Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Karen Augustine"'
Autor:
Faye Wang, Cindy Zhang, Jae Kwagh, Brian Strassle, Jinqing Li, Minxue Huang, Yunling Song, Brenda Lehman, Richard Westhouse, Kamalavenkatesh Palanisamy, Vinay K. Holenarsipur, Robert Borzilleri, Karen Augustine-Rauch
Publikováno v:
iScience, Vol 24, Iss 3, Pp 102133- (2021)
Summary: This study focused on characterizing the potential mechanism of valvular toxicity caused by TGFβ receptor inhibitors (TGFβRis) using rat valvular interstitial cells (VICs) to evaluate early biological responses to TGFβR inhibition. Three
Externí odkaz:
https://doaj.org/article/a68cd93dd958438cb620f93aecf70450
Autor:
Shiuhang Yip, Emily Luk, Anwar Murtaza, Yong Zhang, Michael A. Poss, Louis J. Lombardo, Nimmi Raghavan, Zheng Yang, James Kempson, Audris Huang, David R. Tortolani, Jesse Swanson, Xiaoping Hou, Joseph Pawluczyk, James Smalley, Honghe Wan, Karen E. Parrish, Robert M. Borzilleri, Ashok V. Purandare, Karen Augustine-Rauch, Andrew F. Donnell
Publikováno v:
Journal of Medicinal Chemistry. 64:15787-15798
Inhibition of TGFβ signaling in concert with a checkpoint blockade has been shown to provide improved and durable antitumor immune response in mouse models. However, on-target adverse cardiovascular effects have limited the clinical use of TGFβ rec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aebde71751ab18259045cb79ccd54677
https://doi.org/10.1021/acs.jmedchem.0c02043
https://doi.org/10.1021/acs.jmedchem.0c02043
Autor:
Jennifer Brown, Karen E. Parrish, Andrew J. Tebben, Jonathan Lippy, Kamalavenkatesh Palanisamy, Todd Kinsella, Chetan Padmakar Darne, Vinay K. Holenarsipur, Anwar Murtaza, Muthalagu Vetrichelvan, Chunhong Yan, Karen Augustine-Rauch, Max Ruzanov, Mark Fereshteh, Upender Velaparthi, Gopal Dhar, Gregory D. Vite, Peiying Liu, Steven Sheriff, Jayakumar Sankara Warrier, Aravind Anandam, Marina Gelman, Arvind Mathur, Barri Wautlet, Robert M. Borzilleri, Hasibur Rahaman, Zheng Yang, Anuradha Gupta, Arun Kumar Gupta, Rajinder Singh, Joseph Fargnoli, Jesse Swanson
Publikováno v:
ACS Med Chem Lett
[Image: see text] Novel imidazole-based TGFβR1 inhibitors were identified and optimized for potency, selectivity, and pharmacokinetic and physicochemical characteristics. Herein, we report the discovery, optimization, and evaluation of a potent, sel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57c0a6b7db9a564a606d22c0c365bdb7
https://doi.org/10.1021/acsmedchemlett.9b00552
https://doi.org/10.1021/acsmedchemlett.9b00552
Autor:
Scott Engel, K. Turner, Marlowe J. Schneidkraut, Brian P. Enright, Karen Augustine-Rauch, Mary Ellen McNerney, Paul Barrow, S. Powlin, K. Brannen, Bruce K. Beyer, Michael J. Graziano, David Potter, William S. Nowland, Dinesh Stanislaus, Nicola Powles-Glover
Publikováno v:
Regulatory toxicology and pharmacology : RTP. 124
An IQ DruSafe working group evaluated the concordance of 3 alternative teratogenicity assays (rat whole embryo culture, rWEC; zebrafish embryo culture, ZEC; and murine embryonic stem cells, mESC) with findings from rat or rabbit embryo-fetal developm
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::822c740e5933ddf69fac1cc9f0f30b2c
https://pubmed.ncbi.nlm.nih.gov/34216694
https://pubmed.ncbi.nlm.nih.gov/34216694
Autor:
Richard A. Westhouse, Faye Wang, Jae Kwagh, Brian Strassle, Cindy X. Zhang, Robert M. Borzilleri, Minxue Huang, Vinay K. Holenarsipur, Yunling Song, Kamalavenkatesh Palanisamy, Karen Augustine-Rauch, Jinqing Li, Brenda L. Lehman
Publikováno v:
