MIKIW 2019

The first Medicinal Chemistry Meeting-in-Miniature was organized by faculty from the Departments of Medicinal Chemistry and Pharmacognosy at the Universities of University of Minnesota, University of Illinois at Chicago, The University of Kansas, and The University of Iowa in 1963. Since then, the Departments of Medicinal Chemistry and Pharmacognosy at these universities have alternately hosted the MIKI meeting. MIKI is the longest running and largest regional medicinal chemistry meeting in the U.S., and brings together over 200 graduate students, post-doctoral fellows, and faculty members from the four universities on an annual basis. In 2018, the University of Wisconsin-Madison joined MIKI, giving the conference the new name MIKIW. This year, the graduate students at The University of Kansas are excited to host the 57th Annual MIKIW Meeting and continue this great tradition.

Graduate students from the hosting university have the opportunity to organize and moderate the entire meeting, providing the valuable experience of coordinating a professional event. In addition, participating students receive professional experiences by delivering oral and/or poster presentations, as well as vital networking opportunities. Furthermore, these annual meetings also act as a catalyst for sharing and exchanging ideas among students, postdoctoral researchers, and faculty of the different universities. The meeting features a keynote address from a distinguished scientist in academia, industry, or government, who is a leader in the field of medicinal chemistry.

MIKI Founders

MIKIW 2019 Schedule

Friday, April 12, 2019

Saturday, April 13, 2019

* ISB = KU Integrated Science Building

Sunday, April 14, 2019

* ISB = KU Integrated Science Building

"Inhibitors of HIV-1 Maturation"

Nicholas A. Meanwell, Ph.D., FRSC
Dept. of Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development

Abstract: Maturation of the HIV-1 capsid (CA) peptide by HIV-1 protease-mediated cleavage at the CA-SP1 junction is the final step in the formation of infectious virus capsid. A phenotypic screen identified the betulinic acid derivative bevirimat as an inhibitor specific to this step in virion production and this compound demonstrated antiviral effects in Phase 2a clinical trials. However, naturally-occurring polymorphisms proximal to the cleavage site conferred much reduced sensitivity to the effects of bevirimat in vitro which correlated with the clinical response. Guided by assays incorporating the natural polymorphisms, we identified GSK-3532795/BMS-955176 as a second generation HIV-1 maturation inhibitor that exhibits a broader spectrum of antiviral effect in vitro that translated into improved efficacy in clinical trials. In this presentation, we will describe the strategy and tactics adopted by the drug discovery team that led to the discovery of GSK-3532795/BMS-955176, the antiviral and pharmacokinetic profiles of the molecule and the results of early clinical studies.

Acknowledgements

The 57th Annual MIKIW Medicinal Chemistry Meeting would not be possible without the support of the following sponsors. The MIKIW 2019 Organizing Committee and the Department of Medicinal Chemistry at The University of Kansas express our appreciation and sincere gratitude for these generous financial contributions. Thank you to all of the 2019 MIKIW supporters!

Platinum-level Sponsors

• ACS Medicinal Chemistry Division
• Pfizer

Gold-level Sponsors

• KU School of Pharmacy
• Advion
• KU Chemical Biology of Infectious Disease

Silver-level Sponsors

• Waters
• Teledyne ISCO
• Deciphera
• The University of Kansas Cancer Center
• KU Madison & Lila Self Graduate Fellowship
• Biotage
• Vertex
• Corning
• KU Higuchi Bioscience Center
• Journal of Medicinal Chemistry
• Journal of Natural Products
• ACS Medicinal Chemistry Letters
• Abbvie

Bronze-level Sponsors

• Thincnext
• Strem Chemicals, Inc.
• Bristol-Myers Squibb
• Norell
• Avanti Polar Lipids, Inc.
• Orion Bioscience, Inc.
• Sekisui Xenotech
• BioTools
• KU Alumni Association
• New England Biolabs

The previous keynote speakers are among the most accomplished scientists. This group includes Nobel laureates, members of the National Academy of Sciences, leaders in the pharmaceutical industry, and many members of the ACS Medicinal Chemistry Division Hall of Fame. In 2019, we are pleased to have Dr. Nicholas A. Meanwell of Bristol-Myers Squibb deliver the keynote address.

Past Keynote Lectures

For questions about MIKIW 2019, contact KU Medicinal Chemistry at medchem@ku.edu.