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29 Results  for Everything (Includes Articles)

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The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties

Siu, Tony ; Brubaker, Jason ; Fuller, Peter ; Torres, Luis ; Zeng, Hongbo ; Close, Joshua ; Mampreian, Dawn M ; Shi, Feng ; Liu, Duan ; Fradera, Xavier ; Johnson, Kevin ; Bays, Nathan ; Kadic, Elma ; He, Fang ; Goldenblatt, Peter ; Shaffer, Lynsey ; Patel, Sangita B ; Lesburg, Charles A ; Alpert, Carla ; Dorosh

Journal of medicinal chemistry, 14 December 2017, Vol.60(23), pp.9676-9690 [Peer Reviewed Journal]

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Discovery of 1-3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo4,5cyclohepta1,2-bpyridin-7-yl-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met

Northrup, Alan B ; Katcher, Matthew H ; Altman, Michael D ; Chenard, Melissa ; Daniels, Matthew H ; Deshmukh, Sujal V ; Falcone, Danielle ; Guerin, David J ; Hatch, Harold ; Li, Chaomin ; Lu, Wei ; Lutterbach, Bart ; Allison, Timothy J ; Patel, Sangita B ; Reilly, John F ; Reutershan, Michael ; Rickert, Keith W ; Rosenstein, Craig ; Soisson, Stephen M ; Szewczak

Journal of medicinal chemistry, 28 March 2013, Vol.56(6), pp.2294-310 [Peer Reviewed Journal]

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Structural basis of human p70 ribosomal S6 kinase-1 regulation by activation loop phosphorylation

Sunami, Tomoko ; Byrne, Noel ; Diehl, Ronald E ; Funabashi, Kaoru ; Hall, Dawn L ; Ikuta, Mari ; Patel, Sangita B ; Shipman, Jennifer M ; Smith, Robert F ; Takahashi, Ikuko ; Zugay-Murphy, Joan ; Iwasawa, Yoshikazu ; Lumb, Kevin J ; Munshi, Sanjeev K ; Sharma, Sujata

The Journal of biological chemistry, 12 February 2010, Vol.285(7), pp.4587-94 [Peer Reviewed Journal]

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Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors

Simov, Vladimir ; Deshmukh, Sujal V ; Dinsmore, Christopher J ; Elwood, Fiona ; Fernandez, Rafael B ; Garcia, Yudith ; Gibeau, Craig ; Gunaydin, Hakan ; Jung, Joon ; Katz, Jason D ; Kraybill, Brian ; Lapointe, Blair ; Patel, Sangita B ; Siu, Tony ; Su, Hua ; Young, Jonathan R

Bioorganic & Medicinal Chemistry Letters, 01 April 2016, Vol.26(7), pp.1803-1808 [Peer Reviewed Journal]

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Structure of the bacterial deacetylase LpxC bound to the nucleotide reaction product reveals mechanisms of oxyanion stabilization and proton transfer

Clayton, Gina M ; Klein, Daniel J ; Rickert, Keith W ; Patel, Sangita B ; Kornienko, Maria ; Zugay-Murphy, Joan ; Reid, John C ; Tummala, Srivanya ; Sharma, Sujata ; Singh, Sheo B ; Miesel, Lynn ; Lumb, Kevin J ; Soisson, Stephen M

The Journal of biological chemistry, 22 November 2013, Vol.288(47), pp.34073-80 [Peer Reviewed Journal]

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Structural definition and substrate specificity of the S28 protease family: the crystal structure of human prolylcarboxypeptidase

Rickert Keith W ; Reid John C ; Ford Rachael E ; Hall Dawn L ; Diehl Ronald E ; Byrne Noel J ; Abeywickrema Pravien D ; Patel Sangita B ; Soisson Stephen M ; Shipman Jennifer M ; Sharma Sujata ; Lumb Kevin J

BMC Structural Biology, 01 June 2010, Vol.10(1), p.16 [Peer Reviewed Journal]

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Crystal structure of human phosphodiesterase 3B: atomic basis for substrate and inhibitor specificity

Scapin, Giovanna ; Patel, Sangita B ; Chung, Christine ; Varnerin, Jeffrey P ; Edmondson, Scott D ; Mastracchio, Anthony ; Parmee, Emma R ; Singh, Suresh B ; Becker, Joseph W ; Van Der Ploeg, Lex H T ; Tota, Michael R

