CV

CURRICULUM VITAE: Jetze J. Tepe

Department of Chemistry

Michigan State University

East Lansing, MI 48824

E-mail: tepe@chemistry.msu.edu

 

EDUCATION

Post-Doctoral Research Colorado State University, Fort Collins, Colorado, 1998-2000

Ph.D. Chemistry University of Virginia, Charlottesville, Virginia, 1998

B.S. Chemistry Jacksonville University, Jacksonville, Florida, 1992

Personal Statement: Prof. Tepe’s research is focused on the synthesis and biological evaluation of heterocyclic molecules to explore their use as mechanistically new therapeutic agents to target “undruggable proteins” involved in neurodegenerative disorders and cancer. The Tepe lab is one of the first to explore the enhancement of the 20S proteasome by natural products and synthetic scaffold to induce protein degradation. As part of this effort, the Tepe lab has developed a range of new heterocyclic reactions to synthesize complex marine sponge metabolites and their drug-like derivatives. The drug-like derivatives are subsequently interrogated for their clinical significance in vitro, cell culture and animal models in the lab. In 2006, he founded the biotech company, TCH Pharmaceuticals, Ann Arbor, MI. From 2006-2012, the translational clinical efficacy of his academic drug discovery efforts was further explored by the company, where he served as Vice President of Research. In collaboration with Dr. Yuzbasiyan-Gurkan, one of the compounds is currently examined in a canine trial for hematological cancers at MSU’s Veterinary School, as a proof-of-concept study for possible future human development. For his academic drug discovery efforts, he received the American Cancer Research Scholar award, the Senior Award from the Multiple Myeloma Research Foundation in 2008 and 2010, and the International Myeloma Senior Award in 2013 and 2019. He is currently a faculty member in the Department of Chemistry, Pharmacology & Toxicology at MSU.

A. Positions and Awards

  • International Myeloma Foundation Award, 2019
  • International Myeloma Foundation Award, 2013
  • Multiple Myeloma Research Foundation, Senior Award, 2010
  • Multiple Myeloma Research Foundation, Senior Award, 2008
  • American Cancer Society Research Scholar Award, 2003-2008
  • Teacher-Scholar Award, CNS, Michigan State University, 2005
  • Petroleum Research Fund Award, American Chemical Society, 2002
  • Alfred Burger Fellowship, Senior Thesis Fellowship, University of Virginia, 1997
  • Dean’s Reserve Fellowship, University of Virginia, 1994

POSITIONS

2019 Guest Editor, Molecules, Special Issue on Proteasome Regulators
2018- present Editorial board member, Molecules
2017-present Faculty, Department of Pharmacology & Toxicology, MSU
2016 External reviewer of NIDDK, Bioorganic Chemistry laboratory.
2016-present Member NIH-T32 steering committee (Integrative Pharmacological Sciences Training Program)
2016-present Mentor NIH-T32 (Integrative Pharmacological Sciences Training Program)
2016 Ad Hoc member, MMRF grant review committee
2015 Ad Hoc member, MMRF grant review committee
2013-2016 Mentor NIH-T34 MARC (for underrepresented students in biomedical sciences)
2006-2015 Editorial board member, Current Bioactive Compounds
2006-present Associate Professor of Chemistry, Michigan State University
2006-2012 Vice President of Research, TCH Pharmaceuticals Inc, Ann Arbor, MI
2009-2010 Guest Editor, Current Organic Synthesis, Special Issue: Cycloaddition Reactions
2007-2008 Guest Editor, Current Bioactive Compounds, Special Issue: Anti-cancer Therapies
2006 Co-Founder, TCH Pharmaceuticals Inc, Ann Arbor, MI
2005-present Ad Hoc member, NIH study sections
2004-2005 Chair, Local Section American Chemical Society
2004-2005 Scientific Consultant, Valent Technologies
2003-2005 Scientific Consultant, ChemGenex Therapeutics
2000-2006 Assistant Professor of Chemistry, Michigan State University
1998-2000 Post-doctoral associate with Prof. Robert M. Williams
1992-1998 Graduate student with Prof. Timothy L. Macdonald

 

PROFESSIONAL ACTIVITIES

2006-2012 Co-Founder & Vice President of Research, TCH Pharmaceuticals Inc, Ann Arbor, MI

 

NIH Study Sections:

2019: February BST-55 (High Throughput Screening)
2018: June BST-55 (High Throughput Screening)
2016: November BCMB-G (Biological Chemistry and Macromolecular Biophysics)
2015: November CDDT (Cancer Drug Development and Therapeutics)
2015: March NCI Omnibus Review (Drug Development and Targeting)
2014: October SBCB (Synthetic and Biological Chemistry B)
2014: March CDDT (Cancer Drug Development and Therapeutics)
2013: November CDDT (Cancer Drug Development and Therapeutics)
2010: March FO4A (Synthetic and Biological Chemistry Fellowships)
2009: August BCMB (Biological Chemistry and Macromolecular Biophysics)
2008: March F04A (Synthetic and Biological Chemistry Fellowships)
2006: July F04A (Synthetic and Biological Chemistry Fellowships)
2005: November F04A (Synthetic and Biological Chemistry Fellowships)
2005: July F04A (Synthetic and Biological Chemistry Fellowships)

 

Symposium/Conference organizer/chair:

2016 Section Chair: Medchem. & CADD conference Phoenix, Arizona
2015 Ad-Hoc Advisory Board Member of 2nd Annual Drug Discovery Congress.
2014 Section Chair: MedChem. & CADD conference San Francisco, California.
2012 Co-Organizer: Symposium University of Virginia, Dedication to Prof. T. Macdonald. Articles published in special issue of Bioorganic and Medicinal Chemistry Letters, 2012 issue 22.
2004 Section Chair: Gordon Conference Heterocyclic Chemistry.

