Projects and Grants per year
Personal profile
Research Interests
Target Validation, Lead Discovery, and Lead Optimization for Neglected Diseases
My group focuses on the discovery and preclinical development of new therapeutic leads for neglected diseases. We place a major focus on discovering new therapeutic chemotypes, determining their mechanism of action, and conducting proof-of-concept studies in pharmacokinetic/pharmacodynamic (PK/PD) models of disease. All of the projects are intended to deliver well-validated compounds that have suitable pharmacokinetic and toxicology profiles for detailed in vivo studies. During my independent career, both historically and currently, the projects in my laboratory have been split roughly equally between oncology and protozoal diseases.
Our work spans the entire process from initial identification of new chemical hits through optimization of late leads in animal models and finally to the design and execution of human clinical trials. To date, our work has identified dozens of potential new leads for these diseases with novel mechanisms of action or novel applications. We have contributed to repurposing drugs for clinical trials for ependymoma, infantile ALL, and medulloblastoma; contributed a repurposed clinical candidate for retinoblastoma; and produced a novel clinical candidate, (+)-SJ733, for the treatment of malaria that is currently entering Phase 2 trials (https://clinicaltrials.gov/ct2/show/NCT02867059).
Expertise related to UN Sustainable Development Goals
In 2015, UN member states agreed to 17 global Sustainable Development Goals (SDGs) to end poverty, protect the planet and ensure prosperity for all. This person’s work contributes towards the following SDG(s):
Education/Academic qualification
Physiology, Postdoctoral Fellowship, Relationships between cholesterol homeostasis and ras and hedgehog signaling, University of Texas Southwestern Medical Center
Sep 1 1996 → Sep 1 1998
Doctor of Philosophy, The Scripps Research Institute
1996
Bachelor of Arts, Reed College
1990
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- 1 Similar Profiles
Collaborations and top research areas from the last five years
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Interactions Between Drug Combinations and Resistance Acquisition Risk for Antimalarial ATP4 Inhibitors
Guy, R. K. (PI)
National Institute of Allergy and Infectious Diseases
6/7/24 → 5/31/29
Project: Research project
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Combination of SJ733 with Tafenoquine as a Possible 1 or 2 Dose Radical Cure for P. Vivax Malaria
Guy, R. K. (PI) & Bush, H. (Former CoI)
9/12/23 → 9/30/25
Project: Research project
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Chemical Biology of the Control of Neddylation by DCN1
Guy, R. K. (PI)
7/1/19 → 6/30/25
Project: Research project
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Kentucky Center for Clinical and Translational Science - Institutional Career Development Core
Kelly, T. (PI), Barry-Hundeyin, M. (CoI), Curry, T. (CoI), DiPaola, R. (CoI), Evers, B. M. (CoI), Giannone, P. (CoI), Guy, R. K. (CoI), Helmy, Y. A. (CoI), Jicha, G. (CoI), Kern, P. (CoI), King, V. (CoI), Lephart, S. (CoI), Liu, J. (CoI), Talbert, J. (CoI), Trout, A. (CoI), Williams, L. (CoI), Bush, M. (CoPI), Arnett, D. (Former CoI), Duncan, M. (Former CoI), Heath, E. (Former CoI), Lacy Leigh, M. (Former CoI), McLouth, L. (Former CoI), Roberts, J. (Former CoI), Samaan, M. (Former CoI) & Supinski, G. (Former CoI)
National Center for Advancing Translational Sciences
8/15/16 → 6/30/26
Project: Research project
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Kentucky Center for Clinical and Translational Science
