2022
Meier-Stephenson FS, Meier-Stephenson VC, Carter MD, Meek AR, Wang Y, Pan L, Chen Q, Jacobo S, Wu F, Lu E, Simms GA, Fisher L, McGrath AJ, Fermo V, Barden CJ, Clair HDS, Galloway TN, Yadav A, Campágna-Slater V, Hadden M, Reed M, Taylor M, Kelly B, Diez-Cecilia E, Kolaj I, Santos C, Liyanage I, Sweeting B, Stafford P, Boudreau R, Reid GA, Noyce RS, Stevens L, Staniszewski A, Zhang H, Murty MRVS, Lemaire P, Chardonnet S, Richardson CD, Gabelica V, DePauw E, Brown R, Darvesh S, Arancio O, Weaver DF. Alzheimer's disease as an autoimmune disorder of innate immunity endogenously modulated by tryptophan metabolites. Alzheimers Dement (N Y). 2022 Apr 6;8(1):e12283. doi: 10.1002/trc2.12283. PMID: 35415204; PMCID: PMC8985489.
Alzheimer’s: The ABCDE Paradigm
Gupta M, Weaver DF. Alzheimer's: The ABCDE Paradigm. ACS Chem Neurosci. 2022 May 4;13(9):1355-1357. doi: 10.1021/acschemneuro.2c00195. Epub 2022 Apr 15. PMID: 35427106.
2021
A Series of 2-((1-Phenyl-1H-imidazol-5-yl)methyl)-1H-indoles as Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors
Zheng Y, Stafford PM, Stover KR, Mohan DC, Gupta M, Keke EC, Schiavini P, Villar L, Wu F, Kreft A, Thomas K, Raaphorst E, Pasangulapati JP, Alla SR, Sharma S, Mittapalli RR, Sagamanova I, Johnson SL, Reed MA, Weaver DF. A Series of 2-((1-Phenyl-1H-imidazol-5-yl)methyl)-1H-indoles as Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors. ChemMedChem. 2021 Mar 23. doi: 10.1002/cmdc.202100107. Epub ahead of print. PMID: 33759400.
Design, synthesis, and biological evaluation of furosemide analogs as therapeutics for the proteopathy and immunopathy of Alzheimer's disease
Wang Z, Wang Y, Pasangulapati JP, Stover KR, Liu X, Schier SW, Weaver DF. Design, synthesis, and biological evaluation of furosemide analogs as therapeutics for the proteopathy and immunopathy of Alzheimer's disease. Eur J Med Chem. 2021 Jun 2;222:113565. doi: 10.1016/j.ejmech.2021.113565. Epub ahead of print. PMID: 34118718.
Mild Microglial Responses in the Cortex and Perivascular Macrophage Infiltration in Subcortical White Matter in Dogs with Age-Related Dementia Modelling Prodromal Alzheimer's Disease
Thomsen BB, Madsen C, Krohn KT, Thygesen C, Schütt T, Metaxas A, Darvesh S, Agerholm JS, Wirenfeldt M, Berendt M, Finsen B. Mild Microglial Responses in the Cortex and Perivascular Macrophage Infiltration in Subcortical White Matter in Dogs with Age-Related Dementia Modelling Prodromal Alzheimer's Disease. J Alzheimers Dis. 2021 May 26. doi: 10.3233/JAD-210040. Epub ahead of print. PMID: 34057083.
Furazans in Medicinal Chemistry
Mancini RS, Barden CJ, Weaver DF, Reed MA. Furazans in Medicinal Chemistry. J Med Chem. 2021 Feb 25;64(4):1786-1815. doi: 10.1021/acs.jmedchem.0c01901. Epub 2021 Feb 11. PMID: 33569941.
Phenothiazines as dual inhibitors of SARS-CoV-2 Mpro and COVID-19 inflammation
Katrina L. Forrestall, Darcy E. Burley, Meghan K. Cash, Ian R. Pottie, and Sultan Darvesh. Phenothiazines as dual inhibitors of SARS-CoV-2 main protease and COVID-19 inflammation. Canadian Journal of Chemistry. e-First. doi:10.1139/cjc-2021-0139.
2020
2-Pyridone natural products as inhibitors of SARS-CoV-2 main protease
Katrina L. Forrestall, Darcy E. Burle , Meghan K. Cash, Ian R. Pottie, Sultan Darvesh. 2-Pyridone Natural Products as Inhibitors of SARS-CoV-2 Main Protease. Chem Biol Interact. 2021 Feb 1;335:109348. doi: 10.1016/j.cbi.2020.109348. Epub 2020 Dec 2. PMID: 33278462 PMCID: PMC7710351
Intact Olfactory Memory in the 5XFAD Mouse Model of Alzheimer’s Disease From 3 to 15 Months of Age
O’Leary TP, Mantolino HM, Stover K, Darvesh S, Brown RE. 2020. Intact olfactory memory in the 5XFAD mouse model of Alzheimer’s disease from 3 to 15 months of age. Behavioural Brain Research. 393: 112731. PMID: 32522622.
Is Inhaled Furosemide a Potential Therapeutic for COVID-19?
Brennecke A, Villar L, Wang Z, Doyle LM, Meek A, Reed M, Barden C, Weaver DF. Is Inhaled Furosemide a Potential Therapeutic for COVID-19? Am J Med Sci. 2020 Sep;360(3):216-221. doi: 10.1016/j.amjms.2020.05.044. Epub 2020 Jun 1. PMID: 32622469.
