Publications by authors named "B Scorneaux"
Exploiting the intrinsic misfolding propensity of the KRAS oncoprotein.
Proc Natl Acad Sci U S A
February 2023
Article Synopsis
- Mutant KRAS is a key factor in many cancers but is difficult to target with traditional drugs, prompting researchers to seek alternative methods.
- The study reveals that specific regions in KRAS are prone to aggregation, especially in common mutations, making them potential weak points that can be manipulated.
- By using synthetic peptides (Pept-ins™) from these regions, researchers were able to induce misfolding of mutant KRAS, leading to reduced cancer cell growth and tumor shrinkage in mice.
SCY-078 Is Fungicidal against Candida Species in Time-Kill Studies.
Antimicrob Agents Chemother
March 2017
SCY-078 is an orally bioavailable ß-1,3-glucan synthesis inhibitor (GSI) and the first-in-class of structurally novel triterpene antifungals in clinical development for treating candidemia and invasive candidiasis. susceptibilities by broth microdilution, antifungal carryover, and time-kill dynamics were determined for three reference (ATCC) strains ( 90028, 90018, and 750), a quality-control (QC) strain ( 6258), and four other strains ( MYA-2732, 64124, and 76485 and 90030). Caspofungin (CASP), fluconazole (FLC), and voriconazole (VRC) were comparators.
View Article and Find Full Text PDFBackground & Aims: SCY-635 is a non-immunosuppressive analog of cyclosporin A that inhibits cyclophilins A and B and hepatitis C virus (HCV) replication in vitro. In a phase 1b multi-dose escalation study, we evaluated the safety, plasma pharmacokinetics, and antiviral activity of 15 days of monotherapy with SCY-635 in adults with chronic genotype 1 HCV infection.
Methods: Twenty adults with chronic HCV genotype 1 were randomized to SCY-635 oral doses of 100, 200, or 300 mg three times daily for 15 days.
Article Synopsis
- - A new method for synthesizing [D-lysine](8)cyclosporin A has been created, making the process more efficient.
- - Various analogs of [D-lysine](8)cyclosporin A have been produced, showing potential effectiveness against HCV (hepatitis C virus).
- - Notably, compounds 39 and 43 demonstrated strong anti-HCV activity with EC(50) values under 200 nM and are significantly less immunosuppressive compared to the original cyclosporin A.
SCY-635 is a novel nonimmunosuppressive cyclosporine-based analog that exhibits potent suppression of hepatitis C virus (HCV) replication in vitro. SCY-635 inhibited the peptidyl prolyl isomerase activity of cyclophilin A at nanomolar concentrations but showed no detectable inhibition of calcineurin phosphatase activity at concentrations up to 2 microM. Metabolic studies indicated that SCY-635 did not induce the major cytochrome P450 enzymes 1A2, 2B6, and 3A4.
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