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- Publications
- Influence
Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules.
- W. Galloway, Albert Isidro-Llobet, D. Spring
- Biology, Medicine
- Nature communications
- 21 September 2010
Biologically active molecules can be identified through the screening of small-molecule libraries. Deficiencies in current compound collections are evidenced by the continuing decline in… Expand
Diversity-oriented synthesis of macrocyclic peptidomimetics
- Albert Isidro-Llobet, Tiffanie Murillo, +6 authors D. Spring
- Chemistry, Medicine
- Proceedings of the National Academy of Sciences
- 7 March 2011
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 strategy… Expand
Novel and efficient copper-catalysed synthesis of nitrogen-linked medium-ring biaryls.
- Jayne L. Kenwright, W. Galloway, +6 authors D. Spring
- Chemistry, Medicine
- Chemistry
- 1 March 2011
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 through… Expand
MrgX2 is a promiscuous receptor for basic peptides causing mast cell pseudo‐allergic and anaphylactoid reactions
- J. Grimes, S. Desai, +11 authors A. Brown
- Chemistry, Medicine
- Pharmacology research & perspectives
- 1 December 2019
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 and… Expand
Sulfatase-cleavable linkers for antibody-drug conjugates
- Jonathan D Bargh, S. J. Walsh, Albert Isidro-Llobet, S. Omarjee, J. Carroll, David R Spring
- Chemistry
- 5 March 2020
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 two… Expand
In Vivo Imaging of Small Molecular Weight Peptides for Targeted Renal Drug Delivery: A Study in Normal and Polycystic Kidney Diseased Mice
- Steve Lenhard, Allen McAlexander, +13 authors E. Hu
- Medicine
- The Journal of Pharmacology and Experimental…
- 1 September 2019
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 a… Expand
A diversity-oriented synthesis strategy enabling the combinatorial-type variation of macrocyclic peptidomimetic sca ff olds †
- Albert Isidro-Llobet, K. H. Georgiou, +7 authors D. Spring
- 2015
Macrocyclic peptidomimetics are associated with a broad range of biological activities. However, despite such potentially valuable properties, the macrocyclic peptidomimetic structural class is… Expand
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 two… Expand