Biochemistry, 25 May 2004, Vol.43(20), pp.6091-100 [Peer Reviewed Journal]

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Synthesis and Evaluation of Heterocyclic Catechol Mimics as Inhibitors of Catechol-O-methyltransferase (COMT)

Harrison, Scott T ; Poslusney, Michael S ; Mulhearn, James J ; Zhao, Zhijian ; Kett, Nathan R ; Schubert, Jeffrey W ; Melamed, Jeffrey Y ; Allison, Timothy J ; Patel, Sangita B ; Sanders, John M ; Sharma, Sujata ; Smith, Robert F ; Hall, Dawn L ; Robinson, Ronald G ; Sachs, Nancy A ; Hutson, Pete H ; Wolkenberg, Scott E ; Barrow, James C

ACS medicinal chemistry letters, 12 March 2015, Vol.6(3), pp.318-23 [Peer Reviewed Journal]

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Structural basis for selective small molecule kinase inhibition of activated c-Met

Rickert, Keith W ; Patel, Sangita B ; Allison, Timothy J ; Byrne, Noel J ; Darke, Paul L ; Ford, Rachael E ; Guerin, David J ; Hall, Dawn L ; Kornienko, Maria ; Lu, Jun ; Munshi, Sanjeev K ; Reid, John C ; Shipman, Jennifer M ; Stanton, Elizabeth F ; Wilson, Kevin J ; Young, Jonathon R ; Soisson, Stephen M ; Lumb, Kevin J

The Journal of biological chemistry, 01 April 2011, Vol.286(13), pp.11218-25 [Peer Reviewed Journal]

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The three‐dimensional structure of MAP kinase p38β: different features of the ATP‐binding site in p38β compared with p38α

Patel, Sangita B. ; Cameron, Patricia M. ; O' Keefe, Stephen J. ; Frantz‐Wattley, Betsy ; Thompson, Jed ; O' Neill, Edward A. ; Tennis, Trevor ; Liu, Luping ; Becker, Joseph W. ; Scapin, Giovanna

Acta Crystallographica Section D, 01 August 2009, Vol.65(8), pp.777-785 [Peer Reviewed Journal]

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Expression, purification and crystallization of human prolylcarboxypeptidase

Abeywickrema, Pravien D. ; Patel, Sangita B. ; Byrne, Noel J. ; Diehl, Ronald E. ; Hall, Dawn L. ; Ford, Rachael E. ; Rickert, Keith W. ; Reid, John C. ; Shipman, Jennifer M. ; Geissler, Wayne M. ; Pryor, Kelly D. ; Sinharoy, Ranabir ; Soisson, Stephen M. ; Lumb, Kevin J. ; Sharma, Sujata

Acta Crystallographica Section F, 01 June 2010, Vol.66(6), pp.702-705 [Peer Reviewed Journal]

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12
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Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines

Kim, Dooseop ; Kowalchick, Jennifer E ; Brockunier, Linda L ; Parmee, Emma R ; Eiermann, George J ; Fisher, Michael H ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn ; Scapin, Giovanna ; Patel, Sangita B ; Petrov, Aleksandr ; Pryor, Kellyann D ; Roy, Ranabir Sinha ; Wu, Joseph K ; Zhang, Xiaoping ; Wyvratt, Matthew J ; Zhang, Bei B ; Zhu, Lan ; Thornberry

Journal of medicinal chemistry, 14 February 2008, Vol.51(3), pp.589-602 [Peer Reviewed Journal]

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13
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The structural basis for the selectivity of benzotriazole inhibitors of PTP1B

Scapin, Giovanna ; Patel, Sangita B ; Becker, Joseph W ; Wang, Qingping ; Desponts, Caroline ; Waddleton, Deena ; Skorey, Kathryn ; Cromlish, Wanda ; Bayly, Christopher ; Therien, Michel ; Gauthier, Jacques Yves ; Li, Chun Sing ; Lau, Cheuk K ; Ramachandran, Chidambaram ; Kennedy, Brian P ; Asante-Appiah, Ernest

Biochemistry, 07 October 2003, Vol.42(39), pp.11451-9 [Peer Reviewed Journal]

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14
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(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-1,2,4triazolo1,5-a-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

