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Medicinal Chemistry

Our lab develops new chemical methodologies to mimic the diverse structural features found in natural products with the goal to capture their unique biological properties in drug-like scaffolds. Students in the lab with synthesize and test the new scaffolds in order to optimize the natural product mimics for potency, selectivity, cytotoxicity ADME, PK and PD properties. Using a battery of assays, no-go/go decisions will be made along the way as we evaluate the suitability of the compound for further evaluation.  Current programs are focused on novel therapeutics for multiple myelomaneurodegenerative diseases, and tuberculosis.

Some recent representative publications of different compound classes under development in our group are:

  • Substituted quinolines as noncovalent proteasome inhibitors, Bioorganic and Medicinal Chemistry201624, 2441-2450.
  • Inhibition of the human proteasome by imidazoline scaffolds. Journal of Medicinal Chemistry2013, 56, 5974-5978. *Article Highlighted in Science Business Exchange SciBX 6(28),  July 25, 2013
  • Noncompetitive modulation of the proteasome by imidazoline scaffolds overcomes bortezomib resistance and delays MM tumor growth in vivo. ACS Chemical Biology2013, 8, 578-587. *Article Highlighted: ACS Chemical Biology editors highlight article from Volume 8, Issue 3 and speak with author Jetze Tepe on itunes podcast, March 2013.
  • Radioprotection by hymenialdisine-derived checkpoint kinase 2 inhibitors. ACS Chemical Biology 20127, 172-184.
  • Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors. Bioorganic & Medicinal Chemistry 201220, 1475-1481.
  • Non-competitive inhibition of the human proteasome attenuates collagen-induced arthritis. Bioorganic & Medicinal Chemistry Letters 201222, 4816-4819.  
  • Structural activity relationship of functionalized trans-imidazolines as potent inhibitors of interleukin-6 production. Bioorganic & Medicinal Chemistry200917, 3093-3103.
  • Nuclear Factor-κB Mediated Inhibition of Cytokine Production by Imidazoline Scaffolds. Journal of Medicinal Chemistry 200952, 1302-1309. *Article highlighted in: Science-Business eXchange 2009, 2, 18.

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Latest News

May 23, 2022 Very grateful for the NIH's continued support of our work and the funding of our new grant!

Thank you Taylor, Sophie and Allison of all your hard work in helping me put this together and for the data needed to get his funded!

May 22, 2022 Congrats to Rahman Saleem, who was awarded the Vice Chancellors Award for Teaching Excellence at LUMS!

Rahman was selected as one of the five faculty members from Pakistan's leading research intensive university, LUMS, to receive this award. Rahman is currently an Associate Professor at LUMS after getting his PhD from the Tepe lab at MSU in 2011.

Congrats from all of us!

April 19, 2022 Congrats Evert and Allison on your new publication in Biomedicine! Great work.

 Biomedicines 2022, 10, 938. https://doi.org/10.3390/biomedicines10050938

Title: Small molecule 20S proteasome enhancer regulates MYC protein stability and exhibits antitumor activity in multiple myeloma.

April 18, 2022 ...and a big congrats also to Sophie and Corey for their new article in the Journal of Medicinal Chemistry!

Journal of Medicine Chemistry 2022, in print.

Title: "Design, Synthesis and Biological Evaluation of Potent 20S Proteasome Activators for the Potential Treatment of α-synucleinopathies"

More News