Search Results - "Kirby, Mark S" :: K.UTB vyhledávací portál | TBU Library Retrieval Portal

Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

by Augeri, David J, Robl, Jeffrey A, Betebenner, David A, Magnin, David R, Khanna, Ashish, Robertson, James G, Wang, Aiying, Simpkins, Ligaya M, Taunk, Prakash, Huang, Qi, Han, Song-Ping, Abboa-Offei, Benoni, Cap, Michael, Xin, Li, Tao, Li, Tozzo, Effie, Welzel, Gustav E, Egan, Donald M, Marcinkeviciene, Jovita, Chang, Shu Y, Biller, Scott A, Kirby, Mark S, Parker, Rex A, Hamann, Lawrence G
Published in Journal of medicinal chemistry (28.07.2005)

Get full text

Journal Article

Involvement of DPP‐IV catalytic residues in enzyme–saxagliptin complex formation

Involvement of DPP‐IV catalytic residues in enzyme–saxagliptin complex formation

by Metzler, William J., Yanchunas, Joseph, Weigelt, Carolyn, Kish, Kevin, Klei, Herbert E., Xie, Dianlin, Zhang, Yaqun, Corbett, Martin, Tamura, James K., He, Bin, Hamann, Lawrence G., Kirby, Mark S., Marcinkeviciene, Jovita
Published in Protein science (01.02.2008)

Get full text

Journal Article

Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors

Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors

by Zhao, Guohua, Kwon, Chet, Wang, Aiying, Robertson, James G., Marcinkeviciene, Jovita, Parker, Rex A., Kirby, Mark S., Hamann, Lawrence G.
Published in Bioorganic & medicinal chemistry letters (15.03.2013)

Get full text

Journal Article

Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes

Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes

by Brigance, Robert P., Meng, Wei, Fura, Aberra, Harrity, Thomas, Wang, Aiying, Zahler, Robert, Kirby, Mark S., Hamann, Lawrence G.
Published in Bioorganic & medicinal chemistry letters (01.08.2010)

Get full text

Journal Article

Optimization of Activity, Selectivity, and Liability Profiles in 5‑Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)‑2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo‑5H‑pyrrolo[3,4‑b]pyridin-6(7H)‑yl)‑N,N‑dimethylacetamide (BMS-767778)

Optimization of Activity, Selectivity, and Liability Profiles in 5‑Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)‑2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo‑5H‑pyrrolo[3,4‑b]pyridin-6(7H)‑yl)‑N,N‑dimethylacetamide (BMS-767778)

by Devasthale, Pratik, Wang, Ying, Wang, Wei, Fevig, John, Feng, JianXin, Wang, Aiying, Harrity, Tom, Egan, Don, Morgan, Nathan, Cap, Michael, Fura, Aberra, Klei, Herbert E, Kish, Kevin, Weigelt, Carolyn, Sun, Lucy, Levesque, Paul, Moulin, Frederic, Li, Yi-Xin, Zahler, Robert, Kirby, Mark S, Hamann, Lawrence G
Published in Journal of medicinal chemistry (26.09.2013)

Get full text

Journal Article

Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors

Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors

by Meng, Wei, Brigance, Robert P, Chao, Hannguang J, Fura, Aberra, Harrity, Thomas, Marcinkeviciene, Jovita, O’Connor, Stephen P, Tamura, James K, Xie, Dianlin, Zhang, Yaqun, Klei, Herbert E, Kish, Kevin, Weigelt, Carolyn A, Turdi, Huji, Wang, Aiying, Zahler, Robert, Kirby, Mark S, Hamann, Lawrence G
Published in Journal of medicinal chemistry (12.08.2010)

Get full text

Journal Article

Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

by Wang, Aiying, Dorso, Charles, Kopcho, Lisa, Locke, Gregory, Langish, Robert, Harstad, Eric, Shipkova, Petia, Marcinkeviciene, Jovita, Hamann, Lawrence, Kirby, Mark S
Published in BMC pharmacology (04.04.2012)

Get full text

Journal Article

DPP8 and DPP9 expression in cynomolgus monkey and Sprague Dawley rat tissues

DPP8 and DPP9 expression in cynomolgus monkey and Sprague Dawley rat tissues

by Harstad, Eric. B., Rosenblum, Jonathan S., Gorrell, Mark D., Achanzar, William E., Minimo, Lauro, Wu, Jiangyue, Rosini-Marthaler, Laura, Gullo, Russell, Ordway, Nicole D., Kirby, Mark S., Chadwick, Kristina D., Cosma, Gregory N., Moyer, Carolyn F.
Published in Regulatory peptides (10.09.2013)

Get full text

Journal Article

Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)

Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)

by Kim, Young B., Kopcho, Lisa M., Kirby, Mark S., Hamann, Lawrence G., Weigelt, Carolyn A., Metzler, William J., Marcinkeviciene, Jovita
Published in Archives of biochemistry and biophysics (2006)

Get full text

Journal Article

7-Oxopyrrolopyridine-derived DPP4 inhibitors—mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site

7-Oxopyrrolopyridine-derived DPP4 inhibitors—mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site

by Wang, Wei, Devasthale, Pratik, Wang, Aiying, Harrity, Tom, Egan, Don, Morgan, Nathan, Cap, Michael, Fura, Aberra, Klei, Herbert E., Kish, Kevin, Weigelt, Carolyn, Sun, Lucy, Levesque, Paul, Li, Yi-Xin, Zahler, Robert, Kirby, Mark S., Hamann, Lawrence G.
Published in Bioorganic & medicinal chemistry letters (15.11.2011)