 

Ad hoc reviewer:

Grants: NIH, NSF, PRF, Wellcome Trust Fund, US Civilian Research & Development Foundation. Journals: Science Reports, Journal of the American Chemical Society, Nature protocols, ACS Chemical Biology, ACS MedChem., ACS Nano, ACS Omega, ACS Neurochemical Science, Journal of Medicinal Chemistry, Organic Letters, Journal of Organic Chemistry, European Journal of Organic Chemistry, European Journal of Medicinal Chemistry, ChemMedChem, PlosOne, Bioorganic & Medicinal Chemistry Letters, Bioorganic & Medicinal Chemistry, Journal of Combinatorial Chemistry, Science Advances, Australian Journal of Chemistry, Molecules, Tetrahedron, Tetrahedron Letters, Current Bioactive Compounds, Current Organic Synthesis, Synthesis, SynLett.

 

Research group:

Former student: 15 students received PhD degrees

                              6 students received MS degrees

                              3 post-doctoral students

                              2 sabbatical visits for associate professor

                             23 undergraduate researchers

Current students: 9 graduate students (PhD track)

 

PUBLICATIONS

  1. Mehedi, Md Shafaat Al and Tepe, Jetze J. Sc(OTf)3 mediated one pot synthesis of 2,3-disubstituted quinolines from anilines and epoxides, J. Org. Chem. 2020, 85, 6741-6746. DOI:10.1021/acs.joc.0c00803

Sc(OTf)3 mediated one pot synthesis of 2,3-disubstituted quinolines from anilines and epoxides

  1. Njomen, Evert; Lansdell, Theresa A.; Vanecek, Allison, Benham, V. ; Krieger-Burke, Teresa; Bernard, Matthew; Yang Ya-Ting; Alkharabsheh, Omar; Al-Janadi, Anas; Bailie, Marc; Taylor, Catherine; Lau, Sarah; Bernard, Jamie; Yuzbasiayan-Gurkan, V. and Tepe, Jetze J. 20S Proteasome enhancement targets the intrinsically disordered c-MYC and induces in vivo anti-tumor efficacy, 2020, submitted.
  2. Jones, Corey and Tepe, Jetze. Proteasome Activation to Combat Proteotoxicity, Molecules, 2019, 24, 2841. PMID 31387243  DOI: 10.3390/molecules24152841
    1. Special Issue: Proteasome Regulators: Activators and Inhibitors
  3. Njomen, Evert and Tepe, Jetze. Regulation of Autophagic Flux by the 20S proteasome. Cell, Chemical Biology, 2019, 26, 1283-1294. PMID31327703 DOI: 10.1016/j.chembiol.2019.07.002
  4. Njomen, Evert and Tepe, Jetze J. Proteasome activation as a new therapeutic approach to target proteotoxic disorders, Journal of Medicinal Chemistry, 2019, 62, 6469-6481. PMID: 30839208. DOI: 10.1021/acs.jmedchem.9b00101
    1. Article recommended by F1000Prime

Proteasome activation as a new therapeutic approach to target proteotoxic disorders

  1. Mehedi, Md Shafaat Al and Tepe, Jetze J. Diastereoselective one-pot synthesis of oxazolines using sulfur ylides and acyl imines, Journal of Organic Chemistry, 2019, 84, 7219-7226. PMID: 31117573. DOI: 10.1021/acs.joc.9b00883

Diastereoselective one-pot synthesis of oxazolines using sulfur ylides and acyl imines

  1. Giletto, Matthew B; Osmulski, Pawel A.; Jones, Corey L.; Gaczynska Marie E. and Tepe, Jetze J. Pipecolic esters as new templates for proteasome inhibition, Organic & Biomolecular Chemistry, 2019, 17, 2734-2746. PMID: 30778435. DOI: 10.1039/c9ob00122k
  2. Gao, Shuang, Bethel, Travis K. Kakeshpour T.; Hubbell, Grace E., Jackson, James, E. and Tepe, Jetze J. Substrate Controlled Regioselective Bromination of 2-Aycl Pyrroles Using Tetrabutyl Ammonium Tribromide (TBABr3), Journal of Organic Chemistry, 2018, 83, 9250-9255. PMID: 29969032. DOI: 10.1021/acs.joc.8b01251

Substrate Controlled Regioselective Bromination of 2-Aycl Pyrroles Using Tetrabutyl Ammonium Tribromide (TBABr3)

  1. Njomen, Evert; Osmulski, Pawel A.; Jones, Corey L; Lansdell, Theresa A. Gaczynska, Maria E. and Tepe, Jetze J. Small Molecule Modulation of Proteasome Assembly, Biochemistry 2018, 57,4214-4224. PMID: 29897236. DOI: 10.1021/acs.biochem.8b00579
    1. Article recommended by F1000Prime

Small Molecule Modulation of Proteasome Assembly

  1. Jones, Corey L.; Njomen, Evert; Sjogren B.; Dexheimer, Thomas S. and Tepe, Jetze J. Small molecule enhancement of 20S proteasome activity targets intrinsically disordered proteins, ACS Chemical Biology 2017, 15, 2240-2247. PMID: 28719185. DOI: 10.1021/acschembio.7b00489

Small molecule enhancement of 20S proteasome activity targets intrinsically disordered proteins

  1. McDaniel, Tanner J.; Lansdell, Theresa A.; Dissanayake, Amila A.; Azevedo, Lauren M.; Claes, Jacob; Odom, Aaron L. and Tepe, Jetze J. Substituted quinolines as noncovalent proteasome inhibitors, Bioorganic and Medicinal Chemistry, 2016, 24, 2441-2450. PMID: 27112450. DOI: 10.1016/j.bmc.2016.04.005

Substituted quinolines as noncovalent proteasome inhibitor

  1. Zaib, Rahman S. and Tepe, Jetze J. A concise total synthesis of hymenialdisine, Tetrahedron Letters, 2015, 56, 3011-3013. DOI: 10.1016/j.tetlet.2014.10.022
    1. Article selected for: Special Issue dedicated to Prof. H. Wasserman.

