Dai Lu

Dai Lu

Associate Professor of Pharmaceutical Sciences

Texas A&M Irma Lerma Rangel College of Pharmacy
1010 W. Ave. B
Kingsville, Texas   78363

Phone: 361.221.0745
Fax: 361.221.0793

Education and Training

Harvard Medical School
Instructor of Neurology, 2007-2011

Brigham and Women’s Hospital & Harvard Medical School, Center for Neurologic Disease
Senior Chemist, 2006-2011

Harvard Medical School
Research Fellow, 2006-2007

National Institute of Health and Northeastern University
Postdoctoral Fellow, 2005-2006

University of Connecticut
Ph.D. in Pharmaceutical Sciences and Medicinal Chemistry, 2005

Peking Union Medical College, Chinese Academy of Medical Sciences, Beijing, China
M.S. in Medicinal Chemistry, 1991

Nankai University, Tianjin, China
B.S., Organic Chemistry, 1987

Teaching Interests

  • Entry level and advanced medicinal and organic chemistry
  • Pharmacology of drugs for oncology, diabetes and neurodegenerative diseases
  • Pharmaceutical sciences related to nanomedicine

Research Interests

  • Organic/medicinal chemistry
  • Natural products for developing potential therapeutic agents
  • Nanomedicine/Nanofabrication of drug loaded nanoparticles

The Lu laboratory is medicinal chemistry laboratory working in the interface of organic chemistry and pharmaceutical sciences. The lab is engaged in the discovery of potential therapeutics for the treatment of cancer, neurodegenerative diseases and various disorders associated with the endocannabinoid system such as pain, drug-addiction and obesity. The current research projects in the Lu lab include the synthesis of water-soluble analogs of natural products such as taxanes and cannabinoids; the synthesis of various pharmacologically important cannabinoid ligands including agonists, inverse agonists, and allosteric modulators; the synthesis of novel protein kinase inhibitors to regulate the Abelson kinases (ABLs) and cyclin dependent kinases (CDKs). The Lu lab is also interested in the preparation and fabrication of multi-drug-loaded nanoparticles to tackle the deadly pancreatic cancer. These research projects have been funded by National Institute of Health and the State of Texas. Dr. Lu’s contributions in medicinal chemistry include the discovery of the first type of intrinsically fluorescent ligands for the G-protein-coupled receptor CB1 and CB2, the discovery of one of the first two selective agonists for the CB2 cannabinoid receptor, the discovery of water-soluble cannabinoids, the discovery of a novel class of protein kinase inhibitors, and the discovery of a clinical drug candidate Buagafuran.

