Doemling Lab

{SCIENCE} Our interests range from basic questions in chemistry & biology to applied science.

{WE ARE DRUG HUNTERS} We design and discover novel small molecular weight chemotypes for targets in oncology, infection and CNS related diseases. A current major project is the discovery and development of Mdm2 and Mdm4 antagonists for cancer (in collaboration with Tad Holak, Billy Day and others). Methodologically, we employ multicomponent reactions (MCR), medicinal and combinatorial chemistry, design methods and docking. We are developing novel tools for drug discovery, e.g. a novel approach to predict small molecular weight antagonists of protein protein interactions (in collaboration with Carlos Camacho). Our biological targets are related to apoptosis, to the cytoskeleton, the cell membrane and the ribosome. As an academic lab we are keen to prepare tools for moleculer biology, to better understand cellular interrelationsships at an molecular level.
In chemistry we are interested in the advancement of MCRs, e.g. stereoselective variations, novel scaffolds, novel MCRs and chemoinformatic of MCRs.
Our lab is located in the Biomedical Science Tower 3 (BST3) at the University of Pittsburgh, one of the worldwide premium academic centers for basic biomedical research and drug discovery.

Recent Development in Isocyanide Based Multicomponent Reactions in Applied Chemistry
(-)Bacillamide C: The Convergent Approach

First Cocrystal Structure of an Mdmx-p53 Antagonist

The Gewald Multicomponent Reaction

Picture of the Month: Hot spot of the protein-protein interaction p53/mdm2. Dual-action p53/mdm2/mdm4 antagonists “could be used to treat 2,000,000 - 3,000,000 new cancers each year, and so might be the main drugs of tomorrow, assuming that their therapeutic index is acceptable” (F. Toledo, G. M. Wahl. Nat. Rev. Canc. 2006).

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