Edmondson, Scott D ; Mastracchio, Anthony ; Mathvink, Robert J ; He, Jiafang ; Harper, Bart ; Park, You-Jung ; Beconi, Maria ; Di Salvo, Jerry ; Eiermann, George J ; He, Huaibing ; Leiting, Barbara ; Leone, Joseph F ; Levorse, Dorothy A ; Lyons, Kathryn ; Patel, Reshma A ; Patel, Sangita B ; Petrov, Aleksandr ; Scapin, Giovanna ; Shang, Jackie ; Roy

Journal of medicinal chemistry, 15 June 2006, Vol.49(12), pp.3614-27 [Peer Reviewed Journal]

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15
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(2R)-4-oxo-4-3-(trifluoromethyl)-5,6-dihydro1,2,4triazolo4,3-apyrazin-7(8H)-yl-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

Kim, Dooseop ; Wang, Liping ; Beconi, Maria ; Eiermann, George J ; Fisher, Michael H ; He, Huaibing ; Hickey, Gerard J ; Kowalchick, Jennifer E ; Leiting, Barbara ; Lyons, Kathryn ; Marsilio, Frank ; Mccann, Margaret E ; Patel, Reshma A ; Petrov, Aleksandr ; Scapin, Giovanna ; Patel, Sangita B ; Roy, Ranabir Sinha ; Wu, Joseph K ; Wyvratt, Matthew J ; Zhang

Journal of medicinal chemistry, 13 January 2005, Vol.48(1), pp.141-51 [Peer Reviewed Journal]

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Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

Lu, Jun ; Byrne, Noel ; Wang, John ; Bricogne, Gerard ; Brown, Frank K ; Chobanian, Harry R ; Colletti, Steven L ; Di Salvo, Jerry ; Thomas-Fowlkes, Brande ; Guo, Yan ; Hall, Dawn L ; Hadix, Jennifer ; Hastings, Nicholas B ; Hermes, Jeffrey D ; Ho, Thu ; Howard, Andrew D ; Josien, Hubert ; Kornienko, Maria ; Lumb, Kevin J ; Miller

Nature structural & molecular biology, July 2017, Vol.24(7), pp.570-577 [Peer Reviewed Journal]

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17
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Discovery of a 5H-benzo4,5cyclohepta1,2-bpyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer

Katz, Jason D ; Jewell, James P ; Guerin, David J ; Lim, Jongwon ; Dinsmore, Christopher J ; Deshmukh, Sujal V ; Pan, Bo-Sheng ; Marshall, C Gary ; Lu, Wei ; Altman, Michael D ; Dahlberg, William K ; Davis, Lenora ; Falcone, Danielle ; Gabarda, Ana E ; Hang, Gaozhen ; Hatch, Harold ; Holmes, Rachael ; Kunii, Kaiko ; Lumb, Kevin J ; Lutterbach

Journal of medicinal chemistry, 23 June 2011, Vol.54(12), pp.4092-108 [Peer Reviewed Journal]

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18
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Lattice stabilization and enhanced diffraction in human p38α crystals by protein engineering

Patel, Sangita B ; Cameron, Patricia M ; Frantz-Wattley, Betsy ; O'Neill, Edward ; Becker, Joseph W ; Scapin, Giovanna

BBA - Proteins and Proteomics, 2004, Vol.1696(1), pp.67-73 [Peer Reviewed Journal]

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Crystallization and preliminary X‐ray diffraction analysis of the catalytic domain of recombinant human phosphodiesterase 3B

Patel, Sangita B. ; Varnerin, Jeffrey P. ; Tota, Michael R. ; Edmondson, Scott D. ; Parmee, Emma R. ; Becker, Joseph W. ; Scapin, Giovanna

Acta Crystallographica Section D, January 2004, Vol.60(1), pp.169-171 [Peer Reviewed Journal]

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20
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Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors

Edmondson, Scott D ; Mastracchio, Anthony ; Cox, Jason M ; Eiermann, George J ; He, Huaibing ; Lyons, Kathryn A ; Patel, Reshma A ; Patel, Sangita B ; Petrov, Aleksandr ; Scapin, Giovanna ; Wu, Joseph K ; Xu, Shiyao ; Zhu, Bing ; Thornberry, Nancy A ; Roy, Ranabir Sinha ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 01 August 2009, Vol.19(15), pp.4097-4101 [Peer Reviewed Journal]

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21
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Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors

Gao, Ying-Duo ; Feng, Dennis ; Sheridan, Robert P ; Scapin, Giovanna ; Patel, Sangita B ; Wu, Joseph K ; Zhang, Xiaoping ; Sinha-Roy, Ranabir ; Thornberry, Nancy A ; Weber, Ann E ; Biftu, Tesfaye