A concise total synthesis of hymenialdisine

  1. Kuszpit, Michael R.; Giletto, Matthew B.; Jones, Corey L.; Bethel, Travis K. and Tepe, Jetze J. Hydroxyamination of olefins using Br-N-(CO2Me)2. Journal of Organic Chemistry, 2015, 80, 1440-1445. PMID: 25574949. DOI: 10.1021/jo502369d

Hydroxyamination of olefins using Br-N-(CO2Me)2

  1. Beck, Philipp; Lansdell, Theresa A.; Hewlett, Nicole M.; Tepe, Jetze J. and Groll, Michael. Indolo-phakellins as b5-specific noncovalent proteasome inhibitors, Angewandte Chemie International Edition, 2015, 54, 2830-2833. PMID: 25581903. DOI: 10.1002/anie.201410168
    1. Article highlighted by editors as: Hot Paper.
  2. Basson, Marc D.; Zeng B; Downey C; Siriveluprabhakara S, Tepe, Jetze J. Increased extracellular pressure stimulates tumor proliferation by a mechanosensitive calcium channel and PKC-b, Molecular Oncology, 2015, 9, 513-526. PMC: 4487881. DOI: 10.1016/j.molonc.2014.10.008
  3. Hewlett, Nicole M. and Tepe, Jetze J. 2-Phenyl oxazolone, Electronic Encyclopedia of Reagents for Organic Synthesis, 2014, 1-3. DOI: 10.1002/047084289X.rn01743
  4. Azevedo, Lauren M.; Lansdell, Theresa A.; Ludwig, Jacob R.; Mosey, R. Adam; Woloch, Daljinder K.; Cogan, Dillon P.; Patten, Gregory P.; Kuszpit, Michael R.; Fisk, Jason S. and Tepe, Jetze J. Inhibition of the human proteasome by imidazoline scaffolds, Journal of Medicinal Chemistry, 2013, 56, 5974-5978. PMC: 3844044. DOI: 10.1021/jm400235r
    1. Article Highlighted in Science Business Exchange SciBX 6(28), July 25, 2013

Inhibition of the human proteasome by imidazoline scaffolds

  1. Lansdell, Theresa A.; Hurchla, Michelle A.; Xiang, J.; Hovde, S.; Weilbaecher, Katherine N.; Henry, R. William; Tepe, Jetze J. Noncompetitive modulation of the proteasome by imidazoline scaffolds overcomes bortezomib resistance and delays MM tumor growth in vivo, ACS Chemical Biology, 2013, 8, 578-587. PMC: 3600058. DOI: 10.1021/cb300568r
    1. Article Highlighted: ACS Chemical Biology editors highlight article from Volume 8, Issue 3 and speak with author Jetze Tepe on itunes podcast, March 2013.
    2. Article recommended by F1000Prime

Noncompetitive modulation of the proteasome by imidazoline scaffolds overcomes bortezomib resistance and delays MM tumor growth in vivo

  1. Nguyen, Thu N.T.; Saleem, Rahman S. Z.; Luderer, Micah, J.; Tepe, Jetze J. Radioprotection by hymenialdisine-derived checkpoint kinase 2 inhibitors, ACS Chemical Biology, 2012, 7, 172-184. PMID: 22004065. DOI: 10.1021/cb200320c

Radioprotection by hymenialdisine-derived checkpoint kinase 2 inhibitors

  1. Lansdell, Theresa A.; O'Reilly, Sandra; Woolliscroft, Tracey; Azevedo, Lauren M.; Kahlon, Daljinder K.; Hovde, Stacy; McCormick, J. Justin; Henry, R. William; Cornicelli, Joseph A.; Tepe, Jetze J. Non-competitive inhibition of the human proteasome attenuates collagen-induced arthritis, Bioorganic & Medicinal Chemistry Letters, 2012, 22, 4816-4819.  PMID: 22682057. DOI: 10.1016/j.bmcl.2012.05.056

Non-competitive inhibition of the human proteasome attenuates collagen-induced arthritis

  1. Lansdell, Theresa A.; Hewlett, Nicole M.; Skoumbourdis, Amanda P.; Fodor, Matthew D.; Seiple, Ian B.; Su, Shun; Baran, Phil. S.; Feldman, Ken S.; Tepe, Jetze J. Palau’amine and Related Oroidin-alkaloids Dibromophakellin and Dibromophakellstatin Inhibit the Human 20S Proteasome. Journal of Natural Products, 2012, 75, 980-985.  PMC: 3367325. DOI: 10.1021/np300231f
    1. Article recommended by F1000Prime, 17 Jul 2018; F1000Prime.com/717748071

Palau’amine and Related Oroidin-alkaloids Dibromophakellin and Dibromophakellstatin Inhibit the Human 20S Proteasome

