Vertex Pharmaceuticals, Inc.

Michael Shin-San Su

Keith P Wilson

Ursula A Germann

Ted Fox

Roger D Tung

Bigin Li

The invention relates to methods for designing inhibitors of serine/threonine kinases and tyrosine kinases, particularly MAP kinases, through the use of ATP-binding site mutants of those kinases. The methods of this invention take advantage of the fact that the mutant kinases are capable of binding inhibitory compounds of other kinases with greater affinity than the corresponding wild-type kinase. The invention further relates to the mutant kinases themselves and crystallizable co-complexes of the mutant kinase and the inhibitory compound.

Methods for designing inhibitors of serine/threonine kinases and tyrosine kinases

This invention relates to the use of butyrate prodrugs derived from lactic acid for treating inflammatory bowel disease. The invention also relates to the use of those prodrugs for the treatment of a chemotherapy-induced mucocutaneous side effect in a patient. The invention further relates to the use of butyrate prodrugs for treating lung, colo-rectal or prostate cancer. And the invention also relates to the use of butyrate prodrugs to treat cystic fibrosis and to enhance the efficiency of gene therapy.

Butyrate prodrugs derived from lactic acid

Methods for designing inhibitors of serine/threonine-kinases and

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Newton, MA, United States of America

Michael Shin-San Su