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(14), pp.3877-3879 [Peer Reviewed Journal]

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22
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Expression, refolding, and purification of recombinant human phosphodiesterase 3B: definition of the N-terminus of the catalytic core

Varnerin, Jeffrey P ; Chung, Christine C ; Patel, Sangita B ; Scapin, Giovanna ; Parmee, Emma R ; Morin, Nancy R ; Macneil, Douglas J ; Cully, Doris F ; Van Der Ploeg, Lex H.T ; Tota, Michael R

Protein Expression and Purification, 2004, Vol.35(2), pp.225-236 [Peer Reviewed Journal]

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23
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Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors

Edmondson, Scott D ; Wei, Lan ; Xu, Jinyou ; Shang, Jackie ; Xu, Shiyao ; Pang, Jianmei ; Chaudhary, Ashok ; Dean, Dennis C ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn A ; Patel, Reshma A ; Patel, Sangita B ; Scapin, Giovanna ; Wu, Joseph K ; Beconi, Maria G ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(7), pp.2409-2413 [Peer Reviewed Journal]

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24
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4-Aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV

Duffy, Joseph L ; Kirk, Brian A ; Wang, Liping ; Eiermann, George J ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn A ; Patel, Reshma A ; Patel, Sangita B ; Petrov, Alexsandr ; Scapin, Giovanna ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(10), pp.2879-2885 [Peer Reviewed Journal]

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25
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4-Arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV

Kaelin, David E ; Smenton, Abigail L ; Eiermann, George J ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn A ; Patel, Reshma A ; Patel, Sangita B ; Petrov, Alexsandr ; Scapin, Giovanna ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E ; Duffy, Joseph L

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(21), pp.5806-5811 [Peer Reviewed Journal]

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26
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Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors

Xu, Jinyou ; Wei, Lan ; Mathvink, Robert J ; Edmondson, Scott D ; Eiermann, George J ; He, Huaibing ; Leone, Joseph F ; Leiting, Barbara ; Lyons, Kathryn A ; Marsilio, Frank ; Patel, Reshma A ; Patel, Sangita B ; Petrov, Aleksandr ; Scapin, Giovanna ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(20), pp.5373-5377 [Peer Reviewed Journal]

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27
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A potent broadly neutralizing human RSV antibody targets conserved site IV of the fusion glycoprotein

Tang, Aimin ; Chen, Zhifeng ; Cox, Kara S ; Su, Hua-Poo ; Callahan, Cheryl ; Fridman, Arthur ; Zhang, Lan ; Patel, Sangita B ; Cejas, Pedro J ; Swoyer, Ryan ; Touch, Sinoeun ; Citron, Michael P ; Govindarajan, Dhanasekaran ; Luo, Bin ; Eddins, Michael ; Reid, John C ; Soisson, Stephen M ; Galli, Jennifer ; Wang, Dai ; Wen

Nature communications, 12 September 2019, Vol.10(1), pp.4153 [Peer Reviewed Journal]

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Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase

Stelmach, John E ; Liu, Luping ; Patel, Sangita B ; Pivnichny, James V ; Scapin, Giovanna ; Singh, Suresh ; Hop, Cornelis E.C.A ; Wang, Zhen ; Strauss, John R ; Cameron, Patricia M ; Nichols, Elizabeth A ; O'Keefe, Stephen J ; O'Neill, Edward A ; Schmatz, Dennis M ; Schwartz, Cheryl D ; Thompson, Chris M ; Zaller, Dennis M ; Doherty, James B

Bioorganic & Medicinal Chemistry Letters, 2003, Vol.13(2), pp.277-280 [Peer Reviewed Journal]

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29
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Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase

Stelmach, John E ; Liu, Luping ; Patel, Sangita B ; Pivnichny, James V ; Scapin, Giovanna ; Singh, Suresh ; Hop, Cornelis E C A ; Wang, Zhen ; Strauss, John R ; Cameron, Patricia M ; Nichols, Elizabeth A ; O'Keefe, Stephen J ; O'Neill, Edward A ; Schmatz, Dennis M ; Schwartz, Cheryl D ; Thompson, Chris M ; Zaller, Dennis M ; Doherty

Bioorganic & medicinal chemistry letters, 20 January 2003, Vol.13(2), pp.277-80 [Peer Reviewed Journal]

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