Get full text

Journal Article

Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors

Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors

by O’Connor, Stephen P., Wang, Ying, Simpkins, Ligaya M., Brigance, Robert P., Meng, Wei, Wang, Aiying, Kirby, Mark S., Weigelt, Carolyn A., Hamann, Lawrence G.
Published in Bioorganic & medicinal chemistry letters (01.11.2010)

Get full text

Journal Article

Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors

Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors

by Simpkins, Ligaya M., Bolton, Scott, Pi, Zulan, Sutton, James C., Kwon, Chet, Zhao, Guohua, Magnin, David R., Augeri, David J., Gungor, Timur, Rotella, David P., Sun, Zhong, Liu, Yajun, Slusarchyk, William S., Marcinkeviciene, Jovita, Robertson, James G., Wang, Aiying, Robl, Jeffrey A., Atwal, Karnail S., Zahler, Robert L., Parker, Rex A., Kirby, Mark S., Hamann, Lawrence G.
Published in Bioorganic & medicinal chemistry (01.12.2007)

Get full text

Journal Article

Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors

Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors

by Zhao, Guohua, Taunk, Prakash C., Magnin, David R., Simpkins, Ligaya M., Robl, Jeffrey A., Wang, Aiying, Robertson, James G., Marcinkeviciene, Jovita, Sitkoff, Doree F., Parker, Rex A., Kirby, Mark S., Hamann, Lawrence G.
Published in Bioorganic & medicinal chemistry letters (15.09.2005)

Get full text

Journal Article

Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1

Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1

by Magnin, David R., Taunk, Prakash C., Robertson, James G., Wang, Aiying, Marcinkeviciene, Jovita, Kirby, Mark S., Hamann, Lawrence G.
Published in Bioorganic & medicinal chemistry letters (15.03.2006)

Get full text

Journal Article

Probing prime substrate binding sites of human dipeptidyl peptidase-IV using competitive substrate approach

Probing prime substrate binding sites of human dipeptidyl peptidase-IV using competitive substrate approach

by Kopcho, Lisa M., Kim, Young B., Wang, Aiying, Liu, Margaret A., Kirby, Mark S., Marcinkeviciene, Jovita
Published in Archives of biochemistry and biophysics (15.04.2005)

Get full text

Journal Article

Scorpion toxins targeted against the sarcoplasmic reticulum Ca(2+)-release channel of skeletal and cardiac muscle

Scorpion toxins targeted against the sarcoplasmic reticulum Ca(2+)-release channel of skeletal and cardiac muscle

by Valdivia, H H, Kirby, M S, Lederer, W J, Coronado, R
Published in Proceedings of the National Academy of Sciences - PNAS (15.12.1992)

Get full text

Journal Article

Two-photon-excitation fluorescence imaging of three-dimensional calcium-ion activity

Two-photon-excitation fluorescence imaging of three-dimensional calcium-ion activity

by Piston, D W, Kirby, M S, Cheng, H, Lederer, W J, Webb, W W
Published in Applied optics (2004) (01.02.1994)

Get more information

Journal Article

Optimization of Activity, Selectivity, and Liability Profiles in 5-0xopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichloropheny1)-2-methyl5-oxo-5H-pyrrolo(3,4-b)pyridin-6(7H)-y1)-N,N-dimethylacetamide (BMS-767778)

Optimization of Activity, Selectivity, and Liability Profiles in 5-0xopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichloropheny1)-2-methyl5-oxo-5H-pyrrolo(3,4-b)pyridin-6(7H)-y1)-N,N-dimethylacetamide (BMS-767778)

by Devasthale, Pratik, Wang, Ying, Wang, Wei, Fevig, John, Feng, JianXin, Wang, Aiying, Harrity, Tom, Egan, Don, Morgan, Nathan, Cap, Michael, Fura, Aberra, Klei, Herbert E., Kish, Kevin, Weigelt, Carolyn, Sun, Lucy, Levesque, Paul, Moulin, Frederic, Li, Yi-Xin, Zahler, Robert, Kirby, Mark S., Hamann, Lawrence G.
Published in Journal of medicinal chemistry (26.09.2013)

Get full text

Journal Article

Sodium/calcium exchanger in heart muscle: molecular biology, cellular function, and its special role in excitation-contraction coupling

Sodium/calcium exchanger in heart muscle: molecular biology, cellular function, and its special role in excitation-contraction coupling

by Schulze, Dan, Kofuji, Paulo, Hadley, Robert, Kirby, Mark S, Kieval, Robert S, Doering, Andrea, Niggli, Ernst, Lederer, W J
Published in Cardiovascular research (01.10.1993)

Get full text

Journal Article

Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate ( Sa )-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5 H -pyrrolo[3,4- b ]pyridin-6(7 H )-yl)- N , N -dimethylacetamide (BMS-767778)

Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate ( Sa )-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5 H -pyrrolo[3,4- b ]pyridin-6(7 H )-yl)- N , N -dimethylacetamide (BMS-767778)

by Devasthale, Pratik, Wang, Ying, Wang, Wei, Fevig, John, Feng, JianXin, Wang, Aiying, Harrity, Tom, Egan, Don, Morgan, Nathan, Cap, Michael, Fura, Aberra, Klei, Herbert E., Kish, Kevin, Weigelt, Carolyn, Sun, Lucy, Levesque, Paul, Moulin, Frederic, Li, Yi-Xin, Zahler, Robert, Kirby, Mark S., Hamann, Lawrence G.
Published in Journal of medicinal chemistry (26.09.2013)

Get full text

Journal Article