Werner J. Geldenhuys, B.Pharm., Ph.D.
Assistant Professor of Pharmaceutical Sciences
Dr. Geldenhuys graduated from Potchefstroom University, South Africa (now North-West University) in 1999 with a pharmacy degree. He then went on to receive a Ph.D. in medicinal chemistry (2004) after completing a Masters Degree in medicinal chemistry (2002), both from North-West University.
After graduation, he was a post-doctoral research scientist at Texas Tech Health Science Center School of Pharmacy (TTUHSC) in Amarillo, TX, where he studied iron uptake into neuronal cells via the L-type calcium channel. Afterwards, he worked in the blood-brain barrier field, also at TTUHSC, where he investigated the effects of cigarette smoke on the distribution of drugs across the blood-brain barrier.
2004: Ph.D. in Medicinal Chemistry/Pharmaceutical Sciences, Potchefstroom University (now North-West University), South Africa
2002: M.Sc. in Pharmaceutical Chemistry, Potchefstroom University, Potchefstroom, South Africa
1999: B.Pharm., Potchefstroom University, Potchefstroom, South Africa
2008-present: Graduate Faculty Member (Neuroscience and Pharmacology), Kent State University, School of Biomedical Sciences, Kent, OH
2008-present: Director, Computational and modeling lab, Department of Pharmaceutical Sciences, Northeastern Ohio Universities College of Pharmacy, Rootstown, OH
2007-present: Assistant Professor, Department of Pharmaceutical Sciences, Northeastern Ohio Universities College of Pharmacy, Rootstown, OH
2004-2006: Postdoctoral Research Associate, Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech Health Sciences Center, Amarillo, TX
My group focuses on developing and understanding novel compounds which could be used in the treatment and prevention of neurodegenerative disorders, such as Parkinson’s, Alzheimer’s disease and stroke. We utilize in silico computer-assisted drug design (CADD) techniques. Novel compounds are either identified through virtual screening or are synthesized in our lab. Currently, the main drug target we are pursuing is a mitochondrial protein called mitoNEET (CISD1). This novel protein may play an important role regulating the oxidative capacity of mitochondria, and could be modulated to prevent apoptosis of neurons. We have identified several lead compounds (synthetic and from natural dietary sources) and are currently evaluating the biology and structure-activity relationships of these compounds.
A second focus of my group, is the development of novel drug delivery systems, such as nanoparticles. The blood-brain barrier and blood-retinal barrier are selectively permeable, and prevents several compounds/drugs from reaching the active site in sufficiently high concentrations to be effective. By understanding the physiology of these barriers, and developing novel nanoparticles, we are able to deliver compounds such as anti-cancer drugs more effectively to the brain or the eye.
Pharmaceutics with lab: In this course the Pharm.D. candidates are introduced to the different dosage forms used in clinical practice, as well as the physical-chemical pharmacy background. Additionally, the students are taught to interpret a prescription, as well as how to compound a prescription. In the lab, the students are engaged in preparing compounded medications, such as suspensions, capsules, PLO-gels, creams, ointments and troches, to name a few. Veterinary compounding is also discussed and shown in the lab. Another component of the course is the introduction to over-the-counter (OTC) or non-prescription medications, which allows the students to suggest an appropriate treatment for a OTC-specific symptom in the pharmacy. Course Director, course length is 156 hours.
Cosmeceuticals: In this course, the pharmacy students are introduced to advance compounding techniques via cosmetic product formulation. The science of cosmeceuticals blends traditional cosmetics with natural products, which will enhance lives. In this lab, students are taught how to prepare shampoos, gels, ointments, lipsticks, sunscreens and perfumes/spray-on solutions. Additionally, the students work on developing their own brand of cosmetic/cosmeceutical product(s) for their pharmacy. Course Director.
Nutraceuticals: In this course, the Pharm.D. students are introduced to aspects of homeopathy, as well as natural product pharmacology, such as ginseng. Additionally, vitamins, supplements (e.g. chondriotin, glucosamine) and sports supplements are introduced. Assistant Course Director.
