Ett urval av artiklar publicerade av ledningen av AlzeCure Pharma.
NeuroRestore
Neurotrophin targeted therapeutics – a gateway to cognition and more? Dr. Gunnar Nordvall, Head of Chemistry, Dr. Pontus Forsell, Head of Research and Discovery and Dr. Johan Sandin, CSO, Aug 16, 2022
Characterization of positive allosteric modulators of TrkB for the treatment of depression Sandin, J., Nordvall, G., Madjid, N., Dahlström, M., Parrado, C., Backlund, M., Lidell, V., Halldin, M. and Forsell, P., ECNP 2021, October 2-5.
ACD856, a novel cognitive enhancer targeting neurotrophin signaling for the treatment of Alzheimer’s Disease Forsell, P., Halldin, M., Dahlström, M., Madjid, N., Rother, M., Van Es-Johansson, A., Lundkvist, J., Eriksdotter, M., Jönsson, M., Winblad, B. and Sandin, J., CTAD 2020, Nov 4-7.
Identification of Novel Positive Allosteric Modulators of Neurotrophin Receptors for the Treatment of Cognitive Dysfunction
Märta Dahlström; Nather Madjid; Gunnar Nordvall; Magnus M. Halldin; Erika Vazquez-Juarez; Maria Lindskog; Johan Sandin; Bengt Winblad; Maria Eriksdotter; Pontus Forsell Cells 2021, Volume 10, Issue 8, 1871
ACD856, a positive modulator of neurotrophin signaling reverses scopolamine- or age-induced cognitive deficits
Pontus Forsell, Gunnar Nordvall, Nather Madjid, Märta Dahlström, Magnus Halldin, Johan Lundkvist, Bengt Winblad, Prof Maria Eriksdotter, Prof Johan Sandin, Martin Jönsson., 2020 April 2-5; AAT-ADPD.
ACD856 – a novel positive allosteric modulator of Trk-receptors in clinical development for the treatment of Alzheimer’s disease
Nordvall, G., Madjid, N., Backlund, M., Halldin, M., Rother., M., Nilsson, B., Sandin, J.* and Forsell, P., AAIC 2021, July 26-30
Stimulating Neurotrophin Receptors in the Treatment of Neurodegenerative Disorders
Nordvall G & Forsell P. Annual Reports in Medicinal Chemistry, 2014;49:59–73.
The Use of TrkA-PathHunter Assay in High-Throughput Screening to Identify Compounds That Affect Nerve Growth Factor Signaling
Forsell P, Almqvist H, Hillertz P, Akerud T, Otrocka M, Eisele L, Sun K, Andersson H, Trivedi S, Wollberg AR, Dekker N, Rottici D & Sandberg K. J. Biomol. Screen., 2013 Jul;18(6):659-69.
Cholinesterase inhibitors improve both memory and complex learning in aged beagle dogs
Araujo JA, Greig NH, Ingram DK, Sandin J, de Rivera C & Milgram NW. J. Alzheimers Dis., 2011;26(1):143-55.
Characterization of positive allosteric modulators of TrkB for the treatment of depression; Scientific presentation at ECNP
Sandin, J., Nordvall, G., Madjid, N., Dahlström, M., Parrado, C., Backlund, M., Lidell, V., Halldin, M. and Forsell, P., 2021 October 2-5.
Alzstatin
γ-Secretase modulators show selectivity for γ-secretase–mediated amyloid precursor protein intramembrane processing Tobias A. Weber, Johan Lundkvist, Johanna Wanngren, Hlin Kvartsberg, ShaoBo Jin, Pia Larssen, Dan Wu, Daniel V. Oliveira, Karolina Minta, Gunnar Brinkmalm, Henrik Zetterberg, Kaj Blennow, Gunnar Nordvall, Bengt Winblad, Erik Portelius, Helena Karlström., Journal of Cellular and Molecular Medicine, 20 December 2021
Gamma-secretase modulators show selectivity for gamma-secretase mediated Ab production
Lundkvist, J., Weber, TA., Wanngren, J., Kvartsberg, H., Larssen, P., Wu, D., Oliviera, DW., Sandin, J, Zetterberg, H., Blennow, K., Nordvall, G., Winblad, B., Portelius E. and Karlström H., CTAD 2020, CTAD 2020, Nov 4-7.
γ-Secretase: An Unusual Enzyme with Many Possible Disease Targets, Including Alzheimer’s Disease
Lundkvist J. Lendahl U.