  1. Saleem, Rahman Shah Zaib; Lansdell, Theresa A.; Tepe, Jetze J. Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors, Bioorganic & Medicinal Chemistry, 2012, 20, 1475-1481. PMID: 20481587. DOI: 10.1016/j.bmc.2011.12.054

Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors

  1. Hewlett, Nicole M.; Tepe, Jetze J. Total synthesis of the natural product (±)-dibromophakellin and analogues, Organic Letters, 2011, 13, 4550-4553. PMC: 3162990. DOI: 10.1021/ol201741r

Total synthesis of the natural product (±)-dibromophakellin and analogues

  1. Nguyen, T. N. T.; Tepe, Jetze J. Checkpoint kinase inhibitors. Current Medicinal Chemistry, 2011, 18, 4368-4374. DOI: 10.2174/092986711797200390
  2. Qu, Ke; Fisk, Jason S.; Tepe, Jetze J. Azomethine ylide mediated inversion of configuration of quaternary imidazoline carbon: converting trans- to its cis- imidazolines, Tetrahedron Letters, 2011, 52, 4840-4842. PMC: 3157035. DOI: 10.1016/j.tetlet.2011.07.022

Azomethine ylide mediated inversion of configuration of quaternary imidazoline carbon: converting trans- to its cis- imidazolines

  1. Frawley Cass, Samantha M.; Tepe, Jetze J.  Identification of phosphoproteins and their impact as biomarkers in cancer therapeutics,   Current Signal Transduction Therapy, 2011, 6, 113-140. DOI: 10.2174/157436211794109389
  2. Kuszpit, Michael R.; Wulff, William D.; Tepe, Jetze J. One-Pot Synthesis of 2-Imidazolines via the Ring Expansion of Imidoyl Chlorides with Aziridines,  Journal of Organic Chemistry, 2011, 76, 2913-2919. PMC: 3074022. DOI: 10.1021/jo200101q

One-Pot Synthesis of 2-Imidazolines via the Ring Expansion of Imidoyl Chlorides with Aziridines

  1. Saleem, Rahman Shah Zaib; Tepe, Jetze J. Synthesis of 1,2,4-triazolines and triazoles utilizing oxazolones,  Journal of Organic Chemistry, 2010, 75, 4330-4332. DOI: 10.1021/jo100716m
    1. Article highlighted in Synfacts 2010, 0997.

Synthesis of 1,2,4-triazolines and triazoles utilizing oxazolones

  1. Tepe, Jetze J. Recent advances in cycloaddition reactions in natural product synthesis, Current Organic Synthesis, 2010,7, 311. DOI: 10.2174/157017910791414481
  2. Wang, Wei-Han; Palumbo, Amanda M.; Tan, Yu-Jing; Reid, Gavin E.; Tepe, Jetze J.; Bruening, Merlin L. Identification of p65-Associated Phosphoproteins by Mass Spectrometry after On-Plate Phosphopeptide Enrichment Using Polymer-oxotitanium Films, Journal of Proteomic Research, 2010, 9, 3005-3015. DOI: 10.1021/pr901200m

Identification of p65-Associated Phosphoproteins by Mass Spectrometry after On-Plate Phosphopeptide Enrichment Using Polymer-oxotitanium Films

  1. Hupp, Christopher D.; Tepe, Jetze J. 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide Hydrochloride-Mediated Oxazole Rearrangement: Gaining Access to a Unique Marine Alkaloid Scaffold, Journal of Organic Chemistry, 2009, 74, 3406-3413. DOI: 10.1021/jo900264p

1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide Hydrochloride-Mediated Oxazole Rearrangement: Gaining Access to a Unique Marine Alkaloid Scaffold

  1. Frawley Cass, Samantha M.; Reid, Gavin E.; Tepe, Jetze J. Synthesis of diazo ketone solid supports and their application towards the enrichment of phosphorylated peptides, Organic and Biomolecular Chemistry, 2009, 7, 3291-3299. DOI: 10.1039/b906577f

Synthesis of diazo ketone solid supports and their application towards the enrichment of phosphorylated peptides,

  1. Hewlett, N. M.; Hupp, C. D.; Tepe, J. J. Reactivity of oxazol-5-(4H)-ones and their application toward natural product synthesis, Synthesis, 2009, 17, 2825-2839. DOI: 10.1055/s-0029-1216924
  2. Nguyen, T. N. T.; Tepe, Jetze J. Preparation of hymenialdisine, analogs and their evaluation as kinase inhibitors, Current Medicinal Chemistry, 2009, 16, 3122-3143. DOI: 10.2174/092986709788803015
  3. Tepe, Jetze J. Natural Product Inspired Small Molecular Scaffolds in Anticancer Therapy, Current Bioactive Compounds, 2009, 5, 1. DOI: 10.2174/157340709787580883
  4. Kahlon, Daljinder K.; Lansdell, Theresa A.; Fisk, Jason S.; Tepe, Jetze J. Structural activity relationship of functionalized trans-imidazolines as potent inhibitors of interleukin-6 production, Bioorganic & Medicinal Chemistry, 2009, 17, 3093-3103. DOI: 10.1016/j.bmc.2009.03.002

Structural activity relationship of functionalized trans-imidazolines as potent inhibitors of interleukin-6 production

  1. Mosey, Robert A.; Tepe, Jetze J. New Synthetic Route to Access (±) Salinosporamide A via an Oxazolone Mediated Ene-type reaction, Tetrahedron Letters, 2009, 50, 295-297. DOI: 10.1016/j.tetlet.2008.10.154

New Synthetic Route to Access (±) Salinosporamide A via an Oxazolone Mediated Ene-type reaction

  1. Kahlon, Daljinder K.; Lansdell, Theresa A.; Fisk, Jason S.; Hupp, Christopher D.; Friebe, Timothy L.; Hovde, Stacy; Jones, A. Daniel; Dyer, Richard D.; Henry, R. William; Tepe, Jetze J. Nuclear Factor-κB Mediated Inhibition of Cytokine Production by Imidazoline Scaffolds, Journal of Medicinal Chemistry, 2009, 52, 1302-1309. PMID: 19220017 DOI: 10.1021/jm8013162
    1. Article highlighted in: Science-Business eXchange 2009, 2, 18.

