Research ArticleArticle
Metabolites of PPI-2458, a Selective, Irreversible Inhibitor of Methionine Aminopeptidase-2: Structure Determination and In Vivo Activity
Christopher C. Arico-Muendel, Bruce Belanger, Dennis Benjamin, Heather S. Blanchette, Teresa M. Caiazzo, Paolo A. Centrella, Jennifer DeLorey, Elisabeth G. Doyle, Ulrike Gradhand, Sarah T. Griffin, Susan Hill, Matthew T. Labenski, Barry A. Morgan, Gary O’Donovan, Kavirayani Prasad, Steven Skinner, Nazbeh Taghizadeh, Charles D. Thompson, James Wakefield, William Westlin and Kerry F. White
Drug Metabolism and Disposition April 2013, 41 (4) 814-826; DOI: https://doi.org/10.1124/dmd.112.048355
Christopher C. Arico-Muendel
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Bruce Belanger
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Dennis Benjamin
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Heather S. Blanchette
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Teresa M. Caiazzo
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Paolo A. Centrella
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Jennifer DeLorey
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Elisabeth G. Doyle
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Ulrike Gradhand
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Sarah T. Griffin
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Susan Hill
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Matthew T. Labenski
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Barry A. Morgan
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Gary O’Donovan
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Kavirayani Prasad
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Steven Skinner
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Nazbeh Taghizadeh
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Charles D. Thompson
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
James Wakefield
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
William Westlin
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
Kerry F. White
GlaxoSmithKline, Waltham, Massachusetts (C.C.A.-M., G.O., S.S.); Merrimack Pharmaceuticals, Cambridge, Massachusetts (B.B.); Seattle Genetics, Inc., Bothell, Washington (D.B.); Cubist Pharmaceuticals, Lexington, Massachusetts (H.B.); Pfizer Inc., Andover, Massachusetts (T.M.C.); X-Chem, Inc., Waltham, Massachusetts (P.A.C.); Vertex Pharmaceuticals, Cambridge, Massachusetts (E.G.D.); Chemical Research and Development, Pfizer, Inc., Groton, Connecticut (S.T.G.); Merck, Boston, Massachusetts (S.H.); Celgene Avilomics Research, Bedford, Massachusetts (M.T.L.); Department of Organic Chemistry, Indian Institute of Science, Bangalore, India (K.P.); Brigham and Women’s Hospital, Newton, Massachusetts (N.T.); Merck & Company, Inc., West Point, Pennsylvania (C.D.T.); Ironwood Pharmaceuticals, Cambridge, Massachusetts (J.W.); Infinity Pharmaceuticals, Cambridge, Massachusetts (K.F.W.); Praecis Pharmaceuticals, Inc., Waltham, Massachusetts (C.C.A.-M., B.B., D.B., H.S.B., T.M.C., P.A.C., J.D., E.G.D., U.G., S.T.G., S.H., M.T.L., B.A.M., G.O., K.P., S.S., N.T., C.D.T., J.W., W.W., K.F.W.)
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Active Metabolites of PPI-2458, A Selective MetAP2 Inhibitor
Christopher C. Arico-Muendel, Bruce Belanger, Dennis Benjamin, Heather S. Blanchette, Teresa M. Caiazzo, Paolo A. Centrella, Jennifer DeLorey, Elisabeth G. Doyle, Ulrike Gradhand, Sarah T. Griffin, Susan Hill, Matthew T. Labenski, Barry A. Morgan, Gary O’Donovan, Kavirayani Prasad, Steven Skinner, Nazbeh Taghizadeh, Charles D. Thompson, James Wakefield, William Westlin and Kerry F. White
Drug Metabolism and Disposition April 1, 2013, 41 (4) 814-826; DOI: https://doi.org/10.1124/dmd.112.048355
Research ArticleArticle
Active Metabolites of PPI-2458, A Selective MetAP2 Inhibitor
Christopher C. Arico-Muendel, Bruce Belanger, Dennis Benjamin, Heather S. Blanchette, Teresa M. Caiazzo, Paolo A. Centrella, Jennifer DeLorey, Elisabeth G. Doyle, Ulrike Gradhand, Sarah T. Griffin, Susan Hill, Matthew T. Labenski, Barry A. Morgan, Gary O’Donovan, Kavirayani Prasad, Steven Skinner, Nazbeh Taghizadeh, Charles D. Thompson, James Wakefield, William Westlin and Kerry F. White
Drug Metabolism and Disposition April 1, 2013, 41 (4) 814-826; DOI: https://doi.org/10.1124/dmd.112.048355
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