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Themed collection MedChemComm Emerging Investigator Lectureship winners

7 items
Review Article

Strategies to prolong the plasma residence time of peptidedrugs

Well established as well as recently developed strategies to prevent the fast clearance of peptide drugs from the circulation are reviewed.

Graphical abstract: Strategies to prolong the plasma residence time of peptide drugs
Concise Article

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.

Graphical abstract: Synthesis and evaluation of phenoxymethylbenzamide analogues as anti-trypanosomal agents
Concise Article

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.

Graphical abstract: Identification of a potent salicylic acid-based inhibitor of tyrosine phosphatase PTP1B
Concise Article

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.

Graphical abstract: Exploring the structural determinants of selective phosphopeptide recognition using bivalent metal-coordination complexes
Concise Article

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.

Graphical abstract: Phage display libraries of differently sized bicyclic peptides
Concise Article

Rapid 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.

Graphical abstract: Rapid assembly of potent type II dehydroquinase inhibitors via “Click” chemistry
Research Article

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.

Graphical abstract: Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring
7 items

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)

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