Nuclear Factor-κB Mediated Inhibition of Cytokine Production by Imidazoline Scaffolds

  1. Hupp, Christopher D.; Tepe, Jetze J., Total synthesis of a marine alkaloid from the Tunicate Dendrodoa grossularia, Organic Letters, 2008, 10, 3737-3739. PMID: 18680306 DOI: 10.1021/ol801375k

Total synthesis of a marine alkaloid from the Tunicate Dendrodoa grossularia

  1. Mosey, Robert A.; Tepe, Jetze J. Stereocontrolled synthesis of quaternary substituted amino acids using oxazolones, Tetrahedron Asymmetry, 2008, 19, 2755-2762. DOI: 10.1016/j.tetasy.2008.11.033

Stereocontrolled synthesis of quaternary substituted amino acids using oxazolones

  1. Mosey, Robert A.; Fisk, Jason S.; Friebe, Timothy L.; Tepe, Jetze J. Synthesis of tert-Alkyl Amino Hydroxy Carboxylic Esters via an Intermolecular Ene-type Reaction of Oxazolones and Enol Ethers, Organic Letters, 2008, 10, 825-828. PMID: 18232699 DOI: 10.1021/ol702941f

Synthesis of tert-Alkyl Amino Hydroxy Carboxylic Esters via an Intermolecular Ene-type Reaction of Oxazolones and Enol Ethers

  1. Palumbo, Amanda M.; Tepe, Jetze J.; Reid, Gavin E. Mechanistic Insights into the Multistage Gas-Phase Fragmentation Behavior of Phosphoserine- and Phosphothreonine-Containing Peptides, Journal of Proteomic Research, 2008, 7, 771-779. PMID: 18181561 DOI: 10.1021/pr0705136

Mechanistic Insights into the Multistage Gas-Phase Fragmentation Behavior of Phosphoserine- and Phosphothreonine-Containing Peptides

  1. Fisk, Jason S.; Tepe, Jetze J. Intermolecular Ene Reactions Utilizing Oxazolones and Enol Ethers, Journal of the American Chemical Society, 2007, 129, 3058-3059. PMID: 17326632 DOI: 10.1021/ja0627904

Intermolecular Ene Reactions Utilizing Oxazolones and Enol Ethers

  1. Fisk, Jason S.; Mosey, Robert A.; Tepe, Jetze J. The Diverse Chemistry of Azlactones, Chemistry Society Reviews, 2007, 36, 1432-1440. PMID: 17660876 DOI: 10.1039/b511113g

The Diverse Chemistry of Azlactones

  1. Sharma, Vasudha; Hupp, Christopher D.; Tepe, Jetze J. Enhancement of Chemotherapeutic Efficacy by Small Molecule Inhibition of NF-kB and Checkpoint Kinases, Current Medicinal Chemistry, 2007, 14, 1061-1074. PMID: 17456020 DOI: 10.2174/092986707780362844
  2. Sharma, Vasudha; Peddibhotla, Satyamaheshwar; Tepe, Jetze J. Sensitization of Cancer Cells to DNA Damaging Agents by Imidazolines, Journal of the American Chemical Society,  2006, 128, 9137-9143. PMID: 16834387 DOI: 10.1021/ja060273f

Sensitization of Cancer Cells to DNA Damaging Agents by Imidazolines

 

  1. Sharma, Vasudha; Tepe, Jetze J. Diastereochemical Diversity of Imidazoline Scaffolds via Substrate Controlled TMSCl Mediated Cycloaddition of Azlactones, Organic Letters, 2005, 7, 5091-5094. PMID: 16235965 DOI: 10.1021/ol052118w

Diastereochemical Diversity of Imidazoline Scaffolds via Substrate Controlled TMSCl Mediated Cycloaddition of Azlactones

  1. Keni, Manasi; Tepe, Jetze J. One-pot Friedel-Crafts/Robinson-Gabriel Synthesis of Oxazoles Using Oxazolone Templates, Journal of Organic Chemistry, 2005, 70, 4211-4213. PMID: 15876123 DOI: 10.1021/jo0501590

ne-pot Friedel-Crafts/Robinson-Gabriel Synthesis of Oxazoles Using Oxazolone Templates

  1. Sharma, Vasudha; Lansdell, Theresa A.; Peddibhotla, Satyamaheshwar; Tepe, Jetze J. Sensitization of Tumor Cells towards Chemotherapy: Enhancing the Efficacy of Camptothecin by Novel Imidazolines, Chemistry & Biology, 2004, 11, 1689-1699. PMID: 15610853 DOI: 10.1016/j.chembiol.2004.10.006
  2. Peddibhotla, Satyamaheshwar; Tepe, Jetze J. Stereoselective Synthesis of Highly Substituted D1-Pyrrolines: Exo Selective 1,3- Dipolar Cycloaddition Reactions with Azlactones, Journal of the American Chemical Society, 2004, 126, 12776-12777. PMID: 15469263 DOI: 10.1021/ja046149i

