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Discovery and structural diversity of the hepatitis C virus NS3/4A serine protease inhibitor series leading to clinical candidate IDX320. 2015
Christophe C Parsy, and
François-René Alexandre, and
Valérie Bidau, and
Florence Bonnaterre, and
Guillaume Brandt, and
Catherine Caillet, and
Sylvie Cappelle, and
Dominique Chaves, and
Thierry Convard, and
Michel Derock, and
Damien Gloux, and
Yann Griffon, and
Lisa B Lallos, and
Frederic Leroy, and
Michel Liuzzi, and
Anna-Giulia Loi, and
Laure Moulat, and
Musiu Chiara, and
Houcine Rahali, and
Virginie Roques, and
Elodie Rosinovsky, and
Simon Savin, and
Maria Seifer, and
David Standring, and
Dominique Surleraux
IDENIX, a wholly-owned subsidiary of Merck & Co, 1682 rue de la Valsière, Cap Gamma, BP 50001, 34189 Montpellier Cedex 4, France. Electronic address: christophe.parsy@merck.com.
Exploration of the P2 region by mimicking the proline motif found in BILN2061 resulted in the discovery of two series of potent HCV NS3/4A protease inhibitors. X-ray crystal structure of the ligand in contact with the NS3/4A protein and modulation of the quinoline heterocyclic region by structure based design and modeling allowed for the optimization of enzyme potency and cellular activity. This research led to the selection of clinical candidate IDX320 having good genotype coverage and pharmacokinetic properties in various species.
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