The Brain Exposure Efficiency (BEE) Score
Gupta M, Bogdanowicz T, Reed MA, Barden CJ, Weaver DF. The Brain Exposure Efficiency (BEE) Score. ACS Chem Neurosci. 2020 Jan 15;11(2):205-224. doi: 10.1021/acschemneuro.9b00650. Epub 2019 Dec 27. PMID: 31815431.
Small Molecule Therapeutics for COVID-19: Repurposing of Inhaled Furosemide
Wang Z, Wang Y, Vilekar P, Yang SP, Gupta M, Oh MI, Meek A, Doyle L, Villar L, Brennecke A, Liyanage I, Reed M, Barden C, Weaver DF. Small molecule therapeutics for COVID-19: repurposing of inhaled furosemide. PeerJ. 2020 Jul 7;8:e9533. doi: 10.7717/peerj.9533. PMID: 32704455; PMCID: PMC7350920.
2019
The Novel Small Molecule TRVA242 Stabilizes Neuromuscular Junction Defects in Multiple Animal Models of Amyotrophic Lateral Sclerosis
Bose P, Tremblay E, Maois C, Narasimhan V, Armstrong GAB, Liao M, Parker JA, Robitaille R, Wen XY, Barden C, Drapeau P. The Novel Small Molecule TRVA242 Stabilizes Neuromuscular Junction Defects in Multiple Animal Models of Amyotrophic Lateral Sclerosis. Neurotherapeutics. 2019 Oct;16(4):1149-1166. doi: 10.1007/s13311-019-00765-w. PMID: 31342410; PMCID: PMC6985319.
Effects of the Novel IDO Inhibitor DWG-1036 on the Behavior of Male and Female 3xTg-AD Mice
Fertan E, Stover KRJ, Brant MG, Stafford PM, Kelly B, Diez-Cecilia E, Wong AA, Weaver DF, Brown RE. Effects of the Novel IDO Inhibitor DWG-1036 on the Behavior of Male and Female 3xTg-AD Mice. Front Pharmacol. 2019 Sep 24;10:1044. doi: 10.3389/fphar.2019.01044. PMID: 31607909; PMCID: PMC6773979.
The Blood–Brain Barrier (BBB) Score
Gupta M, Lee HJ, Barden CJ, Weaver DF. The Blood-Brain Barrier (BBB) Score. J Med Chem. 2019 Nov 14;62(21):9824-9836. doi: 10.1021/acs.jmedchem.9b01220. Epub 2019 Oct 25. PMID: 31603678.
Chapter Eleven - Misfolded Proteins as a Therapeutic Target in Alzheimer's Disease
Liyanage SI, Weaver DF. Misfolded proteins as a therapeutic target in Alzheimer's disease. Adv Protein Chem Struct Biol. 2019;118:371-411. doi: 10.1016/bs.apcsb.2019.08.003. Epub 2019 Sep 21. PMID: 31928732.
2018
Identification of Potent Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors Based on a Phenylimidazole Scaffold
Brant MG, Goodwin-Tindall J, Stover KR, Stafford PM, Wu F, Meek AR, Schiavini P, Wohnig S, Weaver DF. Identification of Potent Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors Based on a Phenylimidazole Scaffold. ACS Med Chem Lett. 2018 Jan 11;9(2):131-136. doi: 10.1021/acsmedchemlett.7b00488. PMID: 29456801; PMCID: PMC5807880.
Phenylpropanoids and Alzheimer's Disease: A Potential Therapeutic Platform
Kolaj I, Imindu Liyanage S, Weaver DF. Phenylpropanoids and Alzheimer's disease: A potential therapeutic platform. Neurochem Int. 2018 Nov;120:99-111. doi: 10.1016/j.neuint.2018.08.001. Epub 2018 Aug 8. PMID: 30098379.
The Hidden Variables Problem in Alzheimer's Disease Clinical Trial Design
Liyanage SI, Santos C, Weaver DF. The hidden variables problem in Alzheimer's disease clinical trial design. Alzheimers Dement (N Y). 2018 Nov 13;4:628-635. doi: 10.1016/j.trci.2018.09.003. PMID: 30519628; PMCID: PMC6260222.
Phenylindanes in Brewed Coffee Inhibit Amyloid-Beta and Tau Aggregation
Mancini RS, Wang Y, Weaver DF. Phenylindanes in Brewed Coffee Inhibit Amyloid-Beta and Tau Aggregation. Front Neurosci. 2018 Oct 12;12:735. doi: 10.3389/fnins.2018.00735. PMID: 30369868; PMCID: PMC6194148.
Tauopathy in the APPswe/PS1ΔE9 Mouse Model of Familial Alzheimer’s Disease
Metaxas A, Thygesen C, Kempf SJ, Anzalone M, Vaitheeswaran R, Petersen S, Landau AM, Audrain H, Teeling JL, Darvesh S, Brooks DJ, Larsen MR, Finsen B. 2018. Tauopathy in the APPswe/PS1ΔE9 mouse model of familial Alzheimer’s disease. bioRxiv. 405647.
In the Alzheimer Waiting Room
Weaver DF. In the Alzheimer waiting room. CMAJ. 2018 Aug 20;190(33):E989-E990. doi: 10.1503/cmaj.180320. PMID: 30998498; PMCID: PMC6102110.