Stereoselective Synthesis of Highly Substituted D1-Pyrrolines: Exo Selective 1,3- Dipolar Cycloaddition Reactions with Azlactones

  1. Sharma, Vasudha; Tepe, Jetze J. Potent Inhibition of Checkpoint Kinase Activity by a Hymenialdisine-derived Indoloazepine, Bioorganic & Medicinal Chemistry Letters, 2004, 14, 4319-4321. PMID: 15261294 DOI: 10.1016/j.bmcl.2004.05.079

Potent Inhibition of Checkpoint Kinase Activity by a Hymenialdisine-derived Indoloazepine

  1. Sharma, Vasudha; Lansdell, Theresa A.; Jin, Guangyi; Tepe, Jetze J. Inhibition of Cytokine Production by Hymenialdisine Derivatives, Journal of Medicinal Chemistry, 2004, 47, 3700-3703.  PMID: 15214798 DOI: 10.1021/jm040013d

 

Inhibition of Cytokine Production by Hymenialdisine Derivatives

  1. Lansdell, Theresa A.; Tepe, Jetze J. Isolation of Phosphopeptides using Solid Phase Enrichment, Tetrahedron Letters, 2004, 45, 91-93. DOI: 10.1016/j.tetlet.2003.10.111

Isolation of Phosphopeptides using Solid Phase Enrichment

  1. Peddibhotla, S.; Tepe, Jetze J. Multicomponent Synthesis of Highly Substituted Imidazolines via a Silicon Mediated 1,3-Dipolar Cycloaddition, Synthesis, 2003, 9, 1433-1440. DOI: 10.1055/s-2003-40196
  2. Peddibhotla, Satyamaheshwar; Cheng, Zigang; DellaPenna, Dean; Tepe, Jetze J. Efficient Two-step Synthesis of Methylphytylbenzoquinones: Precursor Intermediates in the Biosynthesis of Vitamin E. Tetrahedron Letters, 2003, 44, 237-239. DOI: 10.1016/S0040-4039(02)02564-9
  3. Anderson, Kevin W.; Tepe, Jetze J. Trifluorosulfonic Acid Catalyzed Friedel-Crafts Acylation of Aromatics with β-Lactams. Tetrahedron, 2002, 58, 8475-8481. DOI: 10.1016/S0040-4020(02)01026-8

Trifluorosulfonic Acid Catalyzed Friedel-Crafts Acylation of Aromatics with β-Lactams

  1. Peddibhotla, Satymaheshwar; Jayakumar, S.; Tepe, Jetze J. Highly Diastereoselective Multicomponent Synthesis of Unsymmetrical Imidazoline Scaffolds, Organic Letters, 2002, 4, 3533-3535. PMID: 12323062 DOI: 10.1021/ol026703y

 

Highly Diastereoselective Multicomponent Synthesis of Unsymmetrical Imidazoline Scaffolds

  1. Anderson, Kevin W.; Tepe, Jetze J. First Intermolecular Friedel-Crafts Acylations with β-Lactams, Organic Letters, 2002, 4, 459-461. PMID: 11820904 DOI: 10.1021/ol010291w

irst Intermolecular Friedel-Crafts Acylations with β-Lactams

 

 

PRIOR TO INDEPENDENT CAREE

  1. J.J. Tepe, C. Kosogof, and R.M. Williams. DNA Interstrand Cross-link Formation by Reductive Activation of Dehydropyrrolizidine Progenitors, Tetrahedron, 2002, 58, 3553-3559.
  2. L. Beckenbauer, J.J. Tepe, R. A. Eastman, P. Mixter, R. M. Williams and R. Reeves. Vascular Leak Syndrome and Drug Design: Insights from FR900482 and FK317, Chemistry & Biology, 2002, 9, 427-441.
  3. C. Kosogof, J. J. Tepe and R. M. Williams. DNA Cross-linking by a Phototriggered Pyrrolic Progenitor developed from Monocrotaline, Tetrahedron Letters, 2001, 42, 6641-6643.
  4. L. Beckenbauer, J. J. Tepe, J. Cullison, R. Reeves and R. M. Williams. FR900482 Class of Anti-Tumor Drugs Cross-links Oncoprotein HMG I/Y to DNA in vivo, Chemistry & Biology, 2000, 7, 805-812.
  5. J.J. Tepe and R.M. Williams. Reductive Activation of a Hydroxylamino Hemi-acetal Derivative of Dehydro -monocrotaline. DNA Cross-linking Studies, Angewandte Chemie International Edition, 1999, 38,3501-3503.
  6. J.J. Tepe and R. M. Williams, DNA Cross-linking of a Photoactivated Dehydro- monocrotaline Progenitor, Journal of the American Chemical Society, 1999, 224, 2450-2456.
  7. M.A. Labroli, T. L. Macdonald, and J. J. Tepe; DNA Topoisomerase II Inhibitors, In: Comprehensive Natural Products Chemistry, E.T. Kool, ed., Elsevier-North Holland, Amsterdam, The Netherlands, Chap. 19, 1997.
  8. J.S. Madalengoitia, J. J. Tepe, K. A. Werbovetz, E. K. Lehnert and T. L. Macdonald. Structure-Activity Relationship for DNA Topoisomerase II Induced DNA Cleavage by Azatoxin Analogs, Bioorganic & Medicinal Chemistry, 1997, 5, 1807-1815. [LINK]
  9. J.J. Tepe, J. S. Madalengoitia, K. Miller Slunt, K. W. Werbovetz, P. Grant Spoors and T. L. Macdonald. Inhibition of DNA Topoisomerase II by Aza-elliptitoxins Functionalyzed in the Variable Substituent Domain, Journal of Medicinal Chemistry, 1996, 39, 2188-2196.

