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29 results

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Page 1
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G. Schnute ME, et al. Among authors: berstein g. J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9. J Med Chem. 2018. PMID: 30130103
Efficacy and safety of topical brepocitinib cream for mild-to-moderate chronic plaque psoriasis: a phase IIb randomized double-blind vehicle-controlled parallel-group study.
Landis MN, Smith SR, Berstein G, Fetterly G, Ghosh P, Feng G, Pradhan V, Aggarwal S, Banfield C, Peeva E, Vincent MS, Beebe JS, Tarabar S. Landis MN, et al. Among authors: berstein g. Br J Dermatol. 2023 Jul 7;189(1):33-41. doi: 10.1093/bjd/ljad098. Br J Dermatol. 2023. PMID: 36972293 Clinical Trial.
Identification of a new class of small molecule C5a receptor antagonists.
Chen JJ, Cole DC, Ciszewski G, Crouse K, Ellingboe JW, Nowak P, Tawa GJ, Berstein G, Li W. Chen JJ, et al. Among authors: berstein g. Bioorg Med Chem Lett. 2010 Jan 15;20(2):662-4. doi: 10.1016/j.bmcl.2009.11.058. Epub 2009 Dec 7. Bioorg Med Chem Lett. 2010. PMID: 20004096
Macrocyclic Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonists.
Schnute ME, Trujillo JI, Lee KL, Unwalla R, Vajdos FF, Kauppi B, Nuhant P, Flick AC, Crouse KK, Zhao Y, Samuel A, Lombardo V, Taylor AP, Brault AL, Knafels JD, Vazquez ML, Berstein G. Schnute ME, et al. Among authors: berstein g. ACS Med Chem Lett. 2023 Jan 18;14(2):191-198. doi: 10.1021/acsmedchemlett.2c00500. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793423 Free PMC article.
A Novel C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) Antagonist (PF-07054894) Distinguishes between Homologous Chemokine Receptors, Increases Basal Circulating CCR6+ T Cells, and Ameliorates Interleukin-23-Induced Skin Inflammation.
Li W, Crouse KK, Alley J, Frisbie RK, Fish SC, Andreyeva TA, Reed LA, Thorn M, DiMaggio G, Donovan CB, Bennett D, Garren J, Oziolor E, Qian J, Newman L, Vargas AP, Kumpf SW, Steyn SJ, Schnute ME, Thorarensen A, Hegen M, Stevens E, Collinge M, Lanz TA, Vincent F, Vincent MS, Berstein G. Li W, et al. Among authors: berstein g. J Pharmacol Exp Ther. 2023 Jul;386(1):80-92. doi: 10.1124/jpet.122.001452. Epub 2023 May 4. J Pharmacol Exp Ther. 2023. PMID: 37142443
Structural basis for CCR6 modulation by allosteric antagonists.
Wasilko DJ, Gerstenberger BS, Farley KA, Li W, Alley J, Schnute ME, Unwalla RJ, Victorino J, Crouse KK, Ding R, Sahasrabudhe PV, Vincent F, Frisbie RK, Dermenci A, Flick A, Choi C, Chinigo G, Mousseau JJ, Trujillo JI, Nuhant P, Mondal P, Lombardo V, Lamb D, Hogan BJ, Minhas GS, Segala E, Oswald C, Windsor IW, Han S, Rappas M, Cooke RM, Calabrese MF, Berstein G, Thorarensen A, Wu H. Wasilko DJ, et al. Among authors: berstein g. Nat Commun. 2024 Aug 31;15(1):7574. doi: 10.1038/s41467-024-52045-7. Nat Commun. 2024. PMID: 39217154 Free PMC article.
A phase I, randomized, double-blind study to assess the safety, tolerability and efficacy of the topical RORC2 inverse agonist PF-06763809 in participants with mild-to-moderate plaque psoriasis.
Berstein G, Zhang Y, Berger Z, Kieras E, Li G, Samuel A, Yeoh T, Dowty H, Beaumont K, Wigger-Alberti W, von Mackensen Y, Kroencke U, Hamscho R, Garcet S, Krueger JG, Banfield C, Oemar B. Berstein G, et al. Clin Exp Dermatol. 2021 Jan;46(1):122-129. doi: 10.1111/ced.14412. Epub 2020 Sep 14. Clin Exp Dermatol. 2021. PMID: 32767679 Free PMC article. Clinical Trial.
RORγt inhibition ameliorates IL-23 driven experimental psoriatic arthritis by predominantly modulating γδ-T cells.
Mortier C, Gracey E, Coudenys J, Manuello T, Decruy T, Maelegheer M, Stappers F, Gilis E, Gaublomme D, Van Hoorebeke L, Van Welden S, Ambler C, Hegen M, Symanowicz P, Steyn S, Berstein G, Elewaut D, Venken K. Mortier C, et al. Among authors: berstein g. Rheumatology (Oxford). 2023 Sep 1;62(9):3169-3178. doi: 10.1093/rheumatology/kead022. Rheumatology (Oxford). 2023. PMID: 36661300
Reduction of Inflammatory and Cardiovascular Proteins in the Blood of Patients with Psoriasis: Differential Responses between Tofacitinib and Etanercept after 4 Weeks of Treatment.
Kim J, Tomalin L, Lee J, Fitz LJ, Berstein G, Correa-da Rosa J, Garcet S, Lowes MA, Valdez H, Wolk R, Suarez-Farinas M, Krueger JG. Kim J, et al. Among authors: berstein g. J Invest Dermatol. 2018 Feb;138(2):273-281. doi: 10.1016/j.jid.2017.08.040. Epub 2017 Sep 18. J Invest Dermatol. 2018. PMID: 28927890 Free article. Clinical Trial.
29 results