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Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554
Bioorganic & Medicinal Chemistry 19: 4953

Maezaki H, Banno Y, Miyamoto Y, Moritoh Y, Asakawa T, Kataoka O, Takeuchi K, Suzuki N, Ikedo K, Kosaka T, Sasaki M, Tsubotani S, Tani A, Funami M, Yamamoto Y, Tawada M, Aertgeerts K, Yano J, Oi S (2011)
Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554
Bioorganic & Medicinal Chemistry 19: 4482

Miyamoto Y, Banno Y, Yamashita T, Fujimoto T, Oi S, Moritoh Y, Asakawa T, Kataoka O, Takeuchi K, Suzuki N, Ikedo K, Kosaka T, Tsubotani S, Tani A, Funami M, Amano M, Yamamoto Y, Aertgeerts K, Yano J, Maezaki H (2011)
Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125
Bioorganic & Medicinal Chemistry 19: 172

Miyamoto Y, Banno Y, Yamashita T, Fujimoto T, Oi S, Moritoh Y, Asakawa T, Kataoka O, Yashiro H, Takeuchi K, Suzuki N, Ikedo K, Kosaka T, Tsubotani S, Tani A, Sasaki M, Funami M, Amano M, Yamamoto Y, Aertgeerts K, Yano J, Maezaki H (2011)
Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor
Journal of Medicinal Chemistry 54: 831

Zhang Z, Wallace MB, Feng J, Stafford JA, Skene RJ, Shi L, Lee B, Aertgeerts K, Jennings A, Xu R, Kassel DB, Kaldor SW, Navre M, Webb DR, Gwaltney SL (2011)
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV
Journal of Medicinal Chemistry 54: 510

Aertgeerts K, Levin I, Shi L, Snell GP, Jennings A, Prasad GS, Zhang Y, Kraus ML, Salakian S, Sridhar V, Wijnands R, Tennant MG (2005)
Structural and kinetic analysis of the substrate specificity of human fibroblast activation protein alpha
Journal of Biological Chemistry 280: 19441

Aertgeerts K, Ye S, Shi L, Prasad SG, Witmer D, Chi E, Sang BC, Wijnands RA, Webb DR, Swanson RV (2004)
N-linked glycosylation of dipeptidyl peptidase IV (CD26): effects on enzyme activity, homodimer formation, and adenosine deaminase binding
Protein Science 13: 145

Aertgeerts K, Ye S, Tennant MG, Kraus ML, Rogers J, Sang BC, Skene RJ, Webb DR, Prasad GS (2004)
Crystal structure of human dipeptidyl peptidase IV in complex with a decapeptide reveals details on substrate specificity and tetrahedral intermediate formation
Protein Science 13: 412