Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Robert D, Groneberg"'
Autor:
Darin Smith, Guy Vigers, Sumeet Rana, Michael Burkard, April Cox, Robert D. Groneberg, Ryan J. Watts, Robert Kirk Delisle, Tony Pisal Tang, Andrew T. Metcalf, Kelly Regal, Susan P. Rhodes, Mary K. Geck Do, Karin D. Brown, Joseph P. Lyssikatos, Douglas Mccord Sammond, Matthew Volgraf, Albion D. Wright, Gunawardana Indrani W, Kimberly Scearce-Levie, Jennifer N. Otten, Allen A. Thomas, Michael Siu, Hans E. Purkey, Kevin W. Hunt, Xingrong Liu, Darrin Dutcher
Publikováno v:
Journal of Medicinal Chemistry. 57:878-902
In an attempt to increase selectivity vs Cathepsin D (CatD) in our BACE1 program, a series of 1,3,4,4a,10,10a-hexahydropyrano[4,3-b]chromene analogues was developed. Three different Asp-binding moieties were examined: spirocyclic acyl guanidines, ami
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::936cb574f0793c10f3925c44b16b4302
https://doi.org/10.1021/jm401635n
https://doi.org/10.1021/jm401635n
Autor:
Michael O'sullivan, Kay Brickmann, Peter Bach, Jonas Boström, Darren Martin Harvey, Robert D. Groneberg, J.J.J. van Giezen, Fredrik Zetterberg
Publikováno v:
European Journal of Medicinal Chemistry. 65:360-375
The present paper describes the development of a new series of P2Y12 receptor antagonists based on our previously reported piperazinyl urea series 1 (IC50 binding affinity = 0.33 μM, aq solubility
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b94cca81fda0127b84efce015bc277b8
https://doi.org/10.1016/j.ejmech.2013.04.007
https://doi.org/10.1016/j.ejmech.2013.04.007
Autor:
Michael O'sullivan, Robert D. Groneberg, Mark D. Drew, Andrew Allen, C. Todd Eary, Vivienne Marsh, Devan Balachari, David A. Mareska, Ellen R. Laird, James F. Blake, Zachary Jones, Laurence E. Burgess
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2608-2613
Cholesteryl ester transfer protein is a plasma glycoprotein that transfers cholesterol ester between lipoprotein particles. Inhibition of this protein, in vitro and in vivo, produces an increase in plasma high density lipoprotein cholesterol (HDL-C).
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::729a171e15a026d70339cb61d519bdf9
https://doi.org/10.1016/j.bmcl.2007.01.112
https://doi.org/10.1016/j.bmcl.2007.01.112
Autor:
Burgess Laurence E, Leyla Arik, Chester Chenguang Yuan, Nianhe Han, Randall W. Hungate, Derin C. D'amico, David A. Mareska, Feng-Yin Hsieh, Eileen Johnson, Hong Sun, Qingyian Liu, Barton H. Manning, Bobby Riahi, Christopher H. Fotsch, Gloria Biddlecome, Mark H. Norman, Augustus Kamassah, Ming Huang, Richard Loeloff, Gondi N. Kumar, Andras Toro, Jian J. Chen, Jason Brooks Human, Hideo Suzuki, Robert D. Groneberg, Benny C. Askew, Aiwen Li, Gordon Ng, James Zhan, Kaustav Biswas, Dianna Lester-Zeiner, Hong Dong, David E. Clarke
Publikováno v:
Journal of Medicinal Chemistry. 50:2200-2212
The bradykinin B1 receptor is induced following tissue injury and/or inflammation. Antagonists of this receptor have been studied as promising candidates for treatment of chronic pain. We have identified aryl sulfonamides containing a chiral chroman
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb42b5aad05a1dc5bda8d29f83bc6dc6
https://doi.org/10.1021/jm070055c
https://doi.org/10.1021/jm070055c
Autor:
Jiangpeng Liao, Kelly Regal, Mary K. Geck Do, Kevin W. Hunt, Robert Kirk Delisle, Karin D. Brown, Susan P. Rhodes, Ryan J. Watts, Guy Vigers, Sumeet Rana, Darrin Dutcher, Brad Newhouse, Jennifer N. Otten, Michael Siu, Allen A. Thomas, Darin Smith, April Cox, Michael Burkard, Joseph P. Lyssikatos, Robert D. Groneberg, Xingrong Liu, Hans E. Purkey, Kimberly Scearce-Levie, Albion D. Wright
Publikováno v:
Journal of medicinal chemistry. 57(23)
