Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Naing Aay"'
Autor:
David Wildes, John E. Knox, Daniel M. Whalen, Carlos Stahlhut, Cregg James Joseph, Abby Marquez, Mae Saldajeno-Concar, Adrian Liam Gill, Elena S. Koltun, Frances Zhao, Severin K. Thompson, Nataliya Tobvis Shifrin, Richard Hansen, Micah J. Gliedt, Mallika Singh, Mengqi Zhong, Naing Aay, Lindsay S. Garrenton, Ruiping Zhao, Elsa Quintana, Bao Nguyen, Laura L. McDowell, Jong Choi, Arlyn Tambo-Ong, Andreas Buckl, David C. Montgomery, Atti Tripathi, Alun Bermingham, Zhengping Wang, Jan A. Smith, Grace J. Lee, Daphne Hsieh
Publikováno v:
Cancer Research. 81:1273-1273
The guanine nucleotide exchange factor (GEF) protein SOS1 activates RAS by promoting its conversion from the GDP-bound RAS(OFF) state to the GTP-bound RAS(ON) state. SOS1 catalyzes or accelerates this nucleotide exchange reaction in response to upstr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::84529dd9e8d7b5ae744e473068a78025
https://doi.org/10.1158/1538-7445.am2021-1273
https://doi.org/10.1158/1538-7445.am2021-1273
Autor:
John Woolfrey, Craig Stacy Takeuchi, Arthur Plonowski, Kyoko Yamaguchi, Ron Aoyama, Byung Gyu Kim, Anagha Abhijit Joshi, Paul Foster, Sunghoon Ma, Sharmila Rajan, Tae Gon Baik, Naing Aay, Arlyn Arcalas, Charles M. Blazey, Jonah Cannoy, Peter Lamb, Isabelle Lehoux, Chris A. Buhr, Narsimha Munagala, Matthew Sangyup Lee, John M. Nuss, James W. Leahy, Jae Lee, Sergey Epshteyn, Neel Kumar Anand, Nicole Miller, Longcheng Wang, Katherine Lara, Henry Johnson
Publikováno v:
Journal of Medicinal Chemistry. 56:2218-2234
A series of novel, highly potent, selective, and ATP-competitive mammalian target of rapamycin (mTOR) inhibitors based on a benzoxazepine scaffold have been identified. Lead optimization resulted in the discovery of inhibitors with low nanomolar acti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e37d108d9c419238d27ed27c967013b5
https://doi.org/10.1021/jm3007933
https://doi.org/10.1021/jm3007933
Autor:
Sunghoon Ma, Julie Lougheed, Christopher Jaeger, Scott W. Womble, Jean-Claire Limun Manalo, Chris A. Buhr, Longcheng Wang, Wentao Zhang, Kenneth D. Rice, Steven Charles Defina, Abigail R. Kennedy, Timothy S. Heuer, Michael Yakes, Neel Kumar Anand, Tae-Gon Baik, Curtis Jeff Kimo, Joerg Bussenius, Angie I. Kim, Jonathan C. Li, Michael Pack, Csaba J. Peto, Monique Nicoll, Naing Aay, Simona Costanzo, Jae Lee, Garth Joseph Mcgrath, Charles M. Blazey, Tsze H. Tsang, Shiva Malek, Anagha Abhijit Joshi, Arlyn Arcalas, Ping Huang, Larisa Dubenko, Jean-Francois Martini, Katherine Lara, John M. Nuss, Owen Joseph Bowles
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5396-5404
With structural guidance, tropane-derived HTS hits were modified to optimize for HSP90 inhibition and a desirable in vivo profile. Through an iterative SAR development process 12i (XL888) was discovered and shown to reduce HSP90 client protein conten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd3657e6e173629f0f09489df1637838
https://doi.org/10.1016/j.bmcl.2012.07.052
https://doi.org/10.1016/j.bmcl.2012.07.052
Autor:
John M. Nuss, Gordon Mark Stott, Hongwang Du, E.S. Koltun, A.D Laird, I Ngan, Amy Lew Tsuhako, Adam A. Galan, Ping Huang, Thomas J. Stout, Patrick Kearney, Chan, Stuart Johnston, W. Zhang, R Lin, Stefan Engst, Peiwen Zhou, L Mock, Maurizio Franzini, Brown S David, Moon Hwan Kim, Brian Kane, Naing Aay, Arlyn Arcalas, Wei Xu, Michael Pack, Peiwen Yu, Cristiana A. Zaharia
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3732-3738
A series of substituted benzofuropyrimidinones with pan-PIM activities and excellent selectivity against a panel of diverse kinases is described. Initial exploration identified aryl benzofuropyrimidinones that were potent, but had cell permeability l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84ad4fc4a63c7985616e1d826de93fb2
https://doi.org/10.1016/j.bmcl.2012.04.025
https://doi.org/10.1016/j.bmcl.2012.04.025
Autor:
Arlyn Arcalas, Richards Steven J, Amy Lew Tsuhako, Naing Aay, Kim Ferguson, Arthur Plonowski, Gordon Mark Stott, Wei Xu, Jenny Young, Peiwen Yu, Wentao Zhang, Charles R. Holst, Kevin Noson, Cristiana A. Zaharia, Brown S David, Hongwang Du, Manisha Mohan, Ping Huang, Thomas J. Stout, Adam A. Galan, Patrick Kearney, David W. Markby, Stefan Engst, Maurizio Franzini, Peiwen Zhou, John M. Nuss, Brian Kane, Kenneth J. Shaw, Elena S. Koltun, Scott Robertson, Moon Hwan Kim, Vicky Chan, Jia Li
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3727-3731
