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Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Lorthiois, Edwige; Roache, James; Barnes-Seeman, David; Altmann, Eva; Hassiepen, Ulrich; Turner, Gordon; Duvadie, Rohit; Hornak, Viktor; Karki, Rajeshri G; Schiering, Nikolaus; Weihofen, Wilhelm A; Perruccio, Francesca; Calhoun, Amy; Fazal, Tanzina; Dedic, Darija; Durand, Corinne; Dussauge, Solene; Fettis, Kamal; Tritsch, Fabien; Dentel, Celine; Druet, Adelaide; Liu, Donglei; Kirman, Louise; Lachal, Julie; Namoto, Kenji; Bevan, Douglas; Mo, Rose; Monnet, Gabriela; Muller, Lionel; Zessis, Richard; Huang, Xueming; Lindsley, Loren; Currie, Treeve; Chiu, Yu-Hsin; Fridrich, Cary; Delgado, Peter; Wang, Shuangxi; Hollis-Symynkywicz, Micah; Berghausen, Joerg; Williams, Eric; Liu, Hong; Liang, Guiqing; Kim, Hyungchul; Hoffmann, Peter; Hein, Andreas; Ramage, Paul; D'Arcy, Allan; Harlfinger, Stefanie; Renatus, Martin; Ruedisser, Simon.
Affiliation
  • Lorthiois E; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Roache J; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Barnes-Seeman D; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Altmann E; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Hassiepen U; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Turner G; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Duvadie R; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Hornak V; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Karki RG; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Schiering N; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Weihofen WA; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Perruccio F; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Calhoun A; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Fazal T; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Dedic D; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Durand C; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Dussauge S; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Fettis K; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Tritsch F; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Dentel C; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Druet A; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Liu D; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Kirman L; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Lachal J; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Namoto K; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Bevan D; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Mo R; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Monnet G; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Muller L; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Zessis R; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Huang X; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Lindsley L; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Currie T; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Chiu YH; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Fridrich C; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Delgado P; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Wang S; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Hollis-Symynkywicz M; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Berghausen J; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Williams E; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Liu H; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Liang G; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Kim H; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Hoffmann P; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Hein A; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Ramage P; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • D'Arcy A; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Harlfinger S; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Renatus M; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
  • Ruedisser S; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
J Med Chem ; 63(15): 8088-8113, 2020 08 13.
Article de En | MEDLINE | ID: mdl-32551603

Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Sujet principal: Facteur XIa / Inhibiteurs du facteur Xa Type d'étude: Prognostic_studies Limites: Animals / Humans / Male Langue: En Journal: J Med Chem Sujet du journal: QUIMICA Année: 2020 Type de document: Article Pays d'affiliation: Suisse Pays de publication: États-Unis d'Amérique

Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Sujet principal: Facteur XIa / Inhibiteurs du facteur Xa Type d'étude: Prognostic_studies Limites: Animals / Humans / Male Langue: En Journal: J Med Chem Sujet du journal: QUIMICA Année: 2020 Type de document: Article Pays d'affiliation: Suisse Pays de publication: États-Unis d'Amérique