Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Janet Gunzner-Toste"'
Autor:
Jagath R. Junutula, John A. Flygare, Andrew G. Polson, Paul Polakis, Susan Spencer, Katherine K. Kozak, Janet Gunzner-Toste, Jinhua Chen, Fan Fang, Philip W. Howard, Stephen J. Gregson, Luke Masterson, Donglu Zhang, Amrita V. Kamath, Douglas D. Leipold, Keyang Xu, Carl Ng, Luna Liu, Jintang He, Sharon Yee, Jeffrey Lau, Mary Ann T. Go, Geoffrey Del Rosario, Fiona Zhong, Willy Solis, Kirsten Achilles Poon, Jack Sadowsky, Rachana Ohri, Shang-Fan Yu, Melissa Schutten, Thomas H. Pillow
Supplementary Figures S1-S5, Supplementary Materials and Methods
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14bd04853a3b7478b1a76289e951f293
https://doi.org/10.1158/1535-7163.22503312.v1
https://doi.org/10.1158/1535-7163.22503312.v1
Autor:
Katherine R. Kozak, Siao Ping Tsai, Doug Leipold, Luke Masterson, Hui Yao, Stefan Steinbacher, Jim Nonomiya, Keyang Xu, Helga Raab, Vishal Verma, Binqing Wei, Jeff Lau, Tao Wang, Janet Gunzner-Toste, Shang-Fan Yu, John A. Flygare, Thomas H. Pillow, Leanna Staben, John S. Wai, Zijin Xu, Brian Safina, Gail Dianne Phillips, Philip Howard, Jing Wang, Dian Su, Josefa Chuh, Jinhua Chen, Guiling Zhao, Guangmin Li, Rachana Ohri, Yichin Liu, Amrita V. Kamath, Charles Eigenbrot
Publikováno v:
Journal of Medicinal Chemistry. 61:989-1000
Antibody-drug conjugates (ADCs) have become an important therapeutic modality for oncology, with three approved by the FDA and over 60 others in clinical trials. Despite the progress, improvements in ADC therapeutic index are desired. Peptide-based A
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ec0f3685ed5ba96d277235ba33db5f5
https://doi.org/10.1021/acs.jmedchem.7b01430
https://doi.org/10.1021/acs.jmedchem.7b01430
Autor:
Binqing Wei, Janet Gunzner-Toste, Guangmin Li, Helga Raab, Susan D. Spencer, Gail Lewis Phillips, Shang-Fan Yu, Katherine R. Kozak, Rachana Ohri, Jeffrey Lau, Philip Howard, Andrew Polson, Brian Safina, Luke Masterson, John A. Flygare, Thomas H. Pillow, Martine Darwish, Stephen J. Gregson, Gyoung-Dong Kang, Josefa dela Cruz-Chuh
Publikováno v:
Journal of Medicinal Chemistry. 60:9490-9507
Three rationally designed pyrrolobenzodiazepine (PBD) drug-linkers have been synthesized via intermediate 19 for use in antibody–drug conjugates (ADCs). They lack a cleavable trigger in the linker and consist of a maleimide for cysteine antibody co
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a180d2e49398f22d60da17ee0112defd
https://doi.org/10.1021/acs.jmedchem.7b00736
https://doi.org/10.1021/acs.jmedchem.7b00736
Autor:
Janet Gunzner-Toste, Maureen Caligiuri, Nicholas J. Skelton, Jian Lin, Sophie Mukadam, Weiru Wang, Paul Bauer, Kenneth W. Bair, Xiaozhang Zheng, Karl H. Clodfelter, Bianca M. Liederer, Bang Fu, Thomas O'Brien, Zhongguo Wang, Peter S. Dragovich, Jasleen K. Sodhi, Lei Zhang, Geeta Sharma, Yen-Ching Ho, Chase C. Smith, Dominic J. Reynolds, Bingsong Han, Alexandre J. Buckmelter, Timm Baumeister, Angela Oh, Guiling Zhao, Nikolai Kley, Xiaorong Liang, Yang Xiao, Yuen Po-Wai, Mark Zak
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3531-3538
Potent, reversible inhibition of the cytochrome P450 CYP2C9 isoform was observed in a series of urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors. This unwanted property was successfully removed from the described inhibitors t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01ca604ab818ff8d825e51214466d272
https://doi.org/10.1016/j.bmcl.2013.04.040
https://doi.org/10.1016/j.bmcl.2013.04.040
Autor:
