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Potency of a small molecule that targets the molluscum contagiosum virus processivity factor increases when conjugated to a tripeptide.
Guan, Hancheng; Nuth, Manunya; Scott, Richard W; Parker, Michael H; Strobel, Eric D; Reitz, Allen B; Kulp, John L; Ricciardi, Robert P.
Affiliation
  • Guan H; Department of Basic and Translational Sciences, School of Dental Medicine, University of Pennsylvania, USA.
  • Nuth M; Department of Basic and Translational Sciences, School of Dental Medicine, University of Pennsylvania, USA.
  • Scott RW; Fox Chase Therapeutics Discovery, Inc., USA.
  • Parker MH; Fox Chase Therapeutics Discovery, Inc., USA.
  • Strobel ED; Fox Chase Therapeutics Discovery, Inc., USA.
  • Reitz AB; Fox Chase Therapeutics Discovery, Inc., USA.
  • Kulp JL; Conifer Point Pharmaceuticals, Doylestown, PA, USA.
  • Ricciardi RP; Department of Basic and Translational Sciences, School of Dental Medicine, University of Pennsylvania, USA; Abramson Cancer Center, School of Medicine, University of Pennsylvania, USA. Electronic address: ricciard@upenn.edu.
Antiviral Res ; 226: 105899, 2024 Jun.
Article in En | MEDLINE | ID: mdl-38705201
ABSTRACT
We recently developed compound FC-7269 for targeting the Molluscum contagiosum virus processivity factor (mD4) and demonstrated its ability to inhibit viral processive DNA synthesis in vitro and cellular infection of an mD4-dependent virus (Antiviral Res 211, 2023,105520). However, despite a thorough medicinal chemistry campaign we were unable to generate a potent second analog as a requisite for drug development. We overcame this impasse, by conjugating a short hydrophobic trivaline peptide to FC-7269 to produce FC-TriVal-7269 which significantly increased antiviral potency and reduced cellular toxicity.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Antiviral Agents / Molluscum contagiosum virus Limits: Animals / Humans Language: En Journal: Antiviral Res Year: 2024 Document type: Article Affiliation country: United States
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Antiviral Agents / Molluscum contagiosum virus Limits: Animals / Humans Language: En Journal: Antiviral Res Year: 2024 Document type: Article Affiliation country: United States