 

 

US and WO patents (grouped per general area):

  1. US 2018-62623861A1 Pipecolic esters for inhibition of the proteasome, Jan. 30, 2019
  2. US 2018/0282280A1 Quinoline-based proteasome inhibitors and uses thereof, Oct. 4, 2018.
  3. US 62/539,049. Treatment of malignancies. July 31, 2018
  4. US 62/515,403. Enhancement of proteasome activity for the treatment of neurodegenerative diseases. June 5, 2018
  5. US Provisional patent 62/479,805. Quinoline-based proteasome inhibitors. March 31, 2017
  6. US 8,552,206 B2. and European Patent: 03731545.4. NF-kB inhibitors and uses thereof. Oct. 8, 2013
  7. US 8,252,942 B2. Substituted imidazoline compounds. Aug. 12, 2012
  8. US 7,193,079 B1. Preparation of hymendialdisine derivates and use thereof. March 20, 2007
  9. US 6,878,735 B2. Multi-substituted imidazolines and method of use thereof. April 12, 2005

INVITED SEMINARS at:

  1. Weizmann Institute of Science, 1st conference on 20S proteasome degradation, Israel (Feb. 21, 2021)
  2. Purdue University, Department of Medicinal Chemistry & Molecular pharmacology (March 5th, 2020)
  3. International Myeloma Foundation, Award Ceremony, San Diego, California (December 1, 2018)
  4. Breslin Cancer Institute, Lansing, MI (November 12th, 2018)
  5. 16th Annual Discovery on Target, Boston, MA (September 25th, 2018)
  6. Michigan State University, Cisplatin Symposium, East Lansing (August 3rd, 2018)
  7. Wayne State University, Drug Discovery Symposium (October 14, 2017)
  8. Keynote lecture at MedChem & CADD 2016, Phoenix, Arizona (December 2016)
  9. Michigan State University, Department of Pediatrics and Human Development (April 6, 2016)
  10. Sparrow Cancer Center, Lansing, Michigan (March 21, 2016)
  11. Lemmon-Holton Cancer Pavilion, Spectrum Health, Grand Rapids, Michigan (January 13, 2016)
  12. MedChem & CADD 2015, Atlanta, (November 2th, 2015)
  13. Drug Discovery & Therapy, World Congress 2015, Boston, Massachusetts (July 24th, 2015)
  14. Drug Discovery Seminar Series, MSU Pharmacology & Toxicology (January 16th, 2015)
  15. MedChem & CADD 2014, San Francisco, (December 8th, 2014)
  16. Drug Discovery USA, Boston Massachusetts (Oct. 21, 2014)
  17. University of Pittsburgh, Department of Pharmaceutical Sciences (September 16, 2014)
  18. Fusion Conference, Drug Discovery Re-invented, Scottsdale, Arizona (October 16th, 2013)
  19. MedChem & CADD 2013, Las Vegas, Nevada (October 15th, 2013)
  20. Colorado State University, Williams Symposium (September 28th, 2013)
  21. Drug Discovery & Therapy, World Congress 2013, Boston, Massachusetts (June 6th, 2013)
  22. University of Illinois at Chicago (Nov. 27th, 2012)
  23. Latest Trends in Organic Synthesis, Ontario CAN (August 12th, 2012)
  24. University of Virginia, Macdonald Symposium (April 27th, 2012)
  25. Washington University, School of Medicine (May 5th, 2011)
  26. Michigan State University, Pharmacology and Toxicology (January 12, 2011)
  27. Butler University (March 26th, 2010)
  28. National Institutes of Health, (October 2, 2009)
  29. University of Minnesota (July 1, 2009)
  30. CERMAC, Symposium on Chemical Biology (March 20-23, 2009)
  31. Wayne State University (February 18th, 2009)
  32. BioFine USA, Life Science Conference, Fl (December 2nd, 2008)
  33. University of Utah, (October 9th, 2008)
  34. Breslin Cancer Institute (January 18th, 2008)
  35. MSU, Breast Cancer Group (Oct. 5th, 2007)
  36. Andrews University (March 1st, 2007)
  37. Central Michigan University (September 25, 2006)
  38. Michigan State University, Carcinogenesis (September 19, 2006)
  39. Michigan 21st Century Job Fund (August 15, 2006)
  40. Case Western University (January 19, 2006)
  41. University of Pittsburg (November 3, 2005)
  42. Chamber of Commerce Japan, Seminar Tour with Governor Granholm (July 25)
  43. Kyowa Hakko Co, Japan (July 24, 2005)
  44. Gordon conference, Heterocyclic Chemistry (July 6, 2005)
  45. SUNY at Buffalo/Roswell Cancer Institute (May 16, 2005)
  46. Colorado State University (May 3, 2005)
  47. Scripps Research Institute (May 2, 2005)
  48. University of California at Riverside (April 29, 2005)
  49. University of California at San Diego (April 28, 2005)
  50. University of Maryland (March 31, 2005)
  51. University of Delaware (March 17, 2005)
  52. Pennsylvania State University (March 14, 2005)
  53. SUNY at Buffalo (March 9, 2005)
  54. University of Florida, Heterocyclic Conf. (February 27 -March 2, 2005)
  55. Indiana University (November 29, 2004)
  56. Michigan State University-Frontiers in Science (December 10, 2004)
  57. University of Vermont (November 19, 2004)
  58. University of Wisconsin-Madison (November 12, 2004)
  59. Northwestern University (November 11, 2004)
  60. Colgate University (October 12, 2004)
  61. Wayne State University (October 6, 2004)
  62. Michigan State University-MSU Foundation (May 26, 2004)
  63. American Cancer Society- opening ceremony “Rely-for-Life” Waterloo, IN (May 15)
  64. NIH/NCI- Division of Drug Development (February, 13, 2004)
  65. Oakland University (January 21,2004)
  66. 19th International Congress of Heterocyclic Chemistry (August 10-15, 2003)
  67. Ohio State University (February 27, 2003)
  68. Cleveland State University (April 11, 2002)
  69. Eastern Michigan University (March 27, 2001)
  70. St. Clouds University (March 4, 2001)

