By Michael J. Haas, Associate Editor
Published on Thursday, December 4, 2014
The first disclosed grant under Merck & Co. Inc.‘s Canadian translational initiative will bolster the ability of macrocycle-based Encycle Therapeutics Inc. to conduct lead optimization of its integrin α4b7 inhibitors for inflammatory bowel disease.
Encycle’s macrocycle platform includes three features not found together in other macrocycle platforms: a lack of sulfur to enhance metabolic stability; inclusion of several intramolecular hydrogen bonds that alter the molecules’ folding and increase their ability to permeate cell membranes; and an upper size limit of three to five amino acids, which gives the molecules better oral availability than larger rings typically achieve.3
Haas, M.J. SciBX 7(46); doi:10.1038/scibx.2014.1338
Published online Dec. 4, 2014
1. Kotz, J. SciBX 5(45); doi:10.1038/scibx.2012.1176
2. Cain, C. BioCentury 20(38) A7-A13 (2012); Sept. 17, 2012
3. Haas, M.J. BioCentury 13; Aug. 4, 2014
COMPANIES AND INSTITUTIONS MENTIONED
AstraZeneca plc (LSE:AZN; NYSE:AZN), London, U.K.
The Centre for Drug Research and Development, Vancouver, British Columbia, Canada
CQDM, Montreal, Quebec, Canada
Encycle Therapeutics Inc., Toronto, Ontario, Canada
GlaxoSmithKline plc (LSE:GSK; NYSE:GSK), London, U.K.
IInstitute for Research in Immunology and Cancer Montreal, Quebec, Canada
Institute for Research in Immunology and Cancer-Commercialization of Research, Montreal, Quebec, Canada
MaRS Innovation, Toronto, Ontario, Canada
Merck & Co. Inc. (NYSE:MRK), Whitehouse Station, N.J.
Pfizer Inc. (NYSE:PFE), New York, N.Y.
Polyphor Ltd., Allschwil, Switzerland
Roswell Park Cancer Institute, Buffalo, N.Y.
University of Montreal, Montreal, Quebec, Canada
University of Toronto, Toronto, Ontario, Canada