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A Novel Class of Orally Bioavailable Phenylglycine-Benzoxaborole Conjugates with Antimalarial Activity and Potentially Novel Mechanism of Action 一类具有抗疟活性和潜在新型作用机制的新型口服生物利用型苯甘氨酸-苯并硼杂唑偶联物 Morake, Mokhitli; Taylor, Dale; Coertzen, Dina; Njoroge, Mathew; Krugmann, Liezl; Leshabane, Meta; Da Rocha, Shante; Qahash, Tarrick; Girling, Gareth; Coyle, Rachael; Lee, Marcus C. S.; Wittlin, Sergio; Llinas, Manuel; Birkholtz, Lyn-Marie; Basarab, Gregory S.; Chibale, Kelly 分享 收藏
Medicinal Chemistry Progression of Sapanisertib, the Anticancer and Dual Plasmodium Phosphatidylinositol 4-Kinase Beta and cGMP-Dependent Protein Kinase Inhibitor, for Malaria Sapanisertib的药物化学进展，该化合物为一种抗癌药物，同时是疟原虫磷脂酰肌醇4-激酶β和cGMP依赖性蛋白激酶的双重抑制剂，用于疟疾治疗。 Gachuhi, Samuel; Kamunya, Stephanie; Fienberg, Stephen; Wambua, Lynn; Salomane, Nicolaas; Mayoka, Godfrey; Taylor, Dale; Coertzen, Dina; van der Watt, Mariette; Reader, Janette; Birkholtz, Lyn-Marie; Wittlin, Sergio; Krugmann, Liezl; Coulson, Lauren B.; Chibale, Kelly 分享 收藏
Cell-Based Progression of Spiroindoline Phenotypic Hits Leads to the Identification of Compounds with Diverging Parasitological Profiles against the Human Malaria Parasite Plasmodium falciparum 基于细胞模型的螺吲哚啉表型活性化合物的优化鉴定出对人类疟原虫 *Plasmodium falciparum* 具有不同寄生虫学特征的化合物 Dam, Jean; Boyle, Grant A.; Horatscheck, Andre; Woodland, John G.; Le Manach, Claire; Kaur, Gurminder; Taylor, Dale; Krugmann, Liezl; Njoroge, Mathew; Lawrence, Nina; Brunschwig, Christel; Zdorichenko, Victor; Cox, Brian; Wittlin, Sergio; von Geldern, Thomas W.; Smith, Dennis; Duffy, James; Basarab, Gregory S. 分享 收藏
TKK130 is a 3-Hydroxy-Propanamidine (HPA) with Potent Antimalarial In Vivo Activity and a High Barrier to Resistance Knaab, Tanja C.; Moritz, Alena; de Carvalho, Lais Pessanha; Klein, Saskia; Lungerich, Beate; Lohse, Katharina; Kruse, Linn; Mombo-Ngoma, Ghyslain; Orta, Lily; Thibaud, Jessica L.; de Villiers, Katherine A.; Fidock, David A.; Burckhardt, Bjoern B.; Held, Jana; Wittlin, Sergio; Kurz, Thomas 分享 收藏
A potent and selective reaction hijacking inhibitor of Plasmodium falciparum tyrosine tRNA synthetase exhibits single dose oral efficacy in vivo Xie, Stanley C.; Tai, Chia-Wei; Morton, Craig J.; Ma, Liting; Huang, Shih-Chung; Wittlin, Sergio; Du, Yawei; Hu, Yongbo; Dogovski, Con; Salimimarand, Mina; Griffin, Robert; England, Dylan; de la Cruz, Elisa; Deni, Ioanna; Yeo, Tomas; Burkhard, Anna Y.; Striepen, Josefine; Schindler, Kyra A.; Crespo, Benigno; Gamo, Francisco J.; Khandokar, Yogesh; Hutton, Craig A.; Rabie, Tayla; Birkholtz, Lyn-Marie; Famodimu, Mufuliat T.; Delves, Michael J.; Bolsher, Judith; Koolen, Karin M. J.; van der Laak, Rianne; Aguiar, Anna C. C.; Pereira, Dhelio B.; Guido, Rafael V. C.; Creek, Darren J.; Fidock, David A.; Dick, Lawrence R.; Brand, Stephen L.; Gould, Alexandra E.; Langston, Steven; Griffin, Michael D. W.; Tilley, Leann 分享 收藏
Total Synthesis of Tosyl-Samroiyotmycin A and Its Biological Profiling Kolb, Benedikt; Schmid, Fabian; Weng, Jessica; Altevogt, Luca; Rebelo, Ruben Pereira; Wank, Bianca; Baro, Angelika; Zens, Anna; Shekhar, Aditya; Bilitewski, Ursula; Sax, Sibylle; Wittlin, Sergio; Taylor, Dale; Muller, Rudolf; Laschat, Sabine 分享 收藏
Addressing the Intracellular Vestibule of the Plasmodial Lactate Transporter PfFNT by p-Substituted Inhibitors Amplifies In Vitro Activity Nerlich, Cornelius; Tiedjens, Finn; Hertel, Robin; Henke, Bjoern; Haeuer, Susan; Panitzsch, Lea S.; Hansen, Kerrin; Franck, Ole; Mete, Antonio; Leroy, Didier; Schade, Dennis; Peifer, Christian; Hannus, Stefan; Becker, Frank; Wittlin, Sergio; Spielmann, Tobias; Beitz, Eric 分享 收藏
Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3 具有有效抗疟活性的吡唑并吡啶4-甲酰胺的优化，其抗性与恶性疟原虫转运蛋白ABCI3相关 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, Benoit; Sleebs, Brad E. 分享 收藏
Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria 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, Inigo; Jimenez-Diaz, Maria Belen; Wittlin, Sergio; Campbell, Simon F.; Fidock, David A.; Laleu, Benoit; Charman, Susan A.; Ready, Joseph M.; Phillips, Margaret A. 分享 收藏
Chemoproteomics validates selective targeting of Plasmodium M1 alanyl aminopeptidase as an antimalarial strategy Giannangelo, Carlo; Challis, Matthew P.; Siddiqui, Ghizal; Edgar, Rebecca; Malcolm, Tess R.; Webb, Chaille T.; Drinkwater, Nyssa; Vinh, Natalie; Macraild, Christopher; Counihan, Natalie; Duffy, Sandra; Wittlin, Sergio; Devine, Shane M.; Avery, Vicky M.; De Koning-Ward, Tania; Scammells, Peter; McGowan, Sheena; Creek, Darren J. 分享 收藏
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2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy Dziwornu, Godwin Akpeko; Seanego, Donald; Fienberg, Stephen; Clements, Monica; Ferreira, Jasmin; Sypu, Venkata S.; Samanta, Sauvik; Bhana, Ashlyn D.; Korkor, Constance M.; Garnie, Larnelle F.; Teixeira, Nicole; Wicht, Kathryn J.; Taylor, Dale; Olckers, Ronald; Njoroge, Mathew; Gibhard, Liezl; Salomane, Nicolaas; Wittlin, Sergio; Mahato, Rohit; Chakraborty, Arnish; Sevilleno, Nicole; Coyle, Rachael; Lee, Marcus C. S.; Godoy, Luiz C.; Pasaje, Charisse Flerida; Niles, Jacquin C.; Reader, Janette; van der Watt, Mariette; Birkholtz, Lyn-Marie; Bolscher, Judith M.; de Bruijni, Marloes H. C.; Coulson, Lauren B.; Basarab, Gregory S.; Ghorpade, Sandeep R.; Chibale, Kelly 分享 收藏
On-target, dual aminopeptidase inhibition provides cross-species antimalarial activity Edgar, Rebecca C. S.; Malcolm, Tess R.; Siddiqui, Ghizal; Giannangelo, Carlo; Counihan, Natalie A.; Challis, Matthew; Duffy, Sandra; Chowdhury, Mrittika; Marfurt, Jutta; Dans, Madeline; Wirjanata, Grennady; Noviyanti, Rintis; Daware, Kajal; Suraweera, Chathura D.; Price, Ric N.; Wittlin, Sergio; Avery, Vicky M.; Drinkwater, Nyssa; Charman, Susan A.; Creek, Darren J.; de Koning-Ward, Tania F.; Scammells, Peter J.; McGowan, Sheena 分享 收藏
Next Generation Chemiluminescent Probes for Antimalarial Drug Discovery Hellingman, Angela; Sifoniou, Kleopatra; Buser, Tamara; Thommen, Basil T.; Walz, Annabelle; Passecker, Armin; Collins, James; Hupfeld, Mario; Wittlin, Sergio; Witmer, Kathrin; Brancucci, Nicolas M. B. 分享 收藏
Activity refinement of aryl amino acetamides that target the P. falciparum STAR-related lipid transfer 1 protein 靶向恶性疟原虫星形相关脂质转移1蛋白的芳基氨基乙酰胺的活性精制 Nguyen, William; Boulet, Coralie; Dans, Madeline G.; Loi, Katie; Jarman, Kate E.; Watson, Gabrielle M.; Tham, Wai-Hong; Fairhurst, Kate J.; Yeo, Tomas; Fidock, David A.; Wittlin, Sergio; Chowdury, Mrittika; de Koning-Ward, Tania F.; Chen, Gong; Yan, Dandan; Charman, Susan A.; Baud, Delphine; Brand, Stephen; Jackson, Paul F.; Cowman, Alan F.; Gilson, Paul R.; Sleebs, Brad E. 分享 收藏
hERG, Plasmodium Life Cycle, and Cross Resistance Profiling of New Azabenzimidazole Analogues of Astemizole Mambwe, Dickson; Coertzen, Dina; Leshabane, Meta; Mulubwa, Mwila; Njoroge, Mathew; Gibhard, Liezl; Girling, Gareth; Wicht, Kathryn J.; Lee, Marcus C. S.; Wittlin, Sergio; Moreira, Diogo Rodrigo Magalhaes; Birkholtz, Lyn-Marie; Chibale, Kelly 分享 收藏
Antimalarial Dibenzannulated Medium-Ring Keto Lactams Ren, Rongguo; Wang, Xiaofang; Leas, Derek A.; Scheurer, Christian; Hoevel, Sarah; Cal, Monica; Chen, Gong; Zhong, Longjin; Katneni, Kasiram; Pham, Thao; Patil, Rahul; Sil, Diptesh; Walters, Matthias J.; Schulze, Thomas T.; Neville, Andrew J.; Dong, Yuxiang; Wittlin, Sergio; Kaiser, Marcel; Davis, Paul H.; Charman, Susan A.; Vennerstrom, Jonathan L. 分享 收藏
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