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Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors.
Hopkins BT, Bame E, Bell N, Bohnert T, Bowden-Verhoek JK, Bui M, Cancilla MT, Conlon P, Cullen P, Erlanson DA, Fan J, Fuchs-Knotts T, Hansen S, Heumann S, Jenkins TJ, Gua C, Liu Y, Liu Y, Lulla M, Marcotte D, Marx I, McDowell B, Mertsching E, Negrou E, Romanowski MJ, Scott D, Silvian L, Yang W, Zhong M. Hopkins BT, et al. Bioorg Med Chem. 2021 Aug 15;44:116275. doi: 10.1016/j.bmc.2021.116275. Epub 2021 Jun 15. Bioorg Med Chem. 2021. PMID: 34314938
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model.
Vandeveer GH, Arduini RM, Baker DP, Barry K, Bohnert T, Bowden-Verhoek JK, Conlon P, Cullen PF, Guan B, Jenkins TJ, Liao SY, Lin L, Liu YT, Marcotte D, Mertsching E, Metrick CM, Negrou E, Powell N, Scott D, Silvian LF, Hopkins BT. Vandeveer GH, et al. Among authors: liu yt. Bioorg Med Chem Lett. 2023 Jan 15;80:129108. doi: 10.1016/j.bmcl.2022.129108. Epub 2022 Dec 17. Bioorg Med Chem Lett. 2023. PMID: 36538993
Randomized phase I clinical trial of anti-α-synuclein antibody BIIB054.
Brys M, Fanning L, Hung S, Ellenbogen A, Penner N, Yang M, Welch M, Koenig E, David E, Fox T, Makh S, Aldred J, Goodman I, Pepinsky B, Liu Y, Graham D, Weihofen A, Cedarbaum JM. Brys M, et al. Mov Disord. 2019 Aug;34(8):1154-1163. doi: 10.1002/mds.27738. Epub 2019 Jun 17. Mov Disord. 2019. PMID: 31211448 Free PMC article. Clinical Trial.
Development of an aggregate-selective, human-derived α-synuclein antibody BIIB054 that ameliorates disease phenotypes in Parkinson's disease models.
Weihofen A, Liu Y, Arndt JW, Huy C, Quan C, Smith BA, Baeriswyl JL, Cavegn N, Senn L, Su L, Marsh G, Auluck PK, Montrasio F, Nitsch RM, Hirst WD, Cedarbaum JM, Pepinsky RB, Grimm J, Weinreb PH. Weihofen A, et al. Neurobiol Dis. 2019 Apr;124:276-288. doi: 10.1016/j.nbd.2018.10.016. Epub 2018 Oct 28. Neurobiol Dis. 2019. PMID: 30381260 Free article.
The Parkinson's disease-associated gene ITPKB protects against α-synuclein aggregation by regulating ER-to-mitochondria calcium release.
Apicco DJ, Shlevkov E, Nezich CL, Tran DT, Guilmette E, Nicholatos JW, Bantle CM, Chen Y, Glajch KE, Abraham NA, Dang LT, Kaynor GC, Tsai EA, Nguyen KH, Groot J, Liu Y, Weihofen A, Hurt JA, Runz H, Hirst WD. Apicco DJ, et al. Proc Natl Acad Sci U S A. 2021 Jan 5;118(1):e2006476118. doi: 10.1073/pnas.2006476118. Proc Natl Acad Sci U S A. 2021. PMID: 33443159 Free PMC article.
1,328 results