Strategies to prolong the plasma residence time of
Well established as well as recently developed strategies to prevent the fast clearance of peptide drugs from the circulation are reviewed.
Synthesis and evaluation of phenoxymethylbenzamide analogues as anti-trypanosomal agents
The synthesis of a compound library based on a high throughput screening hit led to the discovery of several potent anti-trypanosomal agents.
Identification of a potent salicylic acid-based
inhibitor of tyrosine phosphatase PTP1B
A screen of a library of diverse small-molecules against a subset of phosphatases identified 7b and 7c, which potently inhibit TC-PTP, PTPσ and PTP1B with no inhibition of PTP-LAR, PRL2 A/S, MKPX or papain.
Exploring the structural determinants of selective phosphopeptide recognition using bivalent metal-coordination complexes
We demonstrate that Lewis acidic coordination complexes equipped with cationic binding groups might be best utilized as selective receptors for binding phosphopeptides with anionic side chain residues proximal to the phosphorylated residue.
Phage display libraries of differently sized bicyclic peptides
Loop length variability in bicyclic peptide libraries increased the diversity of the motifs found in affinity selections towards the tumor-associated protease uPA.
assembly of potent type II dehydroquinase inhibitorsvia “Click” chemistry
The rapid synthesis of a library of potent type II dehydroquinase inhibitors is described. Inhibitors were prepared via a key quinate-derived ene-yne intermediate using Cu(I)-catalysed azide-alkyne cycloaddition (CuAAC) chemistry with a variety of aryl- and heteroaryl-azides.
Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring
Three pairs of regioisomeric 1,2,4- and 1,3,4-oxadiazoles were synthesized as selective CB2 ligands. Although the 1,3,4-oxadiazoles should have better physicochemical and pharmacokinetic properties, their CB2 affinity was reduced.
About this collection
This collection highlights winners of the MedChemComm Emerging Investigator Lectureship. This annual lectureship, established in 2012, recognizes an early-stage career scientist who has made a significant contribution to medicinal chemistry in their early career, particularly if they have brought new ideas to drug discovery.
The winner of 2019 Emerging Investigator Lectureship is Professor Amanda Hargrove, Duke University, USA
2019 Winner Profile
Amanda E. Hargrove, Ph.D. joined the faculty at Duke University in 2013 as an Assistant Professor of Chemistry following an NIH postdoctoral fellowship with Professor Peter B. Dervan at the California Institute of Technology and doctoral research at the University of Texas at Austin with Professors Eric V. Anslyn and Jonathan L. Sessler. Her research group at Duke focuses on developing small molecule probes to investigate the structure and function of RNA molecules relevant to human disease.
Prof. Hargrove holds a secondary appointment in the Biochemistry Department and membership in the Duke Cancer Institute, Duke Cellular and Molecular Biology Program, and the Center for Biological and Tissue Engineering. Her recent honours include the ChemComm Emerging Investigator Lectureship, NSF CAREER Award, Cottrell Scholar Award, and the Prostate Cancer Young Investigator Award.
Winners of the MedChemComm Emerging Investigator Lectureship
2012 Patrick Gunning (University of Toronto, Canada)
2013 Christian Heinis (École Polytechnique Fédérale de Lausanne, Switzerland)
2015 Richard Payne (University of Sydney, Australia)
2016 Alessio Ciulli (University of Dundee, UK)
2017 Laura H. Heitman (Leiden University, Netherlands)
2018 Gonçalo Bernardes (University of Cambridge, UK)