Kern, P. (PI), Adatorwovor, R. (CoI), Bauer, J. (CoI), Bumgardner, V. (CoI), Bush, M. (CoI), Bush, H. (CoI), Campbell, K. (CoI), Cassis, L. (CoI), Coker, A. (CoI), Conwell, D. (CoI), Curry, T. (CoI), Daugherty, A. (CoI), DiPaola, R. (CoI), Duncan, M. (CoI), Durbin, E. B. (CoI), Dutch, R. (CoI), Dwoskin, L. (CoI), Elam, C. (CoI), Ellingson, S. (CoI), Evers, B. M. (CoI), Fisher, S. (CoI), Fowlkes, J. (CoI), Garcia, A. (CoI), Goldstein, L. (CoI), Griffith, C. (CoI), Guy, R. K. (CoI), Harris, J. (CoI), Harris, D. (CoI), Hatton, K. (CoI), Haynes, E. (CoI), Hussain, R. (CoI), Jicha, G. (CoI), Jones, A. (CoI), Kelly, T. (CoI), King, V. (CoI), Kruse-Diehr, A. (CoI), Kryscio, R. (CoI), Lile, J. (CoI), Mahmoud, K. A. (CoI), Messaoudi Powers, I. (CoI), Moseley, H. (CoI), Mudd, G. (CoI), Noehren, B. (CoI), Prisinzano, T. (CoI), Roper, K. (CoI), Rush, C. (CoI), Sawaya, B. (CoI), Schoenberg, N. (CoI), Shaddox, L. (CoI), Sheppard, M. (CoI), Slade, E. (CoI), Smalls, B. (CoI), Stevens-Watkins, D. (CoI), Stoops, W. (CoI), Surratt, H. (CoI), Talbert, J. (CoI), Tannock, L. (CoI), Thompson, J. (CoI), Thorson, J. (CoI), Van Eldik, L. (CoI), Walsh, S. (CoI), Weiss, H. (CoI), Westgate, P. (CoI), Whitehurst, L. (CoI), Williams, L. (CoI), Zhang, X. (CoI), Hartmann, K. (CoPI), Burnett, C. (Former CoI), Cardarelli, K. (Former CoI), Chen, J. (Former CoI), Dugan, A. (Former CoI), Ebbert, M. T. W. (Former CoI), Feltner, F. (Former CoI), Gilbert, P. (Former CoI), Glasser, S. (Former CoI), Hahn, E. (Former CoI), Holloway, L. (Former CoI), Jacobs, N. (Former CoI), Kasarskis, E. (Former CoI), Kavuluru, R. (Former CoI), Li, J. (Former CoI), Malluche, H. (Former CoI), Newman, M. (Former CoI), Peterson, C. (Former CoI), Selwitz, A. (Former CoI), Truszczynski, M. (Former CoI), Waters, T. (Former CoI), Webb, N. (Former CoI), Williams, M. (Former CoI) & de Beer, F. (Former CoI)
National Center for Advancing Translational Sciences
8/15/16 → 6/30/26
Project: Research project
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Antitrypanosomal Chloronitrobenzamides
Carrillo, A. K., Kadayat, T. M., Hwang, J. Y., Chen, Y., Zhu, F., Holbrook, G., Gillingwater, K., Connelly, M. C., Yang, L., Kaiser, M. & Guy, R. K., Mar 14 2024, In: Journal of Medicinal Chemistry. 67, 5, p. 3437-3447 11 p.Research output: Contribution to journal › Article › peer-review
1 Scopus citations -
Feasibility of pharmacy-based research opportunity to enhance community testing and surveillance
Venditto, V. J., Hudspeth, B., Freeman, P. R., Qasrawi, L., Guy, R. K., Farley, V. H., Johnson, R. A., Freeman, E., Henson, D., Marion, R., Wagner, S. B., Doratt, B. M. & Messaoudi-Powers, I., Jun 29 2024, (E-pub ahead of print) In: Journal of the American Pharmaceutical Association (Washington,D.C. : 1996). p. 102151Research output: Contribution to journal › Article › peer-review
1 Scopus citations -
Optimization of diastereomeric dihydropyridines as antimalarials
Van Horn, K. S., Zhao, Y., Parvatkar, P. T., Maier, J., Mutka, T., Lacrue, A., Brockmeier, F., Ebert, D., Wu, W., Casandra, D. R., Namelikonda, N., Yacoub, J., Sigal, M., Knapp, S., Floyd, D., Waterson, D., Burrows, J. N., Duffy, J., DeRisi, J. L. & Kyle, D. E. & 2 others, , Sep 5 2024, In: European Journal of Medicinal Chemistry. 275, p. 116599Research output: Contribution to journal › Article › peer-review
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Optimization of diastereomeric dihydropyridines as antimalarials
Van Horn, K. S., Zhao, Y., Parvatkar, P. T., Maier, J., Mutka, T., Lacrue, A., Brockmeier, F., Ebert, D., Wu, W., Casandra, D. R., Namelikonda, N., Yacoub, J., Sigal, M., Knapp, S., Floyd, D., Waterson, D., Burrows, J. N., Duffy, J., DeRisi, J. L. & Kyle, D. E. & 2 others, , Sep 5 2024, In: European Journal of Medicinal Chemistry. 275, 116599.Research output: Contribution to journal › Article › peer-review
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Synthesis and biological evaluation of 4,7,9-trisubstituted benzoxazepines as antileishmanial agents
Kadayat, T. M., Kwiatkowski, S., Ortiz, D., Shoeran, G., Hammill, J. T., Kim, H. S., Cholewo, J., Landfear, S. M. & Kiplin Guy, R., Dec 1 2024, In: Bioorganic and Medicinal Chemistry Letters. 114, 130003.Research output: Contribution to journal › Article › peer-review
2 Scopus citations
Prizes
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Philip S. Portoghese Medicinal Chemistry Lectureship Award
Guy, R. (Recipient), 2022
Prize: Honorary award
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Activities
- 1 Editorial work
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Journal of Medicinal Chemistry (Journal)
Guy, R. K. (Reviewer)
2014 → …Activity: Publication peer-review and editorial work › Editorial work