Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Tassie L. Collins"'
Autor:
Matthew L. Brown, Jiwen Jim Liu, Michael G. Johnson, Yingcai Wang, Jay Danao, Alison L. Budelsky, Yongli Su, Tassie L. Collins, Bettina Van Lengerich, Tod Martin, Erika Rickel, H Lucy Tang, Lisa Seitz, Wang Shen, An-Rong Li, Julio C. Medina, Xuemei Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1686-1689
Our first generation CRTH2 and DP dual antagonists, represented by AMG 009, are more potent toward the CRTH2 receptor than to the DP receptor. Here we report our efforts in the discovery of CRTH2 and DP dual antagonists with more balanced potencies t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b06929a3e262e7a8d0be964aa900462f
https://doi.org/10.1016/j.bmcl.2011.12.107
https://doi.org/10.1016/j.bmcl.2011.12.107
Autor:
Jason Duquette, Johann Chan, Darin J. Gustin, An-Rong Li, Xiaoqi Chen, Jeff Deignan, Julio C. Medina, Xiaohui Du, George Tonn, Tim Sullivan, Jeffrey T. Mihalic, Bryan Lemon, Kirk Henne, Shichang Miao, Michael Johnson, Zice Fu, Ji Ma, Tassie L. Collins
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:357-362
The optimization of a series of 8-aza-quinazolinone analogs for antagonist activity against the CXCR3 receptor is reported. Compounds were optimized to avoid the formation of active metabolites and time-dependent-inhibitors of CYP3A4. In addition, an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::339aed731e6cb3461777050b365762b1
https://doi.org/10.1016/j.bmcl.2011.10.120
https://doi.org/10.1016/j.bmcl.2011.10.120
Autor:
Zice Fu, Yongli Su, Xuemei Wang, Hua Lucy Tang, Timothy J. Sullivan, Lisa Seitz, Felix Gonzalez-Lopez de Turiso, Julio C. Medina, Mark P. Grillo, Shanna Lawlis, Ying Sun, Wang Shen, M.J. Schmitt, Qiuping Ye, Sarah E. Lively, Matthew L. Brown, An-Rong Li, Yingcai Wang, Bettina Van Lengerich, Jill Wait, Sujen Lai, Jiwen Liu, Michael G. Johnson, Jay Danao, Tassie L. Collins, Qingge Xu
Publikováno v:
ACS Medicinal Chemistry Letters. 2:326-330
Prostaglandin D2 (PGD2) plays a key role in mediating allergic reactions seen in asthma, allergic rhinitis, and atopic dermatitis. PGD2 exerts its activity through two G protein-coupled receptors (GPCRs), prostanoid D receptor (DP or DP1), and chemoa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1412c5f0cb7a55fd9ce712791e8a8c0f
https://doi.org/10.1021/ml1002234
https://doi.org/10.1021/ml1002234
Autor:
Michael Johnson, Zice Fu, Tim Sullivan, Liusheng Zhu, Jay Danao, Andrew P. Marcus, Jiwen Liu, Tassie L. Collins, Julio C. Medina, An-Rong Li, George Tonn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5114-5118
The evaluation of the CXCR3 antagonist AMG 487 in clinic trials was complicated due to the formation of an active metabolite. In this Letter, we will discuss the further optimization of the quinazolinone series that led to the discovery of compounds
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::228e6adf57fa1ccc1f43f109321a1897
https://doi.org/10.1016/j.bmcl.2009.07.032
https://doi.org/10.1016/j.bmcl.2009.07.032
Autor:
Jason Duquette, Emmanuel Sabalan, Ji Ma, Xiaoqi Chen, Shichang Miao, Julio C. Medina, Darin J. Gustin, Zhulun Wang, Lawrence R. McGee, Kirk Henne, Tassie L. Collins, George Tonn, Karen Ebsworth, Tim Sullivan, Xiaohui Du, Bryan Lemon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5200-5204
A general way of improving the potency of CXCR3 antagonists with fused hetero-bicyclic cores was identified. Optimization efforts led to the discovery of a series of imidazo-pyrazine derivatives with improved pharmacokinetic properties in addition to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32b84253576b3d5672e7b511fae6245c
