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Syntex closes Canadian research division.

Syntex Canada closed its research division in Mississauga, ON, in August, eliminating approximately 25 jobs. Some of the research scientists will be transferred to company headquarters in Palo Alto, CA.

The company said it plans to meet its R&D investment objectives by financing work at Canadian universities and hospitals. This is a critical point as the major brand name drug firms had promised to increase R&D spending in Canada in return for extended patent protection.

The move is part of worldwide cutbacks by Syntex. Of its eight manufacturing facilities, four are expected to close. However, it appears that the Mississauga plant will remain open.

The group was headed by Allen Krantz, MCIC, director of research and vice-president, and the current Canadian Society for Chemistry president. (The text which follows was written by Krantz.)

The research group Syntex Canada spent 12 years of discovery research devoted to the design of novel inhibitors of clinically relevant enzymes. The group focused initially on the design of mechanism-based inhibitors, but embraced structure-based strategies and the full gamut of modern drug strategies which have enzymes as targets.

The Canadian team of organic chemists and enzymologists developed drug design motifs, and pursued preparative chemistry, enzymology, molecular biology, and tissue culture studies that were interfaced with biological assays and pharmacokinetic studies carried out in Syntex, Palo Alto, CA.

During the 12-year period over 50 enzymes were investigated in inhibition studies. Flavoenzymes, vitamin [B.sub.6]-dependent enzymes, proteinases in all four subclasses, phospholipases, kinases and transglutaminases, were among the drug targets encompassing numerous therapeutic areas, i.e., inflammation (elastases, cathepsins, matrix metalloproteinases, and phospholipases); cancer (protein typrosine kinase, matrilysin, collagenase IV); acne (transglutaminase).

In particular, the group built a world-wide reputation for its research on the design of proteinase inhibitors, and development of novel inhibitor strategies, demonstrating that a relatively small group of intensely committed and highly focused Canadian scientists could be competitive against much larger pharmaceutical groups. Most recently, its efforts were trained on HIV protease and matrix metalloproteinases, targets for AIDS and inflammation, respectively.

Notable accomplishments include: (1) the first general synthesis of [alpha]-allenyl-[alpha]-amino acids which made available a series of selective and potent inhibitors of specific vitamin [B.sub.6]-dependent enzymes; (2) the novel use of steric effects as a general strategy to block processing of serine acyl enzyme intermediate and hence irreversibly inhibit serine proteinase targets such as elastase; (3) clinical trials of transglutaminase inhibitors as a treatment for acne; (4) the invention of quiescent affinity labels which has essentially revolutionized the affinity label concept. By demonstrating that chemically unreactive groups linked to an appropriate affinity group can be employed in the design of potent and selective inactivators of powerfully nucleophilic cysteine proteinases, the concept of affinity labels was extended beyond the notion of reactive biochemical and pharmacological reagents to include compounds which now hold forth the possibility of practical clinical endpoints.

Syntex Research Canada was a founding and sponsoring member of the Protein Engineering Network of the Federal Centres of Excellence.
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Title Annotation:News Briefs; Syntex Canada
Publication:Canadian Chemical News
Date:Sep 1, 1993
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