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James J Mousseau

Explore the profile of James J Mousseau including associated specialties, affiliations and a list of published articles. Areas
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Articles 45
Citations 662
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Recent Articles
1.
Gerstenberger B, Unwalla R, Farley K, Nuhant P, Lombardo V, Li W, et al.
J Med Chem . 2025 Feb; 68(4):4818-4828. PMID: 39960418
CCR6 is a chemokine receptor that mediates the migration of pathogenic inflammatory leukocytes to sites of inflammation in response to its ligand, CCL20. Herein we report the design of a...
2.
Byrnes L, Choi W, Balbo P, Banker M, Chang J, Chen S, et al.
ACS Chem Biol . 2024 Sep; 19(10):2186-2197. PMID: 39316753
Peptidyl arginine deiminases (PADs) are important enzymes in many diseases, especially those involving inflammation and autoimmunity. Despite many years of effort, developing isoform-specific inhibitors has been a challenge. We describe...
3.
Wasilko D, Gerstenberger B, Farley K, Li W, Alley J, Schnute M, et al.
Nat Commun . 2024 Aug; 15(1):7574. PMID: 39217154
The CC chemokine receptor 6 (CCR6) is a potential target for chronic inflammatory diseases. Previously, we reported an active CCR6 structure in complex with its cognate chemokine CCL20, revealing the...
4.
Raina K, Forbes C, Stronk R, Rappi Jr J, Eastman K, Zaware N, et al.
Cell Chem Biol . 2024 Aug; 31(8):1490-1502.e42. PMID: 39116881
We describe a protein proximity inducing therapeutic modality called Regulated Induced Proximity Targeting Chimeras or RIPTACs: heterobifunctional small molecules that elicit a stable ternary complex between a target protein (TP)...
5.
Nugent J, Lopez-Frances A, Sterling A, Tay M, Frank N, Mousseau J, et al.
Chem Sci . 2024 Jul; 15(28):10918-10925. PMID: 39027309
Bridged bicycloalkanes such as bicyclo[1.1.1]pentanes (BCPs) and bicyclo[3.1.1]heptanes (BCHeps) are important motifs in contemporary drug design due to their potential to act as bioisosteres of disubstituted benzene rings, often resulting...
6.
Allais C, Bernhardson D, Brown A, Chinigo G, Desrosiers J, DiRico K, et al.
Org Process Res Dev . 2023 Aug; PMID: 37552749
Lufotrelvir was designed as a first in class 3CL protease inhibitor to treat COVID-19. Development of lufotrelvir was challenged by its relatively poor stability due to its propensity to epimerize...
7.
Dubois M, Rojas J, Sterling A, Broderick H, Smith M, White A, et al.
J Org Chem . 2023 Mar; 88(10):6476-6488. PMID: 36868184
Four-membered heterocycles offer exciting potential as small polar motifs in medicinal chemistry but require further methods for incorporation. Photoredox catalysis is a powerful method for the mild generation of alkyl...
8.
Raina K, Forbes C, Stronk R, Rappi Jr J, Eastman K, Gerritz S, et al.
bioRxiv . 2023 Jan; PMID: 36711980
While specific cell signaling pathway inhibitors have yielded great success in oncology, directly triggering cancer cell death is one of the great drug discovery challenges facing biomedical research in the...
9.
Rojas J, Torrisi E, Dubois M, Hossain R, White A, Zappia G, et al.
Org Lett . 2022 Mar; 24(12):2365-2370. PMID: 35311271
Annulations that combine diacceptors with bis-nucleophiles are uncommon. Here, we report the synthesis of 1,4-dioxanes from 3-aryloxetan-3-ols, as 1,2-bis-electrophiles and 1,2-diols. Brønsted acid TfNH catalyzes both the selective activation of...
10.
Rojas J, Croft R, Sterling A, Briggs E, Antermite D, Schmitt D, et al.
Nat Chem . 2022 Jan; 14(2):160-169. PMID: 35087220
Bioisosteres provide valuable design elements that medicinal chemists can use to adjust the structural and pharmacokinetic characteristics of bioactive compounds towards viable drug candidates. Aryl oxetane amines offer exciting potential...