Download BIOGRAPHICAL SKETCH

BIOGRAPHICAL SKETCH
Provide the following information for the key personnel and other significant contributors in the order listed on Form Page 2.
Follow this format for each person. DO NOT EXCEED FOUR PAGES.
NAME
POSITION TITLE
Spyros P. Nikas, Ph.D.
Associate Research Professor
Contact info: e-mail: [email protected]; Lab: (617)373-7620
EDUCATION/TRAINING (Begin with baccalaureate or other initial professional education, such as nursing, and include postdoctoral training.)
INSTITUTION AND LOCATION
Aristotle University, Thessaloniki, Greece.
Aristotle University, Thessaloniki, Greece.
National Hellenic Research Foundation, Athens,
Greece.
University of Connecticut, Storrs, CT, U.S.A
DEGREE
(if applicable)
YEAR(s)
FIELD OF STUDY
Ph.D.
1991
1996
Postdoc.
1998-1999
Medicinal Chemistry
Postdoc.
1999-2003
Medicinal Chemistry
B.S.
Chemistry
Organic Chemistry
A. Personal Statement
With the discovery of two families of endogenous cannabinergic ligands represented by anandamide (AEA)
and 2-arachidonoylglycerol (2-AG), cannabinoid research has taken major strides toward arriving at an
understanding of the molecular mechanism of cannabinoid action. Currently, there are multiple characterized
endocannabinoid proteins [at least two receptors, CB1 and CB2 and two enzymes, fatty acid amide hydrolase
(FAAH) and monoacyl glycerol lipase (MGL)] and a transport system, as potential therapeutic targets for the
development of useful medications in the treatment of a multitude of conditions such as drug addiction, pain,
appetite control, and central nervous system disorders. My primary research goals are directed towards the
rational design and synthesis of potent and selective cannabinergic ligands targeting the endocannabinoid
proteins. Many of these ligands can serve as: (a) molecular probes that provide structural information
regarding the binding sites of the endocannabinoid proteins; (b) pharmacological tools, that can be used in
research aimed at understanding the biochemical, physiological and pathophysiological aspects of the
endocannabinoid system; and (c) cannabinergic drug candidates. I have ongoing work in four areas of
cannabinoid-related synthetic and medicinal chemistry: (a) classical and non-classical cannabinoids; (b)
inhibitors of the endocannabinoid deactivating enzymes; (c) labeled cannabinoids; and (d) endocannabinoid
analogs.
B. Positions and Honors
Positions and Employment
1993-1995
Graduate Teaching Assistant, Department of Chemistry, Aristotle University, Thessaloniki,
Greece.
1996-1998
Chemist (quality control of fuels), Laboratory of Petroleum Distribution Command, NATO’s
installation, Larisa, Greece.
1998-1999
Postdoctoral Fellow, Institute of Organic and Pharmaceutical Chemistry, National Hellenic
Research Foundation, Athens, Greece.
1999-2003
Postdoctoral Fellow, School of Pharmacy, University of Connecticut, Storrs, CT, USA.
2003-2004
Assistant Research Professor, School of Pharmacy, University of Connecticut, Storrs, CT, USA.
2004-2005
Senior Research Scientist, Center for Drug Discovery, Northeastern University, Boston, MA,
USA.
2005-2008
Assistant Research Professor, Center for Drug Discovery, Department of Pharmaceutical
Sciences, Northeastern University, Boston, MA, USA.
2008-2010
(a) Adjunct Professor, Center for Drug Discovery, Northeastern University, Boston, MA, USA; (b)
Researcher, Institute of Organic and Pharmaceutical Chemistry, National Hellenic Research
Foundation, Athens, Greece.
2010-present Associate Research Professor, Center for Drug Discovery, Department of Pharmaceutical
Sciences, Northeastern University, Boston, MA, USA.
Honors
Honor award, Petroleum Distribution Command (number: 105/9-6-1997), Larisa, Greece. Highest honor award,
Petroleum Distribution Command (number: 23/4-2-1998), Larisa, Greece. Nominated for honor award from
Hellenic Air Force (F.900/AD. 1001/9 March 1998), Athens, Greece.
Professional Societies
American Chemical Society.
International Cannabinoid Research Society.
Hellenic Chemical Society.
American Association of University Professors.
C. Selected Peer-reviewed Publications
1. Nikas S. P., Thakur G. A., Makriyannis A. Regiospecifically deuterated (-)-9-tetrahydrocannabivarins. J.
Chem. Soc. Perkin Trans. 1, 2002, 2544-2548.
2. Papahatjis D. P., Nikas S. P., Kourouli T., Chari R., Xu W, Pertwee R. G., Makriyannis A. Pharmacophoric
requirements for the cannabinoid side chain. Probing the cannabinoid receptor subsite at C1΄. J. Med.
Chem. 2003, 46, 3221-3229. PMID: 12852753.
3. Nikas S. P., Grzybovska J., Papahatjis D. P., Charalambous A., Banijamali A. R., Chari R., Fan P., Kourouli
T., Lin S., Nitowski A. J., Marciniak G., Guo Y., Li X., Wang C-L. J., Makriyannis A. The role of halogen
substitution in classical cannabinoids. A CB1 pharmacophore model. AAPS Journal. 2004, 6(4), e30
(http://www.aapsj.org). PMID: 15760095.
