Kelvin W. Gee
Professor, Pharmacology
School of Medicine
School of Medicine
Ph.D., University of California, Davis, 1981, Pharmacology & Toxicology
University of California, Irvine
Department of Pharmacology
110C Med Surge 1
Mail Code: 4625
Irvine, CA 92697
Department of Pharmacology
110C Med Surge 1
Mail Code: 4625
Irvine, CA 92697
Research Interests
receptors, drug discovery, early drug development, ion channels, GABA, nicotine
Websites
Research Abstract
Dr. Gee is a neuropharmacologist whose principal interests are mechanisms of regulation of signaling through ligand-gated ion channels and the identification of novel signal transduction-based therapeutic strategies for the treatment of disorders amenable to modulation of signal transduction pathways.
His laboratory is currently characterizing the pharmacology of several novel allosteric modulatory sites on the GABAA receptor complex and the alpha7 nicotinic receptor using tissue and recombinantly derived receptors as well as studying the behavioral consequences of modulatory site activation. These sites include for example one for certain neuroactive steroids and another for compounds related to the fluoroquinolone antibiotics.
The overall mission of the lab is to identify and characterize novel modulatory sites on ligand-gated ion channels, design and synthesize ligands for these sites and evaluate their potential as novel therapeutic agents useful in the treatment of human diseases.
Patents & Patent Applications:
Gee KW, Bolger MB, Brinton RE, Burke D and McEwen, BS: Method, compositions and compounds for modulating brain excitability. U.S. Patent Nos. 5,120,723 and 5,208,227.
Bolger, MB, Gee KW, Lan NC, Tahir H, Belelli D, Mirsadeghi S and Purdy R: Methods, compositions and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series. U.S. Patent No. 5,232,917.
Bolger MB, Gee KW, Lan NC, Belelli D, Mirsadeghi S, Purdy R and Tahir H. Methods, compositions and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series. U.S. Patent No. 5,591,733.
Gee KW: Use of peripheral-type benzodiazepine sites for treatment of CNS trauma or disease. U.S. Patent No. 5,550,124.
Lipkowski A and Gee KW– Substituted Guanidines and the Use Thereof. US Patent 6,875,759.
Hogenkamp DJ, Johnstone T and Gee KW: Novel quinolones for the treatment of neuropsychiatric disorders. U.S. Patent 7,355,047.
Hogenkamp DJ, Johnstone T and Gee KW: Substituted enaminones, their
derivatives and uses thereof. US Patent 7,820,663
Hogenkamp DJ, Johnstone T and Gee KW: Substituted enaminones, their
derivatives and uses thereof. US Patent 7,825,278
Johnstone, T., Hogenkamp, D. J., Gee, K. W.: Substituted heterocycles and their use as allosteric modulators of the nicotinic and GABAA receptors", US Patent 8,865,719.
His laboratory is currently characterizing the pharmacology of several novel allosteric modulatory sites on the GABAA receptor complex and the alpha7 nicotinic receptor using tissue and recombinantly derived receptors as well as studying the behavioral consequences of modulatory site activation. These sites include for example one for certain neuroactive steroids and another for compounds related to the fluoroquinolone antibiotics.
The overall mission of the lab is to identify and characterize novel modulatory sites on ligand-gated ion channels, design and synthesize ligands for these sites and evaluate their potential as novel therapeutic agents useful in the treatment of human diseases.
Patents & Patent Applications:
Gee KW, Bolger MB, Brinton RE, Burke D and McEwen, BS: Method, compositions and compounds for modulating brain excitability. U.S. Patent Nos. 5,120,723 and 5,208,227.
Bolger, MB, Gee KW, Lan NC, Tahir H, Belelli D, Mirsadeghi S and Purdy R: Methods, compositions and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series. U.S. Patent No. 5,232,917.
Bolger MB, Gee KW, Lan NC, Belelli D, Mirsadeghi S, Purdy R and Tahir H. Methods, compositions and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series. U.S. Patent No. 5,591,733.
Gee KW: Use of peripheral-type benzodiazepine sites for treatment of CNS trauma or disease. U.S. Patent No. 5,550,124.
Lipkowski A and Gee KW– Substituted Guanidines and the Use Thereof. US Patent 6,875,759.
