tumwebaze Patrick K, Vanaerschot Manu, Xia Guoqin, Yeo Tomas, You Ashley, Gamo Francisco-Javier, Goldberg Daniel E, Lee Marcus C S, McNamara Case W, Ndiaye Daouda, Rosenthal Philip J, Schreiber Stuart L, Serra Gloria, De Siqueira-Neto Jair Lage, Skinner-Adams Tina S, Uhlemann Anne-Catrin, Kato Nobutaka, Lukens Amanda K, Wirth Dyann F, Fidock David A, Winzeler Elizabeth A

Inhibitors of malaria parasite cyclic nucleotide phosphodiesterases block asexual blood-stage development and mosquito transmission.

疟原虫环核苷酸磷酸二酯酶抑制剂可阻断无性血液期发育和蚊子传播

Gomez-Gonzalez Paula-Josefina, Gupta Antima, Drought Laura G, Patel Avnish, Okombo John, van der Watt Mariëtte, Walker-Gray Ryan, Schindler Kyra A, Burkhard Anna Y, Yeo Tomas, Narwal Sunil K, Bloxham Talia S, Flueck Christian, Walker Eloise M, Rey Joshua A, Fairhurst Kate J, Reader Janette, Park Heekuk, Pollard Harry G, Stewart Lindsay B, Brandner-Garrod Luke, Kristan Mojca, Sterk Geert-Jan, van Nuland Youri M, Manko Emilia, van Schalkwyk Donelly A, Zheng Yang, Leurs Rob, Dechering Koen J, Aguiar Anna Caroline C, Guido Rafael V C, Pereira Dhelio B, Tumwebaze Patrick K, Nosbya Samuel L, Rosenthal Philip J, Cooper Roland A, Palmer Mike, Parkinson Tanya, Burrows Jeremy N, Uhlemann Anne-Catrin, Birkholtz Lyn-Marié, Small-Saunders Jennifer L, Duffy James, Fidock David A, Brown Alan, Gardner Mark, Baker David A

Exploration and characterization of the antimalarial activity of cyclopropyl carboxamides that target the mitochondrial protein, cytochrome b

探索和表征靶向线粒体蛋白细胞色素b的环丙基羧酰胺类化合物的抗疟活性

Awalt, Jon Kyle; Su, Wenyin; Nguyen, William; Loi, Katie; Jarman, Kate E; Penington, Jocelyn S; Ramesh, Saishyam; Fairhurst, Kate J; Yeo, Tomas; Park, Heekuk; Uhlemann, Anne-Catrin; Chandra Maity, Bikash; De, Nirupam; Mukherjee, Partha; Chakraborty, Arnish; Churchyard, Alisje; Famodimu, Mufuliat T; Delves, Michael J; Baum, Jake; Mittal, Nimisha; Winzeler, Elizabeth A; Papenfuss, Anthony T; Chowdury, Mrittika; de Koning-Ward, Tania F; Maier, Alexander G; van Dooren, Giel G; Baud, Delphine; Brand, Stephen; Fidock, David A; Jackson, Paul F; Cowman, Alan F; Dans, Madeline G; Sleebs, Brad E