Seiya Kitamura
Albert Einstein College of Medicine, NY·Chemistry
Finding a small molecule that sticks to a disease-related protein is only the start. Screening large libraries of compounds can turn up initial "hits." But these hits usually need long rounds of medicinal chemistry, the step-by-step redesign of molecules, before they are strong and selective enough to be useful.
- Fields
Chemistry
Pharmacology
Biochemistry
- Topics
chemical biology
medicinal chemistry
chemical probes
- Grants
- 1 known grant, through Jun 2029
What they work on
- Couple the SuFEx click-chemistry high-throughput medicinal chemistry platform with covalent ligands, molecules that bond permanently to proteins, to develop chemical probes for individual underexplored proteins that lack distinct binding sites.
- Extend the SuFEx-based covalent ligand approach proteome-wide, screening across many cellular proteins at once to accelerate probe discovery for poorly characterized targets.
- Develop a SuFEx-enabled synthesis method for extracellular-selective chemical probes, small molecules designed to act only outside the cell.
- Demonstrate approaches to measure organelle-selective target engagement and test whether tuning a molecule's organelle selectivity improves its potency in cells.
More about the research
That bottleneck slows both drug discovery and the making of chemical probes, tool molecules that switch specific proteins on or off so scientists can learn what they do. It is worst for underexplored proteins, many of which lack an obvious pocket for a drug to bind. The research program has two directions. One aims to speed up medicinal chemistry. The other aims to control where in the cell a molecule acts.
Why it matters
Medicinal chemistry is costly and slow, and that delays new medicines. Faster ways to optimize screening hits, together with probes that reach proteins without clear binding sites or act only in one part of the cell, could expand the range of proteins drug developers can target. The resulting probes could reveal how specific proteins contribute to disease and provide proof-of-concept for new therapeutic mechanisms.
Known grants
From NIH and NSF research grants. Labs often have other funding we can't see.
Closest labs
Byoungmoo Kim
Clemson University, SC·Chemistry
Develop one-step, stereospecific and site-selective deoxygenative amination of alcohols, replacing the C–O bond with free amines or nitrogen-containing rings, using a sulfonyl fluoride reagent that reacts through SuFEx click chemistry.
Jaewon Chang
Emory University, GA·Chemistry
Design and synthesize covalent warheads that react with lysine, tyrosine and serine residues on E3 ubiquitin ligases, the enzymes that tag proteins for destruction, going beyond the cysteine-reactive chemistry used so far.
Drew James Adams
Case Western Reserve University, OH·Pharmacology
Determine why small molecules binding the same Cys528 site on Exportin-1 (XPO1), a nuclear transport protein, differ in their effects on nuclear export and cell survival, using structural and functional assays.
The school
Albert Einstein College of Medicine: 21 labs on PI Pages, $361M a year on research, 36 research doctorates a year.
Reach out
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