Research

The NIAAA is the lead agency for U.S. research on the causes, consequences, prevention and treatment of alcohol use disorder and alcohol-related problems.

Section on Medicinal Chemistry

Contact Information

  • Office: 301-443-2807

Overview of the Lab

The principal mission of the lab is to develop selective probes and drug-like molecules to enable the study of molecular mechanisms in alcohol associated diseases. The lab aims to use medicinal chemistry and chemical biology approaches to design, synthesize and biologically characterize novel druggable tools for select GPCRs and enzymatic drug targets implicated in pain, inflammatory and fibrotic disorders. Our overarching goal is to facilitate the development of effective, polypharmacological agents with translatable potential for complex chronic conditions.

Research Projects

  1. Functionally selective modulators targeting the endocannabinoid system
  2. ‘Tailored Polypharmacology’/Designed Multi-target agents for treating inflammatory and fibrotic disorders
  3. Synthetic methodology development for drug discovery
  4. Preclinical studies in collaboration with Section on Fibrotic Disorders and Laboratory of Physiologic Studies

Lab Members

Selected Publications

  1. Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB1 R) Antagonist. Liu, Z.; Iyer, M. R.; Godlewski, G.; Jourdan, T.; Liu, J.; Coffey, N. J.; Zawatsky, C. N.; Puhl, H. L.; Wess, J.; Meister, J.; Liow, J.-S.; Innis, R. B.; Hassan, S. A.; Lee, Y. S.; Kunos, G.; Cinar, R. ACS Pharmacol. Transl. Sci. 2021, 4, 1175-1187.
  2. Dual Inhibition of CB1 Receptors and iNOS as a Potential Novel Approach to the Pharmacological Management of Acute and Long COVID-19. Cinar, R.; Iyer, R.; Kunos, G. Br. J. Pharmacol. 2021, 15461.
  3. Cholesterol as a modulator of cannabinoid CB2 Yeliseev, A.; Iyer, M. R.; Joseph, T.T.; Coffey, N. J.; Cinar, R.; Zoubak. L.; Kunos, G.; Gawrisch, K. Sci Rep. 2021, 11, 3706.
  4. The Therapeutic Potential of Second and Third Generation CB1R Antagonists Cinar, R.; Iyer, M. R.; Kunos G. Ther. 2020, 208, 1-24.
  5. Crystal Structure of Human Cannabinoid Receptor CB2. Li, X.; Hua, T.; Vemuri, K.; Ho, Jo-Hao.; Wu, Y.; Wu, L.; Katrich, V.; Benchama, O.; Zvonok, N.; Locke, K.; Qu, L.; Won Han, G.; Iyer, M. R.; Cinar, R.; Coffey, N. J.; Wang, J.; Wu, M.; Zhao, Su.; Kunos, G.; Bohn, L.; Makriyannis; Stevens, R. C.; Liu Z-J.; Cell, 2019, 176, 459-467.
  6. Design, Synthesis and Biological Evaluation of Novel Non-Brain Penetrant Hybrid Cannabinoid CB1R inverse agonist/inducible nitric oxide synthase (iNOS) inhibitors for the treatment of liver fibrosis. Iyer, M. R.; Cinar, R.; Katz, A..; Gao, M.; Erdelyi, K.; Jourdan, T.; Coffey, N. J.; Pacher, P.; Kunos, G. Med. Chem 2017, 60, 1126-1141.

See Pubmed for all publications. 

Selected Patents (granted):

  1. Cannabinoid Receptor Mediating Compounds
    Inventors: Kunos, G.; Iyer M R.; Cinar, R.; Rice, K. C Patent number: 9765031
  2. Pyrazole Derivatives and their Use as Cannabinoid Receptor Mediators
    Inventors: Kunos, G.; Iyer M R.; Cinar, R.; Rice, K. C Patent number: 10329259
  3. Induction of Highly Specific Antibodies to a Hapten but not to a Carrier Peptide by Immunization with an Adjuvanted Hapten-Peptide Conjugate Associated with Liposomes
    Inventors: Alving, C. R.; Matyas G. R.; Mayorov, A. V.; Rice, K. C.; Iyer, M. R.; Cheng, K.;  Li, F.; Jacobson, A. E. Patent number: 9193739

Other Lab Resources

For CB1/CB2 research tools and compounds, please contact malliga.iyer@nih.gov

Section Alumni/Direct Supervision: Casey Wood, Post-bac IRTA Fellow 2019-2021
Kyu Ah Kim, Post-Doc Visiting Fellow 2017-2019

Summer Students:
Puja Terse (2018)
Arthi Thyagarajan (2018)

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