Specializations
Biochemistry
Molecular and Cellular Biology
Pharmacology
Pathology
Biotechnology and Pharmaceutical Industries
Translational and Entrepreneurial Science
Pharmaceutical and Biotechnology Consulting
Recent Publications
Gerai S., P.C. Shaffer, R.B. Laprairie, D.R. Janero, R.G. Pertwee, A. Straiker and G.A. Thakur. 2021. Design, synthesis, and pharmacological profiling of cannabinoid 1 receptor allosteric modulators: preclinical efficacy of C2-group GAT211 congeners for reducing intraocular pressure. Bioorg. Med. Chem doi:10.1016/j.bmc.2021.116421
Gerai S., L.M. Leo, A.M. Szczesniak, D.P. Hurts, P.C. Shaffer, A. Zagzoog, T. Black, J.R. Deschamps, E. Miess, S. Shulz, D.R. Janero, A. Straiker, R.G. Pertwee. M.E. Abood, M.E.M. Kelly, P.H. Reggio, R.B. Laprairie and G.A Thakur. 2021. Discovery of a biased allosteric modulator for cannabinoid 1 receptor: preclinical anti-glaucoma efficacy. J. Med. Chem. 64:8104-8126.
Schaffer, P.C., P.M Kulkarni, D.R. Janero and G.A Thakur. 2020. Focused structure-activity relationship profiling around the 2-phenylindole scaffold of a cannabinoid type-1 receptor agonist-positive allosteric modulator: site-lll aromatic-ring congeners with enhanced activity and solubility. Bioorg. Med. Chem. doi:10.1016/j.bmc.2020.115727.
Gari, S., P. Kulkarni, P. Schaffer, L. Leo, A Brandt, A. Zagzoog. T. Black, X. Lin, D. Hurst, D.R. Janero, M. Abood, A Straiker, R. Pertwee, M. Kelly, A-M. Szczesniak, E. Denovan-Wright, K. Mackie, A. Hohmann, P. Reggio, R.B. Laprairie and G.A Thakur. 2020. Application of fluorine- and nitrogen-walk approaches: Defining the structural and functional diversity of 2-phenylindole class of CB1-receptor positive allosteric modulators. J. Med. Chem. 63:542:568.
Szymanski, D., M. Papanastasiou, L. Pandarinathan, N. Zvonok, D.R. Janero, S. Pavlopoulos, P. Vouros and A. Makriyannis. 2018. Aliphatic azides as selective cysteine labeling reagents for integral membrane proteins. J. Med. Chem. 61:11199- 11208.
Karageorgos, I., V.I. Silin, N. Zvonok, J. Marino, D.R. Janero and A. Makriyannis. 2017. The role of human monoacylglycerol lipase (hMAGL) binding pocket in breakup of unsaturated phospholipid membranes. Anal. Biochem. 536:90-95.
Zhou, H., Y. Peng, A. Halikhedkar, P. Fan., D.R. Janero, G.A. Thakur, R.W. Mercier, X. Sun, X. Ma and A. Makriyannis. 2017. Human cannabinoid receptor 2 ligandinteraction motif: transmembrane helix 2 cysteine C2.59(89) as determinant of classical cannabinoid agonist activity and binding pose. ACS Chem. Neurosci. 8:1338-1347.
Laprairie, R., P.M. Kulkarni, J.R. Deschamps, M.E.M. Kelley, D.R. Janero, M.G. Cascio. L.A. Stevenson, R.G. Pertwee, T.P Kenakin, E.M. Denovan-Wright and G.A. Thakur. 2017. Enantiospecific allosteric modulation of cannabinoid 1 receptor. ACS Chem. Neurosci. 8:1188-1023.