Hogenkamp DJ, Johnstone T and Gee KW: Novel quinolones for the treatment of neuropsychiatric disorders. U.S. Patent 7,355,047.
Hogenkamp DJ, Johnstone T and Gee KW: Substituted enaminones, their
derivatives and uses thereof. US Patent 7,820,663
Hogenkamp DJ, Johnstone T and Gee KW: Substituted enaminones, their
derivatives and uses thereof. US Patent 7,825,278
Johnstone, T., Hogenkamp, D. J., Gee, K. W.: Substituted heterocycles and their use as allosteric modulators of the nicotinic and GABAA receptors", US Patent 8,865,719.
Publications
Ng H.J., Whittemore E.R., Tran M.B., Hogenkamp D.J., Broide R.S., Johnstone T.B.C., Zheng L., Stevens K.E. and Gee K.W. A nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators. Proc. Natl. Acad. Sci. USA, 104:8059-8064, 2007.
Hogenkamp D.J., Johnstone T.B.C., Huang J-C., Li W-Y., Tran M., Whittemore E.R., Bagnera R.E. and Gee K.W. Enaminone amides as novel orally active GABAA receptor modulators, J. Med. Chem., 50:3369-3379, 2007.
Yoshimura R.F., Hogenkamp D.J., Li W-Y., Tran M., Belluzi J.D., Whittemore E.R., Leslie F.M. and Gee K.W. Negative allosteric modulation of nicotinic acetylcholine receptors blocks nicotine self-administration in rats, J Pharmacol Exp Ther 323:907-915, 2007.
Gee KW, Tran MB, Hogenkamp DJ, Johnstone TB, Bagnera RE, Yoshimura RF, Huang J-C, Belluzzi JD and Whittemore ER: Limiting activity at b1-subunit containing GABAA receptor subtypes reduces sedative liability, J Pharmacol Exp Ther 332:1040-1053, 2010.
Johnstone TBJ, Gu Z, Yoshimura RF, Villegier AS, Hogenkamp DJ, Whittemore ER, Huang JC, Tran MB, Belluzzi JD, Yakel JL and Gee KW: Allosteric modulation of related ligand-gated ion channels synergistically induces long term potentiation in the hippocampus and enhances cognition, J Pharmacol Exp Ther 336:908-915, 2011.
Hogenkamp DJ, Ford-Hutchinson T, Yoshimura RF, Tran MB, Johnstone TBJ, Bascom G, Rollins H, Lu L, Whittemore ER and Gee KW: Design, synthesis and activity of a series of arylpyrid-3-ylmethanones as type I positive allosteric modulators of a7 nicotinic acetylcholine receptors. J Med Chem 56:8352-8365, 2013.
Hogenkamp DJ, Tran MB, Yoshimura RF, Johnstone TB and Gee KW: Pharmacological profile of a 17ß-heteroaryl-substituted neuroactive steroid. Psychopharmacol (Berl) 231:3517-3524, 2014.
Yoshimura RF, Tran MB, Hogenkamp DJ, Johnstone TBJ and Gee KW: Limited central side effects of a beta-subunit subtype selective GABAA receptor allosteric modulator. J Psychopharmacol 28:472-478, 2014.
Gee KW, Olincy A, Kanner R, Johnson L, Hogenkamp D, Harris J, Tran M, Edmonds SA, Sauer W, Yoshimura R, Johnstone T, Freedman R. First in human trial of a type I positive allosteric modulator of alpha7-nicotinic acetylcholine receptors: Pharmacokinetics, safety, and evidence for neurocognitive effect of AVL-3288. J Psychopharmacol. 31:434-441, 2017.
Yoshimura RF, Tran MB, Hogenkamp DJ, Ayala NL, Johnstone T, Dunnigan AJ, Gee TK, Gee KW. Allosteric modulation of nicotinic and GABAA receptor subtypes differentially modify autism-like behaviors in the BTBR mouse model. Neuropharmacology 126:38-47, 2017.
Hogenkamp D.J., Johnstone T.B.C., Huang J-C., Li W-Y., Tran M., Whittemore E.R., Bagnera R.E. and Gee K.W. Enaminone amides as novel orally active GABAA receptor modulators, J. Med. Chem., 50:3369-3379, 2007.