(2011), Book chapter 12 in Aspartic Acid Proteases as Therapeutic Targets: 45 (Methods and Principles in Medicinal Chemistry) eds R. Mannhold, H. Kubinyi, G. Folkers and A.K. Ghosh,
Second generation γ-secretase modulators exhibit different modulation of Notch β and Aβ production
Wanngren J, Ottervald J, Parpal S, Portelius E, Strömberg K, Borgegård T, Klintenberg R, Juréus A, Blomqvist J, Blennow K, Zetterberg H, Lundkvist J, Rosqvist S, Karlström H. J. Biol. Chem., 2012 Sep 21;287(39):32640-50.
Characterization of intermediate steps in Abeta production under near-native conditions
Olsson F, Schmidt S, Althoff V, Munter M, Jin S, Rosqvist S, Lendahl U, Multhaup G & Lundkvist J. The Journal of Biological Chemistry, 2014;289(3):1540-50.
First and second generation gamma-secretase modulators (GSMs) modulate Abeta production through different mechanisms.
Borgegard T, Jureus A, Olsson F, Rosqvist S, Sabirsh A, Rotticci D, Paulsen K, Klintenberg R, Yan H, Waldman M, Stromberg K, Nord J, Johansson J, Regner A, Parpal S, Malinowsky D, Radesater AC, Li T, Singh R, Eriksson H, Lundkvist J. J. Biol. Chem., 2012 Apr 6;287(15):11810-9.
Has inhibition of Aβ production adequately been tested as therapeutic approach in mild AD? A model-based meta-analysis of γ-secretase inhibitor data
Niva C, Parkinson J, Olsson F, van Schaick E, Lundkvist J, Visser SA. Eur. J. Clin. Pharmacol., 2013 Jun;69(6):1247-60.
Alzheimer’s disease: Presenilin 2-sparing γ-secretase inhibition is a tolerable Abeta peptide lowering strategy
Borgegård T, Gustavsson S, Nilsson C, Parpal S, Klintenberg R, Berg A-L, Rosqvist S, Serneels L, Svensson S, Olsson F, Jin S, Yan H, Johanna Wanngren J, Jureus A, Ridderstad-Wollberg A, Wollberg P, Stockling K, Karlström H, Malmberg Å, Lund J, Arvidsson PI, De Strooper B, Lendahl U & Lundkvist J. J. Neurosc., 2012 Nov 28;32(48):17297-305.
Decreased axonal transport rates in the TG2576 APP transgenic mouse: improvement with the gamma-secretase inhibitor MRK-560 as detected by manganese-enhanced MRI
Wang FH, Appelkvist P, Klason T, Gissberg O, Bogstedt A, Eliason K, Martinsson S, Briem S, Andersson A, Visser SAG, Ivarsson M, Lindberg M, Agerman K & Sandin J. Eur. J. Neurosci., 2012;36(9):3165-72.
Sulfonimidamides as Sulfonamides Bioisosteres: Rational Evaluation through Synthetic, in Vitro, and in Vivo Studies with γ-Secretase Inhibitors
Sehgelmeble F, Janson J, Ray C, Rosqvist S, Gustavsson S, Nilsson LI, Minidis A, Holenz J, Rotticci D, Lundkvist J & Arvidsson PI. ChemMedChem., 2012 Mar 5;7(3):396-9.
Changed membrane integration and catalytic site conformation are two mechanisms behind the increased Aβ42/Aβ40 ratio by presenilin 1 familial Alzheimer-linked mutations
Wanngren J, Lara P, Ojemalm K, Maioli S, Moradi N, Chen L, Tjernberg LO, Lundkvist J, Nilsson I & Karlström H. FEBS Open Bio., 2014 Apr 24;4:393-406.
In vivo analysis using a presenilin1-specific inhibitor: presenlin1-containing γ-secretase complexes mediate the majority of CNS Aβ production in the mouse
Borgegård T, Minidis A, Jureus A, Malmborg J, Rosqvist S, Gruber S,Almqvist H, Yan H, Bogstedt A, Olsson F, Dahlström J, Ray C, Närhi K, Malinowsky D, Hagström E, Jin S, Malmberg Å, Lendahl U and Lundkvist J. Alzheimer’s Disease Research Journal. 2011, 3(1): 29-45.
Painless
Developing a Nobel Prize winning target in pain Segerdahl M, Jönsson M, Sandin J. MedNous 2021, 15(10):8-9.
