Christopher Hulme, PhD

Associate Professor of Pharmacology and Toxiclogy
Associate Professor of Organic and Medicinal Chemistry
Director, Southwest Comprehensive Center for Drug Discovery and Development, University of Arizona
Phone Number: 
(520) 626-5322
FAX: 
(520) 626-2466

UACC Information

UACC Organizational Unit: 
Professional Bio: 

Dr. Hulme has built and run several high-throughput medicinal chemistry organizations in industry and transitioned to an academic role in late 2007.  He has managed portfolios of targets spanning the value chain in drug discovery from hit generation to progression of molecules into man and as such managed teams that produced early development candidates for PDEIV (Rhone-Poulenc Rorer) and VR-1 (Amgen).  In total, it is estimated that 60+ targets of interest have passed through his organizations, spanning a multitude of therapeutic areas that include oncology, metabolic disorders, inflammation, pain, and neurodegeneration.

As Director of BIO5 Medicinal Chemistry, Dr. Hulme has the resources and extensive infrastructure in place to initiate and significantly progress the translational campaign. More specifically, CNS projects previously falling under his jurisdiction include the development of inhibitors of JNK-3 for stroke (Amgen), MCHr for obesity (Amgen), Pyk-2 for the treatment of brain gliomas (University of Arizona) and BACE for Alzheimer’s (Lilly). A significant number of other kinases were also part of prior industrial portfolios he ran, including JNK-1, PKB, Aurora A/B and Plk-1, and preliminary collaborations at the University of Arizona and Yale include targeting Plk-4, ROCK and aPKC. Indeed, the Phe is well versed in addressing the need for molecular pre-requisite physico-chemical properties that enable passive BBB penetration and minimization of residence time in the BBB lipid bi-layer to dial out potential pGP efflux liabilities.

Dr. Hulme has been involved in kinase research for ~ 20 years, being a co-author on one of the very early medicinal chemistry reviews in the field. The DYRK1A collaboration with Dr. Travis Dunckley has been active for more than three years although needs sustained funding to build on the significant progress to date. Recent reviews by the collaborators detail the state-of-art relevance of the target and current inhibitor design, and emerging indications for Glioblastoma are being investigated. In short, he is extremely qualified to pursue members of the kinase target-family in the neurodegeneration field and this is supplemented by his national/international reputation in high-throughput medicinal chemistry and file enhancement arenas.

Research Information

Research Program: 
Therapeutic Development
Member Status: 
Research Member
Year of Membership Acceptance: 
2010
Institution: 
University of Arizona
College: 
College of Pharmacy
Selected Publications: 

Dr. Hulme's NCBI bibliography

  1. Hulme, C., Moriarty, K., Huang, F-C., Souness, J. & Djuric, S.W. (1998). Quaternary Substituted PDE4 Inhibitors II: Novel Series of g-lactams. Bioorganic Medicinal Chemistry Letters, 8, 399.
  2. Hulme, C., Mathew, R., Moriarty, K., Souness, J., Cox, P., Uhl, J., & Djuric, S.W. (1998). The Synthesis and Biological Evaluation of a Novel Series of Indole PDEIV Inhibitors. Bioorganic Medicinal Chemistry Letters, 8, 1867.
  3. Hulme, C., Mathew, R., Moriarty, K., Souness, Uhl, J., Huang, F-C., & Djuric, S.W. (1998). Orally Active Indole N-Oxide PDEIV Inhibitors. Bioorganic Medicinal Chemistry Letters, 8, 3053.
  4. Hulme, C., Tang, S. C. Burns, C., & Labaudiniere, R. (1998). Improved Procedure for the Solution Phase Synthesis of 1,4-Benzodiazepines-2,5-dione Libraries via the Ugi reaction and Armstrong’s Convertible Isonitrile. Journal of Organic Chemistry, 63, 8021.
  5. Hulme, C., Ma, L., Romano, J., Morton, G., Tang, S-Y., Cherrier, M-P., Choi, S., & Labaudiniere, R. (2000). Novel Applications of CO2/MeOH for the Synthesis of Hydantoins and Cyclic Ureas via the Ugi Reaction. Tetrahedron Letters, 41, 1883.
  6. Hulme, C., & Gore, V. (2003). Multi-component Reactions: Emerging Chemistry in Drug Discovery. Current Medicinal Chemistry, 10, 151.
  7. Xu, Z., De Moliner, F., Cappelli, A., Hulme, C. (2012). Ugi/Aldol Sequence: Expeditious Entry to Several Families of Densely Substituted Nitrogen Heterocycles. Angewandte Chemie International Edition, 51, 8037-8040.
  8. Hulme, C., Petit, J., Mousses, S., Yin, H., Dietrich, J., Meurice, N. (2010) Formation of the Southwest Comprehensive Center for Drug Discovery and Development: New technologies, organization, work flow and projections. Abstracts of Papers, 239th ACS National Meeting, San Francisco, CA, United States, March 21-25, MEDI-70.
  9. Ariza, G.M., Ayaz, M., Medda, F., Hulme, C. (2014). Synthesis of diverse nitrogen-enriched heterocyclic scaffolds using a suite of tunable one-pot multicomponent reactions. Journal of Organic Chemistry, 79, 5153-5162.
  10. Shaw, A.Y., Gokhale, V., Stratton, S.P., Hulme, C. (2014). Promising, early stage novel Androgen receptor antagonists in head-head comparisons with Enzalutamide and Bicalutamide. Abstract of Papers #2524, AACR Meeting Abstracts, San Diego, CA, April 5-9.
  11. Ariza, G.M., Hulme, C. (2015). Recent advances in allosteric androgen receptor inhibitors for the potential treatment of castration-resistant prostate cancer. Pharmaceutical Patent Analyst, in press.
  12. Shaw, A.Y., Gokhale, V., Stratton, S.P., Hulme, C. (2014). Promising, early stage novel Androgen receptor antagonists in head-head comparisons with Enzalutamide and Bicalutamide. Abstract of Papers #2524, AACR Meeting Abstracts, San Diego, CA, April 5-9.
  13. Ariza, G.M., Hulme, C. (2015). Recent advances in allosteric androgen receptor inhibitors for the potential treatment of castration-resistant prostate cancer. Pharmaceutical Patent Analyst, in press.
Collaborative Research: 
Ongoing:
5R01 CA138702                                 (Meuillet, PI)                                                                                                  07/01/10–06/30/16
NIH/NCI
Inhibition of Novel Molecular Targets of Prostaglandin Formation for Anti-tumor Activity.
The overall goal of the proposal is to develop novel strategies and agents for the improved treatment of colon cancer via modulation of PGE2 levels.
Role: Co-Investigator
 
