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Discovery of Conformationally Constrained ALK2 Inhibitors.
González-Álvarez H, Ensan D, Xin T, Wong JF, Zepeda-Velázquez CA, Cros J, Sweeney MN, Hoffer L, Kiyota T, Wilson BJ, Aman A, Roberts O, Isaac MB, Bullock AN, Smil D, Al-Awar R. González-Álvarez H, et al. Among authors: bullock an. J Med Chem. 2024 Mar 28;67(6):4707-4725. doi: 10.1021/acs.jmedchem.3c02308. Epub 2024 Mar 18. J Med Chem. 2024. PMID: 38498998 Free PMC article.
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.
Ensan D, Smil D, Zepeda-Velázquez CA, Panagopoulos D, Wong JF, Williams EP, Adamson R, Bullock AN, Kiyota T, Aman A, Roberts OG, Edwards AM, O'Meara JA, Isaac MB, Al-Awar R. Ensan D, et al. Among authors: bullock an. J Med Chem. 2020 May 14;63(9):4978-4996. doi: 10.1021/acs.jmedchem.0c00395. Epub 2020 May 5. J Med Chem. 2020. PMID: 32369358 Free PMC article.
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.
Smil D, Wong JF, Williams EP, Adamson RJ, Howarth A, McLeod DA, Mamai A, Kim S, Wilson BJ, Kiyota T, Aman A, Owen J, Poda G, Horiuchi KY, Kuznetsova E, Ma H, Hamblin JN, Cramp S, Roberts OG, Edwards AM, Uehling D, Al-Awar R, Bullock AN, O'Meara JA, Isaac MB. Smil D, et al. Among authors: bullock an. J Med Chem. 2020 Sep 10;63(17):10061-10085. doi: 10.1021/acs.jmedchem.0c01199. Epub 2020 Aug 26. J Med Chem. 2020. PMID: 32787083 Free article.
Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept.
Hudson L, Mui J, Vázquez S, Carvalho DM, Williams E, Jones C, Bullock AN, Hoelder S. Hudson L, et al. Among authors: bullock an. J Med Chem. 2018 Aug 23;61(16):7261-7272. doi: 10.1021/acs.jmedchem.8b00782. Epub 2018 Aug 7. J Med Chem. 2018. PMID: 30085668 Free PMC article.
Mutant ACVR1 Arrests Glial Cell Differentiation to Drive Tumorigenesis in Pediatric Gliomas.
Fortin J, Tian R, Zarrabi I, Hill G, Williams E, Sanchez-Duffhues G, Thorikay M, Ramachandran P, Siddaway R, Wong JF, Wu A, Apuzzo LN, Haight J, You-Ten A, Snow BE, Wakeham A, Goldhamer DJ, Schramek D, Bullock AN, Dijke PT, Hawkins C, Mak TW. Fortin J, et al. Among authors: bullock an. Cancer Cell. 2020 Mar 16;37(3):308-323.e12. doi: 10.1016/j.ccell.2020.02.002. Epub 2020 Mar 5. Cancer Cell. 2020. PMID: 32142668 Free PMC article.
Receptor-interacting protein kinase 2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold.
Suebsuwong C, Dai B, Pinkas DM, Duddupudi AL, Li L, Bufton JC, Schlicher L, Gyrd-Hansen M, Hu M, Bullock AN, Degterev A, Cuny GD. Suebsuwong C, et al. Among authors: bullock an. Eur J Med Chem. 2020 Aug 15;200:112417. doi: 10.1016/j.ejmech.2020.112417. Epub 2020 May 15. Eur J Med Chem. 2020. PMID: 32505849 Free PMC article.
2-Amino-2,3-dihydro-1H-indene-5-carboxamide-Based Discoidin Domain Receptor 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Antipancreatic Cancer Efficacy.
Zhu D, Huang H, Pinkas DM, Luo J, Ganguly D, Fox AE, Arner E, Xiang Q, Tu ZC, Bullock AN, Brekken RA, Ding K, Lu X. Zhu D, et al. Among authors: bullock an. J Med Chem. 2019 Aug 22;62(16):7431-7444. doi: 10.1021/acs.jmedchem.9b00365. Epub 2019 Aug 2. J Med Chem. 2019. PMID: 31310125 Free PMC article.
110 results