Dr. Geldenhuys' publication recently listed in PubMed:
Geldenhuys, W.J. and Van der Schyf, C.J. Designing drugs with multi-target activity: the next step in the treatment of neurodegenerative disorders". Expert Opinion on Drug Discovery, 2013, in press, DOI:10.1517/17460441.2013.744746.
Geldenhuys, W.J. and Van der Schyf, C.J. Rationally designed multi-targeted agents against neurodegenerative diseases. Current Medicinal Chemistry, 2013, in press.
Al-Baghdadi, O.B., Prater, N.I., Van der Schyf, C.J., Geldenhuys WJ. Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease. Bioorganic and Medicinal Chemistry Letters, 2012, 22, 7183-7188.
Lockman, J.A., Geldenhuys, W.J., Jones-Higgins, M.R., Patrick, J.D., Allen, D.D., Van der Schyf, C.J. NGP1-01, a multi-targeted polycyclic cage amine, attenuates brain endothelial cell death in iron overload conditions. Brain Research, 2012, 1489, 133-139.
Wehrung, D., Geldenhuys, W.J., Oyewumi, M.O. Effects of gelucire content on stability, macrophage interaction and blood circulation of nanoparticles engineered from nanoemulsions. Colloid Surf. B: Biointerfaces (2012), doi:10.1016/j.colsurfb. 2012.02.005.
Geldenhuys, W.J., Mbimba, T., Bui, T., Harrison, K., Sutariya, V. “Brain-targeted delivery of paclitaxel using glutathione-coated nanoparticles for brain cancers.” J Drug Target. 2011 Jun 21. [Epub ahead of print]
Lockman, J.A., Geldenhuys, W.J., Bohn, K.A., DeSilva, S.F., Allen, D.D. and Van der Schyf, C.J. “Differential effect of nimodipine in attenuating iron-induced toxicity in brain- and blood-brain barrier-associated cell types.” Neurochemical Research, 2011, in press.
Mbimba, T., Awale, P., Bhatia, D., Geldenhuys, W.J., Darvesh, A.S., Carroll, R.T., Bishayee, A. Alteration of Hepatic Proinflammatory Cytokines is Involved in the Resveratrol-Mediated Chemoprevention of Chemically-Induced Hepatocarcinogenesis. Curr Pharm Biotechnol. -- in press (2011).
Geldenhuys, W.J., Bishayee, A., Darvesh, A.S., Carroll, R.T. Natural Products of Dietary Origin as Lead Compounds in Virtual Screening and Drug Design. Curr Pharm Biotechnol. -- in press (2011).
Geldenhuys, W.J., Ko, K.S., Stinnett, H., Van der Schyf, C.J., and Lim, M.H. “Identification of Multifunctional Small Molecule-Based Reversible Monoamine Oxidase Inhibitors.” Medicinal Chemistry Communications, 2011, in press.
Geldenhuys, W.J., and Van der Schyf, C.J. “Role of serotonin in Alzheimer’s disease: A new therapeutic target?” CNS Drugs, 2011, 25, 765-781.
Geldenhuys, W.J., Youdim, M.B.H., Carroll, R.T., and Van der Schyf, C.J. “The Emergence of Designed Multiple Ligands for Neurodegenerative Disorders.” Progress in Neurobiology, 2011, 94, 347-359.
Geldenhuys W.J., Funk MO, Awale PS, Lin L, Carroll RT. “A novel binding assay identifies high affinity ligands to the rosiglitazone binding site of mitoNEET.” Bioorg Med Chem Lett. 2011 Sep 15;21(18):5498-501.
Carroll, R.T., Dluzen, D.E., Stinnett, H., Awale, P.S., Funk, M.O., Geldenhuys, W.J. “Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.” Bioorg Med Chem Lett. 2011 Aug 15;21(16):4798-803.
Arif W, Xu S, Isailovic D, Geldenhuys WJ, Carroll RT, Funk MO. “Complexes of the outer mitochondrial membrane protein mitoNEET with resveratrol-3-sulfate.” Biochemistry. 2011 Jun 28;50(25):5806-11.