Completed:
No Grant #                                          (Hulme PI)                                                                                                     06/01/12–07/01/13
UA BIO5 Drug Discovery Grant
Discovery and Development of DRK1A inhibitors for Neurodegenerative Disorders
The goal of this proposal was to improve affinity of low uM DRYK1A inhibitors and modulate physicochemical properties to enhance small molecule cell permeability for evaluation in a cell tau phosphoryation assay with the goal of garnering sustained funding for development of small molecule therapeutics for neurodegenerative diseases.
 
5P41 GM086190                                (Hulme PI)                                                                                                      08/05/10–05/31/14
NIH/NIGMS
Expeditious, Biologically Driven Pilot Libraries for File Enhancement
The aim of this application was to produce novel pilot-scale libraries for evaluation via the Molecular Library Screening Network (MLSCN).

Professional Information

Positions and Honors: 
Positions:
1994–1996     Research Scientist, Rhone-Poulenc Rorer, Collegeville, PA.
1996–1997     Senior Research Scientist, Rhone-Poulenc Rorer, Collegeville, PA.
1997–1998     Research Fellow, Rhone-Poulenc Rorer, Collegeville, PA.
1999–2004     Head of High-Throughput Medicinal Chemistry, Amgen, Thousand Oaks, CA.
2004–2007     Head of High-Throughput Medicinal Chemistry, Eli Lilly, Indianapolis, IN.
2007–2010     Associate Professor, University of Arizona, Tucson, AZ.
2010–Present  Professor Medicinal Chemistry, University of Arizona, Director BIO5 Medicinal Chemistry Tucson, AZ.
 
Honors:
2012            Host, 2012 ACS National Medicinal Chemistry Conference, Oro Valley, AZ.
2011            University of Arizona Leading Edge Researcher 2011.
2007–2008  Abbott Laboratories New Faculty Award for Creativity in Organic Chemistry.
2006            Lilly Award for Excellence in File Enhancement.
Other Experience and Professional Memberships/Affiliations: 
2015               Session Chair: MCR2015, Brasilia, Brazil.
2015               ANR Grant Reviewer
2014-Present  Editorial Board Member “Central Nervous System Agents in Medicinal Chemistry”
2014               University of Kansas KOBRE Drug Discovery Grant External Reviewer.
2012–2014     NWO Grant Reviewer.
2012               Host & Chair, ACS National Medicinal Chemistry Conference, Oro Valley, AZ
2011               R19 study section.
2011               Editor: Special Edition on Multi-Component reactions, MODI.
2010               Ad hoc Special Emphasis Panel (P01 grant renewals).
2009               Session Chair. Mastering Medicinal Chemistry, Feb’ 25-27, San Francisco.
2009               SBIR Study Section, October 2009, 2010.
2009               Member External Advisory Board, SPORE lung cancer initiative, University of Louisville.
2008                    Synthetic and Biological Chemistry B Study Section, October 2008.
2008               Member of Special Emphasis Panel July 2008:  NIH renewals for “Centers of Excellence in Chemical Methodologies and Library Development (CMLD).”
2007–2011     Associate Editor, Molecular Diversity.
2007-Present  Arizona Bioindustry Association (AZBio) member.
2007-Present  AACP Member (American Association of Colleges of Pharmacy).
2005               Member Study Section P41 Pilot Scale Libraries.
2004–2011     IUPAC Affiliate Member.
2003-Present  Editorial Advisory Boards of Current Organic Synthesis/ARKIVOC/Open Drug Discovery.
1999-Present  ACS member (American Chemical Society).
1997-Present  Ad hoc reviewer for more than 30 journals.

Academic Information

Post Doctoral: 
University of Texas at Austin
Doctorate: 
Hertford College, Oxford University
Undergraduate School: 
Hertford College, Oxford University