Drug Discovery Stories, Volume 2

Professor Bin Yu obtained his PhD degree from Zhengzhou University and University of Cambridge and currently is a professor of medicinal chemistry at School of Pharmaceutical Sciences, Zhengzhou University. His research interests focus on chemistry driven drug discovery for novel therapeutics. To date, he has published over 120 papers in international high-impact peer-reviewed journals including Journal of Medicinal Chemistry, Organic Letters, Pharmacology & Therapeutics, Journal of Hematology & Oncology, Drug Discovery Today, Acta Pharmaceutica Sinica B, etc., 10 of them were published in journal with impact factor (IF) >10. Peng Zhan obtained his B.S. degree from Shandong University, China, in 2005. He then earned his M.S. and Ph.D. degrees in medicinal chemistry from Shandong University in 2008 and 2010. He subsequently joined Shandong University as a Lecturer (2010−2012). From 2012 to 2014, he worked as a postdoctoral fellow funded by Japan Society for the Promotion of Science. He is currently a full professor in the Department of Medicinal Chemistry, Shandong University. His research interests involve the discovery of novel anti-viral (HIV, HBV, influenza, coronavirus, etc.), anti-gout, and anti-cancer agents based on rational drug design and combinatorial chemistry approaches. He also co-edited six books published by People's Medical Publishing House and Springer Nature, respectively and granted 50 patents (30 of them licensed). He currently serves as advisory editorial board member of Journal of Medicinal Chemistry.

• 1. Daprodustat (GSK-1278863): A Small Molecule Hypoxia Inducible Factor (HIF)-Prolyl Hydroxylase Inhibitor for Anemia2. Repotrectinib (TPX-0005): a macrocyclic ALK/ROS1/TRK inhibitor for the treatment of non-small cell lung cancer3. FRUZAQLA (fruquintinib): a selective oral inhibitor of VEGFR -1, -2 and -3 for treating for adults with metastatic colorectal cancer4. Ensitrelvir: an orally active 3C-like protease inhibitor for COVID-19.5. Danuglipron: Pioneering Oral GLP1 Receptor Agonists Paving the Way for Revolutionizing Diabetes Treatment6. Remdesivir: An Early Repurposed RNA-Dependent RNA Polymerase Inhibitor for Treating COVID-197. RNK05047: A chaperone-mediated protein degrader that selectively targets BRD4 while recruiting the HSP90 chaperone8. Risdiplam: an Orally Active Survival Motor Neuron (SMN2) pre-mRNA Splicing Modifier for Spinal Muscular Atrophy (SMA) in pediatric and adult patients9. Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections10. Etrasimod: a selective sphingosine-1-phosphate (S1P) receptor modulator for the treatment of ulcerative colitis11. NX-5948: an BTK degrader in Ph. Ia/Ib for patients with advanced B-cell malignancies12. Omaveloxolone (RTA-408): an NRF2 activator for Friedreich's ataxia13. Azvudine: a reverse transcriptase inhibitor for AIDS and COVID-19 treatment14. Leniolisib: a potent and selective PI3Kδ inhibitor for treating activated PI3Kδ syndrome15. Leritrelvir (RAY1216): a novel α-ketoamide based peptidomimetic inhibitor of SARS-CoV-2 main protease for COVID-19 treatment16. Belzutifan: a first-in-class oral HIF-2α inhibitor approved for patients with Von Hippel-Landau (VHL) disease-associated renal cell carcinoma17. Sotagliflozin: a Dual SGLT1/2 Inhibitor, for Full Range of Heart Failure18. Fezolinetant: the first FDA-approved NK3 receptor antagonist for treating moderate-to-severe vasomotor symptoms associated with menopause19. Gepirone: a selective partial agonist of the 5-HT1A Receptor in the treatment of Depression20. Aducanumab: A Milestone in Alzheimer's Disease Treatment Targeting Amyloid Beta Plaques21. Varoglutamstat (PQ912): Navigating the Frontiers of Alzheimer's Treatment22. Lequembi: Pioneering Hope in Neurodegenerative Disorders - A Breakthrough Drug Shaping the Future of Treatment