Lipopeptides

What do MIT chemistry professors do in their spare time?  Listen to what Dr. Schimmel, a professor of biochemistry and biophysics at MIT from 1967 to 1998 does to pass the time in the following passage.

Since 1997 he has been a professor of Chemical Biology at the Scripps Research Institute.  He is also one of the founders of Repligen Corporation, Alkermes Inc. and  Cubist Pharmaceuticals, Inc. He is a director of all three companies.

LipopeptidesCubist Pharmaceuticals is developing Daptomycin, the first member of a new class of antimicrobial drugs called lipopeptides. In vitro, Daptomycin rapidly kills virtually all Gram-positive bacteria, including notoriously resistant strains, rather than inhibit their growth as do so-called bacteriostatic agents. Bacteriostats rely on the immune system to destroy the bacteria.

As surfactant specialists, we were intrigued by the name lipopeptides.

Glycopeptides have been known as antibiotics, e.g. Vancomycin. They have cyclic peptide structures and biphenyl containing amino acids. Sugars are attached. Glycopeptides inhibit bacterial cell wall formation by binding to its D-alanyl-D-alanine units (Note: Aspartame is L-aspartyl-L-phenylalanine). Other peptide antibiotics are Bleomycin, Dactinomycin and Bacitracin (as an ointment containing Neomycin). Use of peptide antibiotics is limited by toxicities, e.g. to the kidneys and should not be used by morbidly obese people.

Cubist started operations in February 1993, and until December 31, 2000 accumulated a deficit of $ 108.2 million. They have since also gotten involved in Oncogenes.  The apparently successful Daptomycin was licensed from Eli Lilly in November 1997. This raises a number of questions which we will address in the future. Meanwhile further details can be found in the 2000 Annual Report (Form 10-K) of Cubist Pharmaceuticals.

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