CURRENT RESEARCH SUPPORT

NIH R01 AG066223-01A1 (PI, Tepe) 09/15/19-05/31/23
       Title: Small molecule induced proteolytic destruction of intrinsically disordered proteins

NIH-IGNITE 1R61NS111347-01A1 (PI, Tepe) 12/01/19-11/31/22
       Title: Development of cellular HTS for 20S proteasome enhancers

NIH R21 AG061306-01 (PI, Tepe) 12/01/19-11/31/21
       Title: Multiparameter optimization of new phenothiazines for proteasome activation

International Myeloma Foundation (PI, Tepe) 01/01/19-12/31/19
       Title: Targeting c-Myc degradation to treat myeloma

Previous Research support

NIH 1R21AI117018-01A1 (PI, Abramovitch, Co-PI Tepe) 08/20/16-07/31/19
Title: Non-competitive proteasome inhibitors to treat chronic, drug-resistant tuberculosis

MSU Discretionary Funding Initiative (PI, Tepe) 04/17/18 – 4/16/19
Title: Redesigning phenothiazine as proteasome activators for the treatment of neurodegenerative diseases

MTRAC- Michigan Translational Research and Commercialization (co-PI Tepe) 11/05/17– 10/30/19
Title: Development of new treatments for canine histiocytic sarcomas

CTSI - Clinical and Translational Science Institute (PI, Tepe) 04/15/18 - 04/14/19
Title: Proof-of-concept studies for a new approach to treat neurodegenerative diseases

MSU- Molecule Discovery Grant pilot program (co-PI, Tepe) 03/03/18 - 03/02/19
Title: Exploration of viability of proteasome inhibitors with alternative mechanisms

NIH 1R01GM110195-01 (PI, Neubig, Co-I/Tepe) 04/01/14 - 03/31/18
Title: Small molecule stabilizers of RGS protein expression

Strategic Partnership Grant 14-SPG-2966 (PI, Abramovitch, Co-PI Tepe) 06/01/15 - 05/31/18
Title: Non-competitive proteasome inhibitors to treat chronic, drug-resistant tuberculosis

SPG-CNS match S14-SPG-2966 (PI, Tepe) 06/01/15 - 05/31/18
Title: Non-competitive proteasome inhibitors to treat chronic, drug-resistant tuberculosis

MSU- Molecule Discovery Grant pilot program (PI, Tepe) 03/03/17 - 03/02/18
Title: Development of drug-like TCH-165 derivatives

MSU- Clinical and Translational Science Institute (PI, Tepe) 03/03/17 - 03/02/18
Title: Evaluation of the translational effect of tCH-165 and derivatives on non-responsive and relapsing MM patient samples

MTRAC- Michigan Translational Research and Commercialization (PI, Yuzbasiyan-Gurkan) 12/30/16 - 12/29/17
Title: Development of new treatments for canine histiocytic sarcomas

NIH 1R21CA182926--02 (PI, Tepe) 02/11/14 - 01/31/16
Title: Characterization of non-competitive proteasome binding

International Myeloma Foundation (PI, Tepe) 01/02/13 - 01/01/14
Title: Validation of non-competitive proteasome modulation for multiple myeloma

NIH 1R01CA142644-01 (PI, Tepe) 04/01/10 - 03/31/14
Title: Inhibition of interleukin-6 production for the treatment of multiple myeloma

Multiple Myeloma Research Foundation, Senior Award (PI, Tepe) 05/15/10 - 04/14/12
Title: Development of allosteric proteasome inhibitors for the treatment of MM

MIIE Award (PI, Tepe) 07/01/09 - 06/30/10
Title: Pre-clinical development of non-covalent proteasome inhibitors for the treatment of multiple myeloma.

Multiple Myeloma Research Foundation, Senior Award (PI, Tepe) 06/01/08 - 05/30/10
Title: Phosphoproteomic analysis of NF-kappaB in multiple myeloma

NIH R01 GM071549-01 (PI, Tepe) 08/01/04 - 07/30/09
Title: New Methods in Phosphoproteomics

Michigan Universities Commercialization Initiative (PI, Tepe) 10/08/07 - 07/31/09
Title: Advancing a family of orally available NF-kB inhibitors with novel mechanism of action through pre-clinical development

TCH Pharmaceuticals, INC (PI, Tepe) 06/01/06 - 07/31/08
Title: Cellular Activity and Inhibition of NF-kB

Center Grant: Center for Cancer Proteomic (PI, Tepe) 08/16/06 - 10/30/08
Title: Phosphoproteomic analysis of cancer signaling
 
American Cancer society RSG CDD-106972 (PI, Tepe) 01/01/04 - 12/31/08
Title: Chemopotentiation of Anticancer Drugs by Novel Imidazolines
 
Strategic Partnership Grant (PI, Tepe) 06/01/04 - 05/31/07
Title: Enhancement of efficacy of chemotherapeutic drugs