A series of 2,3,4,4a,10,10a-hexahydropyrano[3,2-b]chromene analogs was developed that demonstrated high selectivity (>2000-fold) for BACE1 vs Cathepsin D (CatD). Three different Asp-binding moieties were examined: spirocyclic acyl guanidines, aminoox
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1cb50753646579b980602888dbffdec3
https://pubmed.ncbi.nlm.nih.gov/25411915
https://pubmed.ncbi.nlm.nih.gov/25411915
Autor:
Andrew T. Metcalf, Allison Marlow, Robert Kirk Delisle, Ryan J. Watts, April Cox, Christopher T. Clark, Kelly Regal, Douglas Mccord Sammond, Kevin W. Hunt, Mary K. Geck Do, Guy Vigers, Sumeet Rana, James P. Rizzi, Tony Pisal Tang, Allen A. Thomas, Nicholas C. Kallan, Xingrong Liu, Adam W. Cook, Michael Siu, Darin Smith, Hans E. Purkey, Gunawardana Indrani W, Darrin Dutcher, Joseph P. Lyssikatos, Michael Burkard, Robert D. Groneberg
Publikováno v:
Journal of medicinal chemistry. 56(8)
A hallmark of Alzheimer's disease is the brain deposition of amyloid beta (Aβ), a peptide of 36-43 amino acids that is likely a primary driver of neurodegeneration. Aβ is produced by the sequential cleavage of APP by BACE1 and γ-secretase; therefo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4993538cb48c85f01cf3f31dd966b90a
https://pubmed.ncbi.nlm.nih.gov/23537249
https://pubmed.ncbi.nlm.nih.gov/23537249
Autor:
Peter, Bach, Jonas, Boström, Kay, Brickmann, J J J, van Giezen, Robert D, Groneberg, Darren M, Harvey, Michael, O'Sullivan, Fredrik, Zetterberg
Publikováno v:
European journal of medicinal chemistry. 65
The present paper describes the development of a new series of P2Y12 receptor antagonists based on our previously reported piperazinyl urea series 1 (IC50 binding affinity = 0.33 μM, aq solubility0.1 μM, microsomal CLint (HLM) ≥300 μM/min/mg). B
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::8fb19daa30b7cb2ccb198999edbc2305
https://pubmed.ncbi.nlm.nih.gov/23747805
https://pubmed.ncbi.nlm.nih.gov/23747805
Autor:
Albion D. Wright, Mark C. Munson, Thomas Pope, Stefan Gross, Pheneger Jed, Robert D. Groneberg, Laurence E. Burgess, Patrice Lee, Corey Custer
Publikováno v:
B35. MUCOSAL IMMUNOLOGY AND INFLAMMATION.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a8f4d9ab2fdf250747d12ab5129317be
https://doi.org/10.1164/ajrccm-conference.2011.183.1_meetingabstracts.a2831
https://doi.org/10.1164/ajrccm-conference.2011.183.1_meetingabstracts.a2831
Autor:
Robert D. Groneberg, Wilhelm Stahl, Adrian L. Smith, Erwin P. Schreiner, T. Miyazaki, N. A. Stylianides, Kyriacos C. Nicolaou, Yoshiharu Iwabuchi, Toshio Suzuki, T. J. Schulze
Publikováno v:
Journal of the American Chemical Society. 115:7593-7611
The first total synthesis of the calicheamicin γ 1 I oligosaccharide fragment in the form of its methyl glycoside (62) has been achieved. The synthetic challenge of the B-ring was recognized and studied initially, resulting in a novel and unique sol
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::63e266b51d816b95a5b8472cb6522478
https://doi.org/10.1021/ja00070a004
https://doi.org/10.1021/ja00070a004
A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core
Autor:
David A. Mareska, Eileen Johnson, Christopher H. Fotsch, Dianna Lester-Zeiner, Qingyian Liu, Gloria Biddlecome, Gordon Ng, James Zhan, Kaustav Biswas, Nianhe Bruce Han, Yueh-Ju Judy Wang, Joe Zhu, Babak Riahi, Gondi N. Kumar, Kevin Yang, Robert D. Groneberg, Derin C. D'amico, Feng-Yin Hsieh, Jian Jeff Chen, Benny C. Askew, Augustus Kamassah
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(8)
The bradykinin 1 (B1) receptor is upregulated during times of inflammation and is important for maintaining inflamed and chronic pain states. Blocking this receptor has been shown to reverse and/or ameliorate pain and inflammation in animal models. I
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5310f114bdf0cdb04629d50164f8f659
https://pubmed.ncbi.nlm.nih.gov/16464576
https://pubmed.ncbi.nlm.nih.gov/16464576