Yoshimura R.F., Hogenkamp D.J., Li W-Y., Tran M., Belluzi J.D., Whittemore E.R., Leslie F.M. and Gee K.W. Negative allosteric modulation of nicotinic acetylcholine receptors blocks nicotine self-administration in rats, J Pharmacol Exp Ther 323:907-915, 2007.
Gee KW, Tran MB, Hogenkamp DJ, Johnstone TB, Bagnera RE, Yoshimura RF, Huang J-C, Belluzzi JD and Whittemore ER: Limiting activity at b1-subunit containing GABAA receptor subtypes reduces sedative liability, J Pharmacol Exp Ther 332:1040-1053, 2010.
Johnstone TBJ, Gu Z, Yoshimura RF, Villegier AS, Hogenkamp DJ, Whittemore ER, Huang JC, Tran MB, Belluzzi JD, Yakel JL and Gee KW: Allosteric modulation of related ligand-gated ion channels synergistically induces long term potentiation in the hippocampus and enhances cognition, J Pharmacol Exp Ther 336:908-915, 2011.
Hogenkamp DJ, Ford-Hutchinson T, Yoshimura RF, Tran MB, Johnstone TBJ, Bascom G, Rollins H, Lu L, Whittemore ER and Gee KW: Design, synthesis and activity of a series of arylpyrid-3-ylmethanones as type I positive allosteric modulators of a7 nicotinic acetylcholine receptors. J Med Chem 56:8352-8365, 2013.
Hogenkamp DJ, Tran MB, Yoshimura RF, Johnstone TB and Gee KW: Pharmacological profile of a 17ß-heteroaryl-substituted neuroactive steroid. Psychopharmacol (Berl) 231:3517-3524, 2014.
Yoshimura RF, Tran MB, Hogenkamp DJ, Johnstone TBJ and Gee KW: Limited central side effects of a beta-subunit subtype selective GABAA receptor allosteric modulator. J Psychopharmacol 28:472-478, 2014.
Gee KW, Olincy A, Kanner R, Johnson L, Hogenkamp D, Harris J, Tran M, Edmonds SA, Sauer W, Yoshimura R, Johnstone T, Freedman R. First in human trial of a type I positive allosteric modulator of alpha7-nicotinic acetylcholine receptors: Pharmacokinetics, safety, and evidence for neurocognitive effect of AVL-3288. J Psychopharmacol. 31:434-441, 2017.
Yoshimura RF, Tran MB, Hogenkamp DJ, Ayala NL, Johnstone T, Dunnigan AJ, Gee TK, Gee KW. Allosteric modulation of nicotinic and GABAA receptor subtypes differentially modify autism-like behaviors in the BTBR mouse model. Neuropharmacology 126:38-47, 2017.
Grants
Gee, Kelvin W. (Principal Investigator), "“Pain drugs based on nicotinic receptor subtype antagonists”," National Institute on Drug Abuse, R01-DA041454, $2,286,832 (DC), (2017 - 2020).
Gee, Kelvin W. (Principal Investigator), “Neurosteroids as a standard medical countermeasure for OP poisoning”, National Institute of Neurological Disorders & Stroke, U01-NS102131, $1,182,525 (DC), (2017 - 2020).
Gee, Kelvin W. (Co-Investigator, PI: Coleen Atkins, University of Miami), "Rehabilitation strategies for Memory Dysfunction after Traumatic Brain Injury," National Institute of Neurological Disorders & Stroke, R01-N069721, $232,235 (DC), (2015 - 2020).
Professional Societies
American Society for Pharmacology and Experimental Therapeutics
The Society for Neuroscience
Western Pharmacology Society
The American Society for Neurochemistry
Sigma Xi
Graduate Programs
Interdepartmental Neuroscience Program
Medicinal Chemistry and Pharmacology
Pharmacological Sciences
Research Centers
The Center for Autism & Neurodevelopmental Disorders
Link to this profile
https://faculty.uci.edu/profile/?facultyId=2310
https://faculty.uci.edu/profile/?facultyId=2310
Last updated
10/26/2017
10/26/2017