PUBLICATIONS

OUR PUBLICATIONS.


Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Johnstone S; Albert JS. Bioorg. Med. Chem. Lett. 2017, 2239; Link.

Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.  Varnes JG; Geschwindner S; Holmquist CR; Forst J; Wang X; Dekker N; Scott CW; Tian G; Wood MW; Albert JS. Bioorg. Med. Chem. Lett. 2016; 197.  Link

Bromodomain inhibitors regulate the C9ORF72 locus in ALS.  Zeier Z; Esanov R; Belle KC; Volmar C-H; Johnstone AL; Halley P; DeRosa BA; Khoury N; van Blitterswijk M; Rademakers R; Albert J; Brothers SP; Wuu J; Dykxhoorn DM; Benatar M; Wahlestedt C. Exp. Neurol. 2015; 241. Link

Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists.  Laliberte S; Vallee F; Fournier P-A; Bedard L; Labrecque J; Albert JS. Bioorg. Med. Chem. Lett. 2014; 3204. Link

Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists. Hu, YJ; St.-Onge, M; Laliberte, S; Vallee, F, Jin, S; Bedard, L; Labrecque, J; Albert, JS. Biorg. Med. Chem. Lett., 2014, 24, 3199. Link

Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists. Laliberte, S; Vallee, F; Fournier, PA; Bedard, L; Labrecque, J; Albert, JS. Biorg. Med. Chem. Lett., 2014, 24, 3204. Link

Development of a Plate-Based Optical Biosensor Fragment Screening Methodology to Identify Phosphodiesterase 10A Inhibitors. Geschwindner S, Dekker N, Horsefield R, Tigerstrom A, Johansson P, Scott CW, Albert JS, J. Med. Chem., 2013. Link

Multiple Roles of Transient Receptor Potential (TRP) Channels in Inflammatory Conditions and Current Status of Drug Development, Radresa, O,Paré, M, Albert, JS, 2013, Current Topics in Med. Chem., 2013. Link

Targets and Emerging Therapies for Schizophrenia; 2012, Wiley Publications, Editors: Albert, JS, Wood, MW.Link

Progress in the Exploration and Development of GlyT1 Inhibitors for Schizophrenia; Albert, JS, Wood, MW.;2012. Link

Isoquinucline-based GlyT1 inhibitors for schizophrenia: Discovery, optimization, synthesis, and in vivo pharmacology, Albert, JS; ACS National Symposium, 2012.

Potent and orally efficacious benzothiazole amides as TRPV1 antagonists. Brown, W, Johnstone, S, Jones, P, Walpole, C, Griffin, AW, et al. BMCL, 2012, 22, 6205. Link

N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration. Zhongyong W; Tremblay, M; Johnstone, S; Tomaszewski, M; Brown, W; Walpole, C; Page, D; et al. BMCL, 2012, 22, 3884. Link

Fragment-based lead discovery; Albert, JS, 2010, Wiley Publications.Link

Discovery of new high-affinity PDE10 inhibitors using fragment based lead generation and knowledge-based design, Albert, JS; ACS National Symposium, 2012

Identification of high-affinity β-secretase inhibitors using fragment-based lead generation; Albert, JS, Edwards, PD, 2008.Link

An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca’s drug discovery programmes, Albert, JS; Blomberg, N., et al.Link

Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta -secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.Edwards, PD; Albert, JS; et al.J. Med. Chem. 2007, 50, 5912-5925. Link

Neurokinin-3 receptor antagonists in schizophrenia, Albert, JS, Potts, W., Expert Opin.Ther. Pat. 2006, 16, 925-937. Link

OUR BOOKS.


 Progress in the exploration and development of GlyT1 inhibitors for schizophrenia. Albert JS; Wood MW. John Wiley & Sons, Inc.; 2012. Link

OUR PATENTS.


Preparation of substituted imidazopyridines as bromodomain inhibitors. Pourashraf, Mehrnaz; Beaulieu, Marc-Andre; Claridge, Stephen; Bayrakdarian, Malken; Johnstone, Shawn; Albert, Jeffrey S.; Griffin, Andrew; 2017. WO2017066876

Substituted benzimidazoles as bromodomain inhibitors, their preparation and their use as pharmaceuticals. Pourashraf M; Jacquemot G; Claridge S; Bayrakdarian M; Johnstone S; Albert JS; Griffin A; 2017.  WO2017024412

N-Substituted bicyclic lactams as bromodomain inhibitors, their preparation and their use as pharmaceuticals. Jacquemot G; Claridge S; Bayrakdarian M; Johnstone S; Albert JS; Griffin A; 2017. WO2017024406

Preparation of aryl-substituted dihydroquinolinones as bromodomain inhibitors. Jacquemot G; Bayrakdarian M; Johnstone S; Albert JS; Griffin A; 2017.  WO2017024408

Preparation of oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors. Albert JS; Johnstone S; Jones P; 2014.  WO2014152029

RECENT PRESENTATIONS.


 Progress in strategies to optimize allosteric modulators. Johnstone S. Cambridge Healthtech Symposium, San Diego 2017.

 Identification of inhibitors of HIF2a as modulators of the hypoxia response for the treatment of cancer. Johnstone S; Masek B; Wang L; Brothers S; Bourgault S; Grazinni E; Coupal M. ACS National Meeting 2016.

Development of highly potent, selective BET bromodomain inhibitors that are CNS penetrant and effective in rodent models of brain cancer. Bayrakdarian M; Johnstone A; Penas C; Stathias V; Brothers S; Ayad N; Wahlestedt C. ACS National Meeting 2016.