Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Dorina Trusca"'
Autor:
Qiaoling Deng, Feroze Ujjainwalla, F. Anthony Romero, Jenna L. Terebetski, Jerry Di Salvo, Ying Li, Dorina Trusca, Ming Wang, Nicholas B. Hastings, Remond Moningka, Vincent Tong, Zhiqiang Guo, Richard G. Ball
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(23)
Here, we report the discovery of a new class of NPBWR1 antagonists identified from a fragment-based screen. Compound 1 (cAMP IC50 = 250 µM; LE = 0.29) emerged as an initial hit. Further optimization of 1 by SAR-by-catalogue and chemical modification
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77e4a6a9cbe7d66ea64b2f90c58c7963
https://pubmed.ncbi.nlm.nih.gov/32898693
https://pubmed.ncbi.nlm.nih.gov/32898693
Autor:
Matthew Lombardo, Eric N. Johnson, John Cummings, Jerry Di Salvo, Thomas Roussel, James R. Tata, Melissa Kirkland, Michael A. Plotkin, Christopher Joseph Sinz, Feroze Ujjainwalla, Dennis Leung, Dorina Trusca, Joel Mane, Taro E. Akiyama, Alejandro Crespo, Mary Ann Powles, Kate Bender, Michael F.A. Finley, Joanna Pols, Candice Alleyne, Michele Pachanski, Andrew D. Howard, Wayne M. Geissler, Ying Lei, Bahanu Habulihaz, Victor N. Uebele, Clare London, Maria Madeira
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(5)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a15bdf4d7ae8e579647d40689c42f33e
https://pubmed.ncbi.nlm.nih.gov/27815121
https://pubmed.ncbi.nlm.nih.gov/27815121
Autor:
Donald Nelson, Gary G. Chicchi, James Dellureficio, Ravi P. Nargund, Peter H. Dobbelaar, Liangqin Guo, Kwei-Lan Tsao, Janet S. Kerr, Bei Zhang, Zhong Lai, Patricia R. Bunting, Shrenik K. Shah, Raman K. Bakshi, Qingmei Hong, Hongbo Qi, Guillermo Fernandez, Mikhail Reibarkh, Qing Shao, Quang Truong, Koppara Samuel, Jian Liu, Sylvia Volksdorf, Zhixiong Ye, Yun-Ping Zhou, Margaret Wu, Cai Li, Stan Mitelman, Andrew D. Howard, Wu Du, Maria E. Trujillo, George J. Eiermann, Shuwen He, Vijay Bhasker G. Reddy, Tianying Jian, Pierre Morissette, Patrick Fitzgerald, Dorina Trusca, Sharon Tong, William K. Hagmann
Publikováno v:
ACS Medicinal Chemistry Letters. 5:748-753
Antagonism of somatostatin subtype receptor 3 (sstr3) has emerged as a potential treatment of Type 2 diabetes. Unfortunately, the development of our first preclinical candidate, MK-4256, was discontinued due to a dose-dependent QTc (QT interval corre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ced576c72131916fe1527dabb0d36e73
https://doi.org/10.1021/ml500028c
https://doi.org/10.1021/ml500028c
Autor:
Christopher Joseph Sinz, Feroze Ujjainwalla, Joel Mane, Eric N. Johnson, John Cummings, Jerry Di Salvo, Michele Pachanski, Michael A. Plotkin, Joanna Pols, Taro E. Akiyama, Andrew D. Howard, Matthew Lombardo, James R. Tata, Maria Madeira, Ying Lei, Wayne M. Geissler, Victor N. Uebele, Michael F.A. Finley, Clare London, Candice Alleyne, Thomas Roussel, Kate Bender, Dennis Leung, Bahanu Habulihaz, Mary Ann Powles, Melissa Kirkland, Dorina Trusca, Alejandro Crespo
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(23)
The transformation of an aryloxybutanoic acid ultra high-throughput screening (uHTS) hit into a potent and selective series of G-protein coupled receptor 120 (GPR120) agonists is reported. uHTS hit 1 demonstrated an excellent rodent pharmacokinetic p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a693b676faad583895d0ff2ed06132a4
https://pubmed.ncbi.nlm.nih.gov/28169160
https://pubmed.ncbi.nlm.nih.gov/28169160
Autor:
Janet Kerr, Gary G. Chicchi, Margaret Wu, Cai Li, Shuwen He, Vijay Bhasker G. Reddy, Sharon Tong, William K. Hagmann, Patrick Fitzgerald, Guillermo Fernandez, Andrew D. Howard, Tianying Jian, Zhe Feng, Raman K. Bakshi, Dorina Trusca, Peter H. Dobbelaar, Donald Nelson, Mikhail Reibarkh, Qing Shao, Liangqin Guo, Yun-Ping Zhou, Ravi P. Nargund, Kwei-Lan Tsao, Edward C. Sherer, Stan Mitelman, Pierre Morissette, Maria E. Trujillo, Quang Truong, Zhixiong Ye, James D. Dellureficio, Hongbo Qi, Melissa Lin, Shrenik K. Shah, Sylvia Volksdorf, Jian Liu, Qingmei Hong, Koppara Samuel, Alexander Pasternak, George J. Eiermann, Patricia B. Bunting, Wu Du, Bei B. Zhang
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(6)