https://doi.org/10.1016/j.bmcl.2009.07.021
https://doi.org/10.1016/j.bmcl.2009.07.021
Autor:
Daniel J. Dairaghi, Qiwei Zhang, Joshua M. Rosenblum, Tassie L. Collins, Robert L. Fairchild, Julio C. Medina, Timothy J. Sullivan, Gerald Siu
Publikováno v:
Transplantation. 87:360-369
Current immunosuppression regimens are toxic to transplant recipients and, in many cases, acute rejection episodes occur because of escape of donor-reactive lymphocytes from the immunosuppression. T cells are the mediators of acute, cell-mediated gra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2aa76e583983d3466cf8eb71deb8bbf1
https://doi.org/10.1097/tp.0b013e31819574e9
https://doi.org/10.1097/tp.0b013e31819574e9
Autor:
Pak-Kei M. Chan, Jesus F. Bermejo-Martin, David J. Kelvin, Julio C. Medina, Yuan Fang, Patricia V. Turner, Longsi Ran, Mark J. Cameron, Tassie L. Collins, Luoling Xu, Nutan Mytle, Ali Danesh, Cheryl M. Cameron, Ran Ran, Thomas Rowe, Timothy J. Sullivan, Michael G. Johnson
Publikováno v:
Journal of Virology
How viral and host factors contribute to the severe pathogenicity of the H5N1 subtype of avian influenza virus infection in humans is poorly understood. We identified three clusters of differentially expressed innate immune response genes in lungs fr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d91f902b48cce7d78ba7573e8f0d18d8
Autor:
Jason Duquette, Lawrence R. McGee, Xiaohui Du, Tim Sullivan, Julio C. Medina, Jay Danao, George Tonn, Michael G. Johnson, Darin J. Gustin, Zice Fu, Jeffrey Deignan, Ji Ma, Liusheng Zhu, Liang Tang, Andrew P. Marcus, An-Rong Li, Phillipe Bergeron, Xiaoqi Chen, Bryan Lemon, Jiwen Liu, Tassie L. Collins, Teresa Arazas Carabeo, Jeffrey T. Mihalic
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:688-693
A series of six–six and six–five fused heterocyclic CXCR3 antagonists has been synthesized and their activities evaluated in an [125I]-IP-10 displacement assay and an ITAC mediated in vitro cell migration assay. The pharmacokinetic properties of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56a2bd5999bfd49a8e8a6ca4e4ac43a4
https://doi.org/10.1016/j.bmcl.2007.11.060
https://doi.org/10.1016/j.bmcl.2007.11.060
Autor:
Jason Duquette, Xiaoqi Chen, George Tonn, Jeffrey T. Mihalic, Julio C. Medina, Ji Ma, Shichang Miao, Karen Ebsworth, Jeffrey Deignan, An-Rong Li, Tassie L. Collins, Xiaohui Du, Bryan Lemon, Tim Sullivan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:608-613
A series of imidazole derivatives have been designed and optimized for CXCR3 antagonism, pharmacokinetic properties, and reduced formation of glutathione conjugates. Our efforts led to the discovery of potent CXCR3 antagonists with good pharmacokinet
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5a9a60c5206e6e66c7bd4d6a6702a47
https://doi.org/10.1016/j.bmcl.2007.11.072
https://doi.org/10.1016/j.bmcl.2007.11.072
Autor:
Jay Danao, Xuemei Wang, Tim Sullivan, Thomas J. Schall, Zice Fu, Dan Dairaghi, Emmanuel Sablan, Jeff Kumer, Feng Xu, Christopher E. Lawrence, Shichang Miao, Alan Huang, Andrew P. Marcus, George Tonn, Michael Johnson, Jiwen Liu, Tassie L. Collins, Julio C. Medina, Qingge Xu, Liusheng Zhu, Karen Ebsworth, An-Rong Li
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3339-3343
A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a (125)I-IP10 displacement assay and in in vitro cell migration assays to IP10, ITAC,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77083451f6ebe846306065d44c875f1a
https://doi.org/10.1016/j.bmcl.2007.03.106
https://doi.org/10.1016/j.bmcl.2007.03.106