Jean-Pierre Falgueyret
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Explore the profile of Jean-Pierre Falgueyret including associated specialties, affiliations and a list of published articles.
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41
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621
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Recent Articles
1.
Bubenik M, Mader P, Mochirian P, Vallee F, Clark J, Truchon J, et al.
J Med Chem
. 2022 Sep;
65(19):13198-13215.
PMID: 36126059
DNA polymerase theta (Polθ) is an attractive synthetic lethal target for drug discovery, predicted to be efficacious against breast and ovarian cancers harboring BRCA-mutant alleles. Here, we describe our hit-to-lead...
2.
Fossati E, Narcross L, Ekins A, Falgueyret J, Martin V
PLoS One
. 2015 Apr;
10(4):e0124459.
PMID: 25905794
Morphinan alkaloids are the most powerful narcotic analgesics currently used to treat moderate to severe and chronic pain. The feasibility of morphinan synthesis in recombinant Saccharomyces cerevisiae starting from the...
3.
Fossati E, Ekins A, Narcross L, Zhu Y, Falgueyret J, Beaudoin G, et al.
Nat Commun
. 2014 Feb;
5:3283.
PMID: 24513861
Benzylisoquinoline alkaloids (BIAs) represent a large class of plant secondary metabolites, including pharmaceuticals such as morphine, codeine and their derivatives. Large-scale production of BIA-based pharmaceuticals is limited to extraction and...
4.
Cote B, Burch J, Asante-Appiah E, Bayly C, Bedard L, Blouin M, et al.
Bioorg Med Chem Lett
. 2014 Jan;
24(3):917-22.
PMID: 24412110
The optimization of a novel series of non-nucleoside reverse transcriptase inhibitors (NNRTI) led to the identification of pyridone 36. In cell cultures, this new NNRTI shows a superior potency profile...
5.
Lai M, Feng M, Falgueyret J, Tawa P, Witmer M, DiStefano D, et al.
Antimicrob Agents Chemother
. 2014 Jan;
58(3):1652-63.
PMID: 24379202
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are a mainstay of therapy for treating human immunodeficiency type 1 virus (HIV-1)-infected patients. MK-1439 is a novel NNRTI with a 50% inhibitory concentration (IC50)...
6.
Singhroy D, Mesplede T, Sabbah A, Quashie P, Falgueyret J, Wainberg M
Retrovirology
. 2013 Jul;
10:73.
PMID: 23866860
Background: Protein arginine methyltransferase 6 (PRMT6) is a nuclear enzyme that methylates arginine residues on histones and transcription factors. In addition, PRMT6 inhibits HIV-1 replication in cell culture by directly...
7.
Fournier P, Arbour M, Cauchon E, Chen A, Chefson A, Ducharme Y, et al.
Bioorg Med Chem Lett
. 2012 Mar;
22(8):2670-4.
PMID: 22450130
The design and optimization of a novel isoxazole S(1) linker for renin inhibitor is described herein. This effort culminated in the identification of compound 18, an orally bioavailable, sub-nanomolar renin...
8.
Lacombe P, Arbour M, Aspiotis R, Cauchon E, Chen A, Dube D, et al.
Bioorg Med Chem Lett
. 2012 Feb;
22(5):1953-7.
PMID: 22325946
The discovery and SAR of a series of potent renin inhibitors possessing a novel 3,4-diarylpiperidine scaffold are described herein. The resulting compound 38 exhibit low nanomolar plasma renin IC(50), had...
9.
Chen A, Aspiotis R, Campeau L, Cauchon E, Chefson A, Ducharme Y, et al.
Bioorg Med Chem Lett
. 2011 Nov;
21(24):7399-404.
PMID: 22071301
The discovery and SAR of a novel series of spirocyclic renin inhibitors are described herein. It was found that by restricting the northern aromatic plate to the bioactive conformation through...
10.
Leclerc J, Falgueyret J, Girardin M, Guay J, Guiral S, Huang Z, et al.
Bioorg Med Chem Lett
. 2011 Sep;
21(21):6505-9.
PMID: 21924609
It has been demonstrated that once-a-day dosing of systemically-distributed SCD inhibitors leads to adverse events in eye and skin. Herein, we describe our efforts to convert a novel class of...