9bjm
From Proteopedia
Crystal Structure of Inhibitor 5c in Complex with Prefusion RSV F Glycoprotein
Structural highlights
FunctionPublication Abstract from PubMedRespiratory syncytial virus (RSV) is a major cause of hospitalization in infants, the elderly, and immune-compromised patients. While a half-life extended monoclonal antibody and 2 vaccines have recently been approved for infants and the elderly, respectively, options to prevent disease in immune-compromised patients are still needed. Here, we describe spiro-azetidine oxindoles as small molecule RSV entry inhibitors displaying favorable potency, developability attributes, and long-acting PK when injected as an aqueous suspension, suggesting their potential to prevent complications following RSV infection over a period of 3 to 6 months with 1 or 2 long-acting intramuscular (IM) or subcutaneous (SC) injections in these immune-compromised patients. Spiro-Azetidine Oxindoles as Long-Acting Injectables for Pre-Exposure Prophylaxis against Respiratory Syncytial Virus Infections.,Kesteleyn B, Herschke F, Darville N, Stoops B, Jacobs T, Jacoby E, Shaffer P, Lammens L, Van Rompaey D, Matcha K, Martinez Lamenca C, Coesemans E, Hache G, Pieters S, Lecomte M, Hu L, Demin S, Milligan C, Abeywickrema P, De Bruyn S, Van Den Berg J, Ysebaert N, De Zwart L, Najera I, Rigaux P, Roymans D, Jonckers THM J Med Chem. 2024 Jul 11;67(13):10986-11002. doi: 10.1021/acs.jmedchem.4c00514. , Epub 2024 Jun 26. PMID:38932487[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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