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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: goldberg ja. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152).
O'Neill DJ, Adedoyin A, Bray JA, Deecher DC, Fensome A, Goldberg JA, Harrison J, Leventhal L, Mann C, Mark L, Nogle L, Sullivan NR, Spangler TB, Terefenko EA, Trybulski EJ, Uveges AJ, Vu A, Whiteside GT, Zhang P. O'Neill DJ, et al. Among authors: goldberg ja. J Med Chem. 2011 Oct 13;54(19):6824-31. doi: 10.1021/jm200733r. Epub 2011 Sep 14. J Med Chem. 2011. PMID: 21916421
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
Zhou J, Bhattacharjee A, Chen S, Chen Y, Duffy E, Farmer J, Goldberg J, Hanselmann R, Ippolito JA, Lou R, Orbin A, Oyelere A, Salvino J, Springer D, Tran J, Wang D, Wu Y, Johnson G. Zhou J, et al. Among authors: goldberg j. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6175-8. doi: 10.1016/j.bmcl.2008.10.011. Epub 2008 Oct 7. Bioorg Med Chem Lett. 2008. PMID: 18947996
Design at the atomic level: generation of novel hybrid biaryloxazolidinones as promising new antibiotics.
Zhou J, Bhattacharjee A, Chen S, Chen Y, Duffy E, Farmer J, Goldberg J, Hanselmann R, Ippolito JA, Lou R, Orbin A, Oyelere A, Salvino J, Springer D, Tran J, Wang D, Wu Y, Johnson G. Zhou J, et al. Among authors: goldberg j. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6179-83. doi: 10.1016/j.bmcl.2008.10.014. Epub 2008 Oct 7. Bioorg Med Chem Lett. 2008. PMID: 18951792
A γ-Lactam Siderophore Antibiotic Effective against Multidrug-Resistant Gram-Negative Bacilli.
Goldberg JA, Nguyen H, Kumar V, Spencer EJ, Hoyer D, Marshall EK, Cmolik A, O'Shea M, Marshall SH, Hujer AM, Hujer KM, Rudin SD, Domitrovic TN, Bethel CR, Papp-Wallace KM, Logan LK, Perez F, Jacobs MR, van Duin D, Kreiswirth BM, Bonomo RA, Plummer MS, van den Akker F. Goldberg JA, et al. J Med Chem. 2020 Jun 11;63(11):5990-6002. doi: 10.1021/acs.jmedchem.0c00255. Epub 2020 Jun 2. J Med Chem. 2020. PMID: 32420736 Free PMC article.
A γ-lactam siderophore antibiotic effective against multidrug-resistant Pseudomonas aeruginosa, Klebsiella pneumoniae, and Acinetobacter spp.
Goldberg JA, Kumar V, Spencer EJ, Hoyer D, Marshall SH, Hujer AM, Hujer KM, Bethel CR, Papp-Wallace KM, Perez F, Jacobs MR, van Duin D, Kreiswirth BN, van den Akker F, Plummer MS, Bonomo RA. Goldberg JA, et al. Eur J Med Chem. 2021 Aug 5;220:113436. doi: 10.1016/j.ejmech.2021.113436. Epub 2021 Apr 8. Eur J Med Chem. 2021. PMID: 33933754
Acetylcholine waves and dopamine release in the striatum.
Matityahu L, Gilin N, Sarpong GA, Atamna Y, Tiroshi L, Tritsch NX, Wickens JR, Goldberg JA. Matityahu L, et al. Among authors: goldberg ja. Nat Commun. 2023 Oct 27;14(1):6852. doi: 10.1038/s41467-023-42311-5. Nat Commun. 2023. PMID: 37891198 Free PMC article.
132 results