CDC7 is a serine/threonine kinase that has been shown to be required for the initiation and maintenance of DNA replication. Up-regulation of CDC7 is detected in multiple tumor cell lines, with inhibition of CDC7 resulting in cell cycle arrest. In thi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::728a0209cfabeafbb8605b83873ecf26
https://doi.org/10.1016/j.bmcl.2012.04.024
https://doi.org/10.1016/j.bmcl.2012.04.024
Autor:
Danny Tam, Amanda Harrison, Jason August Nachtigall, Fawn Qian, Ron Aoyama, Jon Rosen, Peter Lamb, Tao Wang, Artur Plonowski, Belinda Cancilla, Naing Aay, Elena S. Koltun, Patrick Kearney, Adam A. Galan, Arlyn Arcalas, Kwang-Ai Won, Wentao Zhang, Raju Mohan, Hongwang Du, Vicky Chan, Art Hanel, Patricia Finn, Michael Yakes, Jeff Zhang, Richards Steven J, Frauke Bentzien, John M. Nuss, Kathy Ogilvie, Christopher J. Larson
Publikováno v:
Journal of Medicinal Chemistry. 55:4322-4335
Targeting glycosphingolipid synthesis has emerged as a novel approach for treating metabolic diseases. 32 (EXEL-0346) represents a new class of glucosylceramide synthase (GCS) inhibitors. This report details the elaboration of hit 8 with the goal of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0cd8c748fee52922d91c2b98ea12917f
https://doi.org/10.1021/jm300122u
https://doi.org/10.1021/jm300122u
Autor:
Jeffry Kimo Curtis, Julie Lougheed, Stefan Engst, Peiwen Yu, Anagha Abhijit Joshi, Elena S. Koltun, Csaba J. Peto, Neel Kumar Anand, Jean-Claire Limun Manalo, Stuart Johnston, Steven Charles Defina, Abigail R. Kennedy, Naing Aay, Kenneth D. Rice, Larisa Dubenko, Tsze H. Tsang, Jean-Francois Martini, Simona Costanzo, John M. Nuss, Angie I. Kim, Owen Joseph Bowles, Joerg Bussenius, Charles M. Blazey
Publikováno v:
ACS Medicinal Chemistry Letters. 3:416-421
The ERK/MAP kinase cascade is a key mechanism subject to dysregulation in cancer and is constitutively activated or highly upregulated in many tumor types. Mutations associated with upstream pathway components RAS and Raf occur frequently and contrib
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a20c73fff311c30e1eae8739e95812e0
https://doi.org/10.1021/ml300049d
https://doi.org/10.1021/ml300049d
Autor:
Patricia Finn, Jeff Zhang, Patrick Kearney, Raju Mohan, Tao Wang, Peter Lamb, Vicky Chan, Danny Tam, Christopher J. Larson, Kwang-Ai Won, Adam A. Galan, Amanda Harrison, Jason August Nachtigall, Art Hanel, Jon Rosen, Richards Steven J, John M. Nuss, Naing Aay, Fawn Qian, Kevin Noson, Kathleen M. Ogilvie, Hongwang Du, Elena S. Koltun
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6773-6777
A novel series of potent inhibitors of glucosylceramide synthase are described. The optimization of biochemical and cellular potency as well as ADME properties led to compound 23c. Broad tissue distribution was obtained following oral administration
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68aa3f4462e296a5ca699bcb45dea236
https://doi.org/10.1016/j.bmcl.2011.09.037
https://doi.org/10.1016/j.bmcl.2011.09.037
Autor:
Ashutosh S. Jogalekar, Mellem Kevin, Chris M. Semko, Andreas Buckl, Elena S. Koltun, Jacqueline Smith, Naing Aay, Mallika Singh, Christos Tzitzilonis, Robert J. Nichols, Won Walter, Nidhi Tibrewal, Zhengping Wang, Kasia Mordec, Adrian Liam Gill, Gert Kiss, Abby Marquez, Susan E. Wilson, Mae Saldajeno-Concar, David Wilds
Publikováno v:
Cancer Research. 78:4878-4878
Genetic and pharmacologic evidence has shown that SHP2, a non-receptor protein tyrosine phosphatase (PTP) and scaffold protein encoded by the PTPN11 gene, is a convergent signal transduction node that integrates growth factor signals from multiple re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b9799dbbd6e549ae1405a9baa4fbc959
https://doi.org/10.1158/1538-7445.am2018-4878
https://doi.org/10.1158/1538-7445.am2018-4878
Autor:
Adrian Liam Gill, Gert Kiss, Daphne Hsieh, Jacqueline Smith, Robert J. Nichols, Chris M. Semko, Naing Aay, Ashutosh S. Jogalekar, Mellem Kevin, Mae Saldajeno-Concar, David Wildes, Won Walter, Andreas Buckl, Christopher J. Schulze, Carlos Stahlhut, Jason Romero, Christos Tzitzilonis, Elena S. Koltun, Abby Marquez
Publikováno v:
Cancer Research. 78:4877-4877
SHP2 (PTPN11) is a non-receptor protein tyrosine phosphatase and scaffold protein that functions in multiple signal transduction pathways. Genetic and pharmacologic evidence supports a role for SHP2 in driving the proliferation of cancer cells depend
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e7ded4958643dc44622b33737ce5fb4d
https://doi.org/10.1158/1538-7445.am2018-4877
https://doi.org/10.1158/1538-7445.am2018-4877