iScience
iScience, Vol 24, Iss 3, Pp 102133-(2021)
iScience, Vol 24, Iss 3, Pp 102133-(2021)
Summary This study focused on characterizing the potential mechanism of valvular toxicity caused by TGFβ receptor inhibitors (TGFβRis) using rat valvular interstitial cells (VICs) to evaluate early biological responses to TGFβR inhibition. Three T
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8bd59b157c461a0b574214f67fb19f6
http://europepmc.org/articles/PMC7900227
http://europepmc.org/articles/PMC7900227
Publikováno v:
Toxicology and applied pharmacology. 411
Pexacerfont is a corticotrophin-releasing factor subtype 1 receptor (CRF-1) antagonist developed for potential treatment of anxiety and stress-related disorders. In male rats, pexacerfont caused hepatic enzyme induction leading to increased thyroxine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f59b79bc236063f5ced4d159c59ce71
https://pubmed.ncbi.nlm.nih.gov/33340518
https://pubmed.ncbi.nlm.nih.gov/33340518
Autor:
Courtni Newsome, Gregory D Rak, Michael J. Graziano, Gene E. Schulze, Melvin R. White, Karen Augustine-Rauch
Publikováno v:
Journal of applied toxicology : JATREFERENCES. 40(7)
Small-molecule inhibitors of transforming growth factor beta receptor 1 (TGFβRI) have a history of significant class-based toxicities (eg, cardiac valvulopathy) in preclinical species that have limited their development as new medicines. Nevertheles
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8fa5ad0786ba08a67115940e0d62ad72
https://pubmed.ncbi.nlm.nih.gov/32061184
https://pubmed.ncbi.nlm.nih.gov/32061184
Publikováno v:
Birth Defects Research Part B: Developmental and Reproductive Toxicology. 107:4-20
Increasing need for proactive safety optimization of pharmaceutical compounds has led to generation and/or refinement of in vitro developmental toxicology assays. Our laboratory has developed three in vitro developmental toxicology assays to assess t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3a64414c4459b395973fb797b72fe2fa
https://doi.org/10.1002/bdrb.21168
https://doi.org/10.1002/bdrb.21168
Autor:
Cindy X. Zhang, Danielle Greenawalt, Ke Xu, Julie Panzica-Kelly, Richard A. Westhouse, Ronald Fleming, Ashvinikumar V. Gavai, Jennifer Price, Denise Bounous, Shodeinde Coker, Karen Augustine-Rauch, Kezi Unsal-Kacmaz
Publikováno v:
Cancer Research. 80:1742-1742
Bromodomain and extraterminal (BET) proteins recognize acetylated lysine residues for the purpose of transcriptional regulation of genes, including those involved in stem cell renewal and oncogenes such as MYC. Inhibition of BET proteins BRD2, BRD3,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4b3883916b37fbd9d45a48324477e5cf
https://doi.org/10.1158/1538-7445.am2020-1742
https://doi.org/10.1158/1538-7445.am2020-1742
Autor:
Yufen Zhao, Barri Wautlet, Jonathan Lippy, Anne Rose, Andrew J. Tebben, Gregory D. Vite, Max Ruzanov, Joseph Fargnoli, Liping Zhang, Yong Zhang, Zheng Yang, Karen E. Parrish, Robert M. Borzilleri, Yi Fan, Jesse Swanson, Ching-Ping Ho, Karen Augustine-Rauch, Andrew F. Donnell, Brian E. Fink, Steven Sheriff, Mark Fereshteh
[Image: see text] The multifunctional cytokine TGFβ plays a central role in regulating antitumor immunity. It has been postulated that inhibition of TGFβ signaling in concert with checkpoint blockade will provide improved and durable immune respons
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dca61cd13f527f4d17df3df6c932c4f3
https://europepmc.org/articles/PMC6231184/
https://europepmc.org/articles/PMC6231184/