Selected Publications

  • Khurana, L.; Fu, B.; Duddupudi, A. L.; Liao, Y.-H.; Immadi, S. S.; Kendall, D. A.; Lu, D. Pyrimidinyl Biphenylureas: Identification of New Lead Compounds as Allosteric Modulators of the Cannabinoid Receptor CB1. Journal of Medicinal Chemistry 2017, 60, 1089-1104.
  • Zhang, J.; Lu, D.; Wei, H.-X.; Gu, Y.; Selkoe, D. J.; Wolfe, M. S.; Augelli-Szafran, C. E. Part 3: Notch-sparing γ-secretase inhibitors: SAR studies of 2-substituted aminopyridopyrimidinones. Bioorganic & medicinal chemistry letters 2016, 26, 2138-2141.
  • Wei, H.-X.; Lu, D.; Sun, V.; Zhang, J.; Gu, Y.; Osenkowski, P.; Ye, W.; Selkoe, D. J.; Wolfe, M. S.; Augelli-Szafran, C. E. Part 2. Notch-sparing γ-secretase inhibitors: The study of novel γ-amino naphthyl alcohols. Bioorganic & medicinal chemistry letters 2016, 26, 2133-2137.
  • Qiao, C.-J.; Ali, H. I.; Ahn, K. H.; Kolluru, S.; Kendall, D. A.; Lu, D. Synthesis and biological evaluation of indole-2-carboxamides bearing photoactivatable functionalities as novel allosteric modulators for the cannabinoid CB1 receptor. European Journal of Medicinal Chemistry 2016, 121, 517-529.
  • Lu, D.; Wei, H.-X.; Zhang, J.; Gu, Y.; Osenkowski, P.; Ye, W.; Selkoe, D. J.; Wolfe, M. S.; Augelli-Szafran, C. E. Part 1: Notch-sparing γ-secretase inhibitors: The identification of novel naphthyl and benzofuranyl amide analogs. Bioorganic & medicinal chemistry letters 2016, 26, 2129-2132.
  • Lu, D.; Dopart, R.; Kendall, D. A. Controlled downregulation of the cannabinoid CB1 receptor provides a promising approach for the treatment of obesity and obesity-derived type 2 diabetes. Cell Stress and Chaperones 2016, 21, 1-7.
  • Mahmoud, M. M.; Olszewska, T.; Liu, H.; Shore, D. M.; Hurst, D. P.; Reggio, P. H.; Lu, D.; Kendall, D. A. (4-(Bis (4-fluorophenyl) methyl) piperazin-1-yl)(cyclohexyl) methanone hydrochloride (LDK1229): A New Cannabinoid CB1 Receptor Inverse Agonist from the Class of Benzhydryl Piperazine Analogs. Molecular pharmacology 2015, 87, 197-206.
  • Vangara, K. K.; Ali, H. I.; Lu, D.; Liu, J. L.; Kolluru, S.; Palakurthi, S. SN-38-cyclodextrin complexation and its influence on the solubility, stability, and in vitro anticancer activity against ovarian cancer. AAPS PharmSciTech 2014, 15, 472-482.
  • Khurana, L.; Ali, H. I.; Olszewska, T.; Ahn, K. H.; Damaraju, A.; Kendall, D. A.; Lu, D. Optimization of chemical functionalities of indole-2-carboxamides to improve allosteric parameters for the cannabinoid receptor 1 (CB1). Journal of medicinal chemistry 2014, 57, 3040-3052.
  • Mahmoud, M. M.; Ali, H. I.; Ahn, K. H.; Damaraju, A.; Samala, S.; Pulipati, V. K.; Kolluru, S.; Kendall, D. A.; Lu, D. Structure–activity relationship study of indole-2-carboxamides identifies a potent allosteric modulator for the cannabinoid receptor 1 (CB1). Journal of medicinal chemistry 2013, 56, 7965-7975.
  • Ahn, K. H.; Mahmoud, M. M.; Samala, S.; Lu, D.; Kendall, D. A. Profiling two indole-2-carboxamides for allosteric modulation of the CB1 receptor. Journal of neurochemistry 2013, 124, 584-589.
  • Lu, D.; Nikas, S. P.; Han, X.-W.; Parrish, D. A.; Makriyannis, A. Synthesis and characterization of a compact tricyclic resorcinol from (+)-and (−)-3-pinanol. Tetrahedron letters 2012, 53, 4636-4638.
  • Augelli-Szafran, C. E.; Wei, H.-X.; Lu, D.; Zhang, J.; Gu, Y.; Yang, T.; Osenkowski, P.; Ye, W.; Wolfe, M. S. Discovery of notch-sparing γ-secretase inhibitors. Current Alzheimer Research 2010, 7, 207-209.
  • Lu, D.; Guo, J.; Duclos Jr, R. I.; Bowman, A. L.; Makriyannis, A. Bornyl-and isobornyl-Δ8-tetrahydrocannabinols: A novel class of cannabinergic ligands. Journal of medicinal chemistry 2008, 51, 6393-6399.
  • Guo, J.; Yang, D.-P.; Chari, R.; Tian, X.; Pavlopoulos, S.; Lu, D.; Makriyannis, A. Magnetically aligned bicelles to study the orientation of lipophilic ligands in membrane bilayers. Journal of medicinal chemistry 2008, 51, 6793-6799.
  • Duclos, R. I.; Lu, D.; Guo, J.; Makriyannis, A. Synthesis and characterization of 2-substituted bornane pharmacophores for novel cannabinergic ligands. Tetrahedron letters 2008, 49, 5587-5589.
  • Khanolkar, A. D.; Lu, D.; Ibrahim, M.; Duclos, J., Richard I; Thakur, G. A.; Malan, J., T Phillip; Porreca, F.; Veerappan, V.; Tian, X.; George, C. Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity. Journal of medicinal chemistry 2007, 50, 6493-6500.
  • Lu, D.; Kiran Vemuri, V.; Duclos, R. I.; Makriyannis, A. The cannabinergic system as a target for anti-inflammatory therapies. Current topics in medicinal chemistry 2006, 6, 1401-1426.
  • McLaughlin, P. J.; Lu, D.; Winston, K. M.; Thakur, G.; Swezey, L. A.; Makriyannis, A.; Salamone, J. D. Behavioral effects of the novel cannabinoid full agonist AM 411. Pharmacology Biochemistry and Behavior 2005, 81, 78-88.
  • McLaughlin, P.; Brown, C.; Winston, K.; Thakur, G.; Lu, D.; Makriyannis, A.; Salamone, J. The novel cannabinoid agonist AM 411 produces a biphasic effect on accuracy in a visual target detection task in rats. Behavioural pharmacology 2005, 16, 477-486.
  • Lu, D.; Meng, Z.; Thakur, G. A.; Fan, P.; Steed, J.; Tartal, C. L.; Hurst, D. P.; Reggio, P. H.; Deschamps, J. R.; Parrish, D. A. Adamantyl cannabinoids: a novel class of cannabinergic ligands. Journal of medicinal chemistry 2005, 48, 4576-4585.
  • Luk, T.; Jin, W.; Zvonok, A.; Lu, D.; Lin, X. Z.; Chavkin, C.; Makriyannis, A.; Mackie, K. Identification of a potent and highly efficacious, yet slowly desensitizing CB1 cannabinoid receptor agonist. British journal of pharmacology 2004, 142, 495-500.
  • Järbe, T.; DiPatrizio, N.; Lu, D.; Makriyannis, A. (−)-Adamantyl-Δ8-tetrahydrocannabinol (AM-411), a selective cannabinoid CB1 receptor agonist: effects on open-field behaviors and antagonism by SR-141716 in rats. Behavioural pharmacology 2004, 15, 517-521.
  • Liu, Q.; Wang, D.-h.; Li, C.; LU, D.; WANG, W.-j.; GUO, J.-y. Synthesis and CNS activities of alpha-agarofuran derivatives. Chinese Journal of Medicinal Chemistry 2003, 13, 125-130.
  • Guo, J.; Pavlopoulos, S.; Tian, X.; Lu, D.; Nikas, S. P.; Yang, D.-P.; Makriyannis, A. Conformational study of lipophilic ligands in phospholipid model membrane systems by solution NMR. Journal of medicinal chemistry 2003, 46, 4838-4846.
  • Khanolkar, A. D.; Lu, D.; Fan, P.; Tian, X.; Makriyannis, A. Novel conformationally restricted tetracyclic analogs of Δ 8-tetrahydrocannabinol. Bioorganic & medicinal chemistry letters 1999, 9, 2119-2124.