Negative allosteric modulators of TrkA for the treatment of pain; Scientific presentation at IASP Nordvall, G., Dahlström, M., Parrado, C., Backlund, M., Lidell, V., Halldin, M., Sandin, J. and Forsell, P., 2021 June 27-July 1.
ACD440 – A Novel TRPV1 Antagonist for the Topical Treatment of Pain; Scientific presentation at IASP
Schaffler, K., Popescu, T., Hellgren, M., Schipper, N., Gripenhall, A., Sandin, J., Forsell, P., Segerdahl, M. and Rother, M., 2021 June 27-July 1.
Drug discovery & development
Neuronal cell-based high-throughput screen for enhancers of mitochondrial function reveals luteolin as a modulator of mitochondria-endoplasmic reticulum coupling
Naia L, Pinho CM, Dentoni G, Liu J, Leal NS, Ferreira DMS, Schreiner B, Filadi R, Fão L, Connolly NMC, Forsell P, Nordvall G, Shimozawa M, Greotti E, Basso E, Theurey P, Gioran A, Joselin A, Arsenian-Henriksson M, Nilsson P, Rego AC, Ruas JL, Park D, Bano D, Pizzo P, Prehn JHM, Ankarcrona M. BMC Biol. 2021 Mar 24;19(1):57.
The battle of Alzheimer’s Disease – the beginning of the future Unleashing the potential of academic discoveries
Lundkvist J, Halldin MM, Sandin J, Nordvall G, Forsell P, Svensson S, Jansson L, Johansson G, Winblad B & Ekstrand J. Frontiers in Pharmacology, 2014;5:102.
Revisiting the peripheral sink hypothesis: Inhibiting BACE1 activity in the periphery does not alter β-amyloid levels in the CNS
Georgievska B, Gustavsson S, Lundkvist J, Neelissen J, Eketjäll S, Ramberg V, Bueters T, Agerman K, Juréus A, Svensson S, Berg S, Fälting J & Lendahl U. J. Neurochem., 2015;132:477-86.
Creation of Novel Cores for β-Secretase (BACE-1) Inhibitors: A Multi-Parameter Lead Generation Strategy
Viklund J, Kolmodin K, Nordvall G, Swahn B-M, Svensson M, Gravenfors Y & Rahm F. ACS Medicinal Chemistry Letters, 2014;5(4):440-5.
BACE1 Inhibition Induces a Specific Cerebrospinal Fluid β-Amyloid Pattern That Identifies Drug Effects in the Central Nervous System
Mattsson N, Rajendran L, Zetterberg H, Gustavsson M, Andreasson U, Olsson M, Brinkmalm G, Lundkvist J, Jacobson LH, Perrot L, Neumann U, Borghys H, Mercken M, Dhuyvetter D, Jeppsson F, Blennow K & Portelius E. Plos One, 2012;7(2):e31084.
Endogenous APP accumulates in synapses after BACE1 inhibition
Nigam SM, Xu S, Ackermann F, Gregory JA, Lundkvist J, Lendahl U & Brodin L. Neurosci. Res., 2016 Aug;109:9-15.
Pragmatic Approaches to Determine the Exposures of Drug Metabolites in Preclinical and Clinical Subjects in the MIST Evaluation
Haglund J, Halldin MM, Brunnström Å, Eklund G, Kautiainen A, Sandholm A & Iverson SL. Chem. Res. Toxicol., 2014;27(4):601-10.
Assessment of free drug concentration in cyclodextrin formulations is essential to determine drug potency in functional in vitro assays
Sjögren E, Andersson S, Sundgren-Andersson AK, Halldin MM & Stålberg O. J. Pharm. Sci., 2016;105:2913-20.
Preclinical characterization of three transient receptor potential vanilloid receptor 1 antagonists for early use in human intradermal microdose analgesic studies
Sjögren E, Halldin MM, Stålberg O & Sundgren-Andersson AK. European Journal of Pain, 2018;22(5):889-903.
Clinical testing of three novel transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonists in a pharmacodynamic intradermal capsaicin model
Sjögren E, Kullenberg T, Jonzon B, Segerdahl M, Stålberg O, Halldin MM & Sundgren-Andersson AK. European Journal of Pain, 2018;22(7):1214-28.
AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans
Georgievska B, Sandin J, Doherty J, Mörtberg A, Neelissen J, Andersson A, Gruber S, Nilsson Y, Schött P, Arvidsson PI, Hellberg S, Osswald G, Berg S, Fälting J & Bhat RV. J. Neurochem., 2013 May;125(3):446-56.