MK-4256, a tetrahydro-β-carboline sstr3 antagonist, was discontinued due to a cardiovascular (CV) adverse effect observed in dogs. Additional investigations revealed that the CV liability (QTc prolongation) was caused by the hERG off-target activity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6412732d83fd31156d7974bed1994494
https://pubmed.ncbi.nlm.nih.gov/26898814
https://pubmed.ncbi.nlm.nih.gov/26898814
Autor:
Kwei-Lan Tsao, Derun Li, Liangqing Guo, Richard G. Ball, Zhicai Wu, David X. Yang, Gary G. Chicchi, William K. Hagmann, Quang Tuang, Dorina Trusca, Yang Yu, Shuwen He, Qingmei Hong, Ravi P. Nargund, Edward C. Sherer, Yun-Ping Zhou, Zhong Lai, Andrew D. Howard
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(17)
We report SAR studies on a novel non-peptidic somatostatin receptor 3 (SSTR3) agonist lead series derived from (4-phenyl-1H-imidazol-2-yl)methanamine. This effort led to the discovery of a highly potent low molecular weight SSTR3 agonist 5c (EC50=5.2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e290258042757d2c6805a1afb8166f73
https://pubmed.ncbi.nlm.nih.gov/26199120
https://pubmed.ncbi.nlm.nih.gov/26199120
Autor:
Yang Yu, Gary G. Chicchi, Frederick Wong, Janet S. Kerr, Sharon Tong, Zhe Feng, Guillermo Fernandez, Edward C. Sherer, Kwei-Lan Tsao, Qing Shao, Bei B. Zhang, Yun-Ping Zhou, Pierre Morissette, Shuwen He, Shrenik K. Shah, Vijay Bhasker G. Reddy, Liangqin Guo, Ravi P. Nargund, Margaret Wu, Cai Li, Zhixiong Ye, Alexander Pasternak, George J. Eiermann, Patricia R. Bunting, Hongbo Qi, Michele Pachanski, Stan Mitelman, Maria E. Trujillo, Quang Truong, Maria Madiera, Andrew D. Howard, Donald Nelson, Qingmei Hong, Zhong Lai, Yue Feng, Bindhu V. Karanam, Jian Liu, Koppara Samuel, Wu Du, William K. Hagmann, Tianying Jian, Dorina Trusca, Sylvia Volksdorf, Peter H. Dobbelaar
Publikováno v:
ACS medicinal chemistry letters. 6(5)
The imidazolyl-tetrahydro-β-carboline class of sstr3 antagonists have demonstrated efficacy in a murine model of glucose excursion and may have potential as a treatment for type 2 diabetes. The first candidate in this class caused unacceptable QTc i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8391d2d13678e95f2d50ddfa654d1520
https://pubmed.ncbi.nlm.nih.gov/26005524
https://pubmed.ncbi.nlm.nih.gov/26005524
Autor:
David Bramhill, Dorina Trusca
Publikováno v:
Analytical Biochemistry. 307:322-329
Septum formation in Escherichia coli is a complex cascade of interactions among cell-division proteins. The tubulin-like FtsZ division protein localizes to the division site and serves a cytoskeletal role during septum formation. A novel fluorescent-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d7504e3778c63ae710f08507d175fea
https://doi.org/10.1016/s0003-2697(02)00036-2
https://doi.org/10.1016/s0003-2697(02)00036-2
Autor:
Richard G. Ball, Liangqin Guo, Zhicai Wu, Quang Truong, Gary G. Chicchi, Ravi P. Nargund, Dorina Trusca, Kwei-Lan Tsao, Qingmei Hong, Yang Yu, George J. Eiermann, Shuwen He, Yun-Ping Zhou, Bei B. Zhang, William K. Hagmann, Maria E. Trujillo, Michele Pachanski, Hongbo Qi, David X. Yang, Andrew D. Howard, Derun Li, Zhong Lai, Edward C. Sherer
Publikováno v:
ACS medicinal chemistry letters. 5(6)
A novel class of small-molecule, highly potent, and subtype-selective somatostatin SST3 agonists was discovered through modification of a SST3 antagonist. As an example, (1R,2S)-9 demonstrated not only potent in vitro SST3 agonist activity but also i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a64a41cfd844bfc5154bf7fc7e59f92
https://pubmed.ncbi.nlm.nih.gov/24944745
https://pubmed.ncbi.nlm.nih.gov/24944745
Bacterial SOS Checkpoint Protein SulA Inhibits Polymerization of Purified FtsZ Cell Division Protein
Publikováno v:
Journal of Bacteriology. 180:3946-3953
Cell division of Escherichia coli is inhibited when the SulA protein is induced in response to DNA damage as part of the SOS checkpoint control system. The SulA protein interacts with the tubulin-like FtsZ division protein. We investigated the effect
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c214f254eef17e581b86d1f9d733e00c
https://doi.org/10.1128/jb.180.15.3946-3953.1998
https://doi.org/10.1128/jb.180.15.3946-3953.1998