4. Tsotinis A., Vlachou M., Calogeropoulou T., Papahatjis D. P., Nikas S. P., Garratt P. J., Piccio V., Vonhoff
S., Davidson K., The M-T., Sugden D. Mapping the Melatonin Receptor. 7. Subtype selective ligands
based on -substituted N-acyl-5-methoxytryptamines and -substituted N-acyl-5-methoxy-1methyltryptamines. J. Med. Chem. 2006, 49, 3509-3519. PMID: 16759094.
5. Nikas S. P., Thakur G. A., Parish D., Alapafuja S. O., Huestis M. A., Makriyannis A. A concise methodology
for the synthesis of (-)-9-tetrahydrocannabinol and (-)-9-tetrahydrocannabivarin metabolites and their
regiospecifically deuterated analogs. Tetrahedron, 2007, 63, 8112-8123.
6. Papahatjis D. P., Nahmias V. R., Nikas S. P., Andreou T., Alapafuja S. O., Tsotinis A., Guo J., Fan P.,
Makriyannis A. C1´-cycloalkyl side chain pharmacophore in tetrahydrocannabinols. J. Med. Chem.,
2007, 50, 4048-4060. PMID: 17672444.
7. Papahatjis D.P., Nahmias V. R., Nikas S. P., Schimpgen M., Makriyannis A. Design and synthesis of (13S)methyl substituted arachidonic acid analogs: Templates for novel endocannabinoids. Chem. Eur. J.,
2010, 16, 4091-4099. PMID: 20187040.
8. Nikas S. P., Alapafuja S. O., Papanastasiou I., Paronis C. A., Shukla V. G., Papahatjis D. P., Bowman A. L.,
Halikhedkar A., Han X., Makriyannis A. Novel 1ʹ,1ʹ-chain substituted hexahydrocannabinols: 9βhydroxy-3-(1-hexyl-cyclobut-1-yl) hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor
1 (CB1) agonist. J. Med. Chem., 2010, 53, 6996-7010. PMID: 20925434.
9. Godlewski G., Alapafuja S. O., Bátkai S., Nikas S. P., Cinar R., Offertáler L., Osei-Hyiaman D., Liu J.,
Mukhopadhyay B., Harvey-White J., Tam J., Pacak K., Blankman J. L., Cravatt B. F., Makriyannis A.,
Kunos G. Novel inhibitor of fatty acid amide hydrolase normalizes cardiovascular function in
hypertension without adverse metabolic effects. Chem. Biol. 2010, 17, 1256-1266. PMID: 21095576.
10. Spyros P. Nikas, Marsha D’Souza, Alexandros Makriyannis. Enantioselective synthesis of (10S)- and
(10R)-methyl-anandamides. Tetrahedron, 2012, 68, 6329-6337.
11. Shakiru O. Alapafuja, Spyros P. Nikas, Indu T. Bharathan, Vidyanand G. Shukla, Mahmoud L. Nasr, Anna
L. Bowman, Nikolai Zvonok, Jing Li, Xiaomeng Shi, John R. Engen, Alexandros Makriyannis. Sulfonyl
fluoride inhibitors of fatty acid amide hydrolase. J. Med. Chem., 2012, 55, 10074-10089.
12. Gunduz-Cinar, O.; MacPherson, K. P.; Cinar, R.; Gamble-George, J.; Sugden, K.; Williams, B.; Ramikie, T.
S.; Gorka, A. X.; Alapafuja, S. O.; Nikas, S. P.; Makriyannis, A.; Poulton, R.; Patel, S.; Hariri, A. R.;
Caspi, A.; Moffitt, T. E.; Kunos, G.; Holmes, A. Convergent translational evidence of a role for
anandamide in amygdala-mediated fear extinction, threat processing and stress-reactivity. Mol.
Psychiatry 2012, accepted, doi:10.1038/mp.2012.72.
D. Selected Patents
1. Makriyannis, A., Nikas, S. P., Khanolkar, A. D. Νovel bicyclic and tricyclic cannabinoids. WO 03005960 A2,
2003.
2. Makriyannis, A., Nikas, S. P., Khanolkar, A. D. Bicyclic and Tricyclic Cannabinoids. US Patent No. 7057076,
2006.
3. Makriyannis, A., Nikas, S. P., Khanolkar, A. D. Novel bicyclic and tricyclic cannabinoids. Continuation in part,
US Patent No. 7285683, 2007.
4. Makriyannis, A., Nikas, S. P., Khanolkar, D. A., Thakur, G. A., Lu, D. Bicyclic cannabinoids. Continuation in
part, US Patent No. 7446229, 2008.
5. Makriyannis, A., Nikas, S. P., Alapafuja, S. O., Shukla, V. Fatty acid amide hydrolase inhibitors. WO
2008/013963A2, 2008.
6. Makriyannis, A., Nikas, S. P., Alapafuja, S. O., Shukla, V. Monoacylglycerol lipase inhibitors for modulation
of cannabinoid activity. WO 2009/052319 A1, 2009.
7. Makriyannis, A., Nikas, S. P., Alapafuja, S. O. Angiogenic resorcinol derivatives. WO 2011/006099A1, 2011.