• Publications
  • Influence
Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules.
Biologically active molecules can be identified through the screening of small-molecule libraries. Deficiencies in current compound collections are evidenced by the continuing decline inExpand
  • 362
  • 1
Diversity-oriented synthesis of macrocyclic peptidomimetics
Structurally diverse libraries of novel small molecules represent important sources of biologically active agents. In this paper we report the development of a diversity-oriented synthesis strategyExpand
  • 83
  • PDF
Novel and efficient copper-catalysed synthesis of nitrogen-linked medium-ring biaryls.
Herein, a new copper-catalysed strategy for the synthesis of rare nitrogen-linked seven-, eight- and nine-membered biaryl ring systems is described. It is proposed that the reaction proceeds throughExpand
  • 15
  • PDF
MrgX2 is a promiscuous receptor for basic peptides causing mast cell pseudo‐allergic and anaphylactoid reactions
Activation of MrgX2, an orphan G protein‐coupled receptor expressed on mast cells, leads to degranulation and histamine release. Human MrgX2 binds promiscuously to structurally diverse peptides andExpand
  • 7
Sulfatase-cleavable linkers for antibody-drug conjugates
Antibody-drug conjugates (ADCs) are a class of targeted drug delivery agents combining the cell-selectivity of monoclonal antibodies (mAbs) and the cytotoxicity of small molecules. These twoExpand
  • 3
In Vivo Imaging of Small Molecular Weight Peptides for Targeted Renal Drug Delivery: A Study in Normal and Polycystic Kidney Diseased Mice
Autosomal dominant polycystic kidney disease (ADPKD) is a leading monogenetic cause of end-stage renal disease with limited therapeutic repertoire. A targeted drug delivery strategy that directs aExpand
  • 2
  • PDF
A diversity-oriented synthesis strategy enabling the combinatorial-type variation of macrocyclic peptidomimetic sca ff olds †
Macrocyclic peptidomimetics are associated with a broad range of biological activities. However, despite such potentially valuable properties, the macrocyclic peptidomimetic structural class isExpand
Sulfatase-cleavable linkers for antibody-drug conjugates
Antibody-drug conjugates (ADCs) are a class of targeted drug delivery agents combining the cell-selectivity of monoclonal antibodies (mAbs) and the cytotoxicity of small molecules. These twoExpand
  • 1
  • PDF