Darvesh, A.S., Carroll, R.T., Geldenhuys, W.J., Gudelsky, G.A., Klein, J., Meshul, C.K., and Van der Schyf, C.J.: In vivo brain microdialysis: advances in neuropsychopharmacoloy and drug discovery. Expert Opinion on Drug Discovery, 2011, 6, 109-127.
Geldenhuys, W.J., Lockman, P.R., Philip, A.E., McAfee, J.H., Miller, B.L., McCurdy, C.R. and Allen, D.D. 2005. Inhibition of choline uptake by N-cyclohexylcholine, a high affinity ligand for the choline transporter at the blood-brain barrier. J. Drug. Target. 13, 259-266.
Lockman, P.R., McAfee, G., Geldenhuys, W.J., Van der Schyf, C.J., Abbruscato, T.J., Allen, D.D. 2005. Brain Uptake Kinetics of Nicotine and Cotinine after Chronic Nicotine Exposure. J. Pharmacol. Exp. Ther. 314, 636-642.
Geldenhuys, W.J., Lockman,P.R., Nguyen, T.H., Van der Schyf, C.J., Crooks, P.A., Dwoskin, L.P. and Allen, D.D. 2005. 3D-QSAR study of bis-azaaromatic quaternary ammonium analogs at the blood-brain barrier choline transporter. Bioorg. Med. Chem. 13, 4253-4261.
Mdzinarishvili, A., Geldenhuys, W.J., Abbruscato, T.J., Bickel, U., Klein, J., Van der Schyf, C.J. 2005. NGP1-01, a lipophilic polycyclic cage amine, is neuroprotective in focal ischemia. Neurosci. Lett. 383, 49-53.
Dheyongera, J.P., Geldenhuys, W.J., Dekker, T.G., Matsabisa, M.G. and Van der Schyf, C.J. 2005. Antimalarial activity of thioacridone compounds related to the acronycine alkaloid. Bioorg. Med. Chem. 13, 1653-1659.
Dheyongera, J.P., Geldenhuys, W.J., Dekker, T.G. and Van der Schyf, C.J. 2005. Synthesis, biological evaluation, and molecular modeling of novel thioacridone derivatives related to the anticancer alkaloid acronycine. Bioorg. Med. Chem. 13, 689-698.
Geldenhuys, W.J., Malan, S.F., Bloomquist, J.R., Marchand, A.P. and Van der Schyf, C.J. 2005. Pharmacology and structure-activity relationships of bioactive polycyclic cage compounds: A focus on pentacycloundecane derivatives. Med. Res. Rev. 25, 21-48.
Lockman, P. R., McAfee, J.H., Geldenhuys, W.J., and Allen, D.D. 2004. Cation transport specificity at the blood–brain barrier. Neurochem. Res. 29, 2245–2250
Geldenhuys, W.J., Lockman, P.R., McAfee, J.H., Fitzpatrick, K.T., Van der Schyf, C.J. and Allen, D.D. 2004. Molecular modeling studies on the active binding site of the blood-brain barrier choline transporter. Bioorg. Med. Chem. Lett. 14, 3085-3092.
Geldenhuys, W.J., Malan, S.F., Murugesan, T., Van der Schyf, C.J., and Bloomquist, J.R. 2004. Synthesis and biological evaluation of pentacyclo[5.4.0.02,6.03,10.05,9]undecane derivatives as therapeutic agents in Parkinson's disease. Bioorg. Med. Chem. 12, 1799-1806.
Geldenhuys, W.J., Terre'Blanche, G. and Malan, S.F. 2003. Screening of novel pentacyclo-undecylamines for neuroprotective activity. Eur. J. Pharamcol. 458, 73-79.
Multimodal Drugs and Their Future for Alzheimer’s and Parkinson’s Disease. Van der Schyf, C.J., and Geldenhuys, W.J. in: International Review of Neurobiology, Volume 100: Various Aspects of Monoamine Oxidase and Its Inhibitors. Edited by: Moussa B.H. Youdim and Peter Riederer, 2011, ISBN 10: 0-12-366857-3 Elsevier Limited. Oxford, United Kingdom, pp. 107-125, DOI: 10.1016/B978-0-12-386467-3.00006-6