Selected Patents

  • Dai Lu, Changjiang Qiao, Boqiao Fu, Anantha Lakshmi Duddupudi, Zhixing Wu “Functionalized Pyrano[2,3-D]Pyrimidin-7-one Derivatives and Methods For Their Preparation And Use”. US 62/340,393, 2016. PCT/US2017/034082, 2017
  • Corinne Augelli-Szafran, Dai Lu, HanXun Wei, Jing Zhang, Michael Wolfe, Dennis Selkoe, CuiMan Cai, “Novel Sulfonamides”, WO2013/052700, US 61/543,287, 2013
  • Corinne Augelli-Szafran, Dai Lu, HanXun Wei, Jing Zhang, Michael Wolfe, Dennis Selkoe, “Sulfonamide-Containing Compounds”, WO2012/047926, US 61/389,537, 2012
  • Alexandros Makriyannis, Chen Li, Dai Lu, “Cannabinergic Lipid Ligands”. WO/2006/044381, PCT/US2003/026609, U.S. Patent: 8,202,893 B2, 2012.
  • Alexandros Makriyannis, Spyros Nikas, Atmaram Khanolkar, Ganesh A. Thakur, Dai Lu, “Bicyclic cannabinoids” US Patent No. 7446229, 2008.
  • Alexandros Makriyannis, Dai Lu, “Keto Cannabinoids with Therapeutic Indications”. WO/2004/017922, PCT/US2003/026609; U.S. Patent: 7183313, 2007.
  • Alexandros Makriyannis, Dai Lu, Atmaram Khanolkar, “Novel Analgesic and Immunomodulatory Cannabinoids”. International Patent Application, PCT/US99/09701, 2001

Honors and Awards

  • Team Teaching of the Year, TAMHSC RCOP (Cardiovascular Diseases), 2015-2016, 2016-2017
  • Team Teaching of the Year  TAMHSC RCOP (Endocrinology and Metabolic Diseases) 2011-2012
  • NIH National Service Award 2005.
  • International Cannabinoid Research Society, Travel Award, 2003, 2004.
  • Richardson-Vicks/ A. Francis Summa Memorial Award, 2003
  • Doctoral Dissertation Award, University of Connecticut, 2002
  • Boehringer Ingelheim Pharmaceuticals Research Fellowship, 1998-2000
  • Neurosciences Predoctoral Research Fellow, University of Connecticut, 1998, 1999, 2001