Carl Ng, Melissa Schutten, Geoffrey Del Rosario, Donglu Zhang, Luke Masterson, Jintang He, Jagath Reddy Junutula, Jack Sadowsky, Katherine K. Kozak, Fiona Zhong, Stephen J. Gregson, Amrita V. Kamath, Paul Polakis, Philip Howard, Andrew Polson, Mary Ann T. Go, Douglas D. Leipold, John A. Flygare, Willy Solis, Jeffrey Lau, Rachana Ohri, Shang-Fan Yu, Jinhua Chen, Keyang Xu, Thomas H. Pillow, Fan Fang, Sharon Yee, Kirsten Achilles Poon, Janet Gunzner-Toste, Luna Liu, Susan D. Spencer
Publikováno v:
Molecular cancer therapeutics. 16(5)
A novel disulfide linker was designed to enable a direct connection between cytotoxic pyrrolobenzodiazepine (PBD) drugs and the cysteine on a targeting antibody for use in antibody–drug conjugates (ADCs). ADCs composed of a cysteine-engineered anti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f4779fe39a8fdd4dd7fb71a89514555
https://pubmed.ncbi.nlm.nih.gov/28223423
https://pubmed.ncbi.nlm.nih.gov/28223423
Autor:
Janet Gunzner-Toste, Edna F. Choo, Bruno Alicke, Stephen E. Gould, Rebecca Pulk, Ellen R. Laird, Zhaoyang Wen, Li Ren, Jonas Grina, Jason Boggs, David A. Moreno, Joachim Rudolph, Alexandre J. Buckmelter, Simon Mathieu, Guiling Zhao, Stefan Gradl, Walter C. Voegtli, Yingqing Ran, Ignacio Aliagas, Joshua D. Hansen, Georgia Hatzivassiliou, Wendy Lee, Victoria Dinkel, Steve Wenglowsky, Gregg Hastings, Susan L. Gloor
Publikováno v:
Journal of Medicinal Chemistry. 55:2869-2881
Recent clinical data provided proof-of-concept for selective B-Raf inhibitors in treatment of B-Raf(V600E) mutant melanoma. Pyrazolopyridine-type B-Raf inhibitors previously described by the authors are potent and selective but exhibit low solubility
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe406c81e2b726f608483bebd89badca
https://doi.org/10.1021/jm300016v
https://doi.org/10.1021/jm300016v
Autor:
Yuen Po-Wai, Deepak Sampath, Xiaolei Ma, Yongbo Liu, Anthony M. Giannetti, Janet Gunzner-Toste, Guiling Zhao, Xiaozhang Zheng, Weiru Wang, Thomas O'Brien, Nicholas J. Skelton, Yang Xiao, Leslie Wang, Rongbao Hua, Yen-Ching Ho, Yezhen Feng, Peter S. Dragovich, Youming Shen, Qiang Zhao, Chengcheng Wang, Eric Cheng, Brandon J. Bravo, Timm Baumeister, Lisa Crocker, Kenneth W. Bair, Bianca M. Liederer, Mark Zak, Hongxing Wu, Jason Oeh
Publikováno v:
Journal of medicinal chemistry. 57(3)
Potent, trans-2-(pyridin-3-yl)cyclopropanecarboxamide-containing inhibitors of the human nicotinamide phosphoribosyltransferase (NAMPT) enzyme were identified using fragment-based screening and structure-based design techniques. Multiple crystal stru
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58b578f8fb1eaeb416a5762c86e608fa
https://pubmed.ncbi.nlm.nih.gov/24405419
https://pubmed.ncbi.nlm.nih.gov/24405419
Autor:
Maureen Caligiuri, Jian Lin, Alexandre J. Buckmelter, Timm Baumeister, Janet Gunzner-Toste, Leslie Wang, Karl H. Clodfelter, Guiling Zhao, Geeta Sharma, Chase C. Smith, Justin Ly, Dominic J. Reynolds, Yen-Ching Ho, Bingsong Han, Angela Oh, Thomas O'Brien, Peter S. Dragovich, Xiaozhang Zheng, Zhongguo Wang, Yang Xiao, Yuen Po-Wai, Nikolai Kley, Weiru Wang, Mark Zak, Paul Bauer, Kenneth W. Bair, Bianca M. Liederer
Publikováno v:
Journal of medicinal chemistry. 56(16)
Crystal structures of several urea- and thiourea-derived compounds in complex with the nicotinamide phosphoribosyltransferase (Nampt) protein were utilized to design a potent amide-containing inhibitor bearing an aza-indole moiety (7, Nampt BC IC50 =
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea9aff746bfdb4a79b0db19ef2167fcf
https://pubmed.ncbi.nlm.nih.gov/23859118
https://pubmed.ncbi.nlm.nih.gov/23859118
Autor:
Weiru Wang, Peter S. Dragovich, Kenneth W. Bair, Jian Lin, Karl H. Clodfelter, Alexandre J. Buckmelter, Xiaozhang Zheng, Janet Gunzner-Toste, Timm Baumeister, Maureen Caligiuri, Guiling Zhao, Zhongguo Wang, Yuen Po-Wai, Paul Bauer, Nikolai Kley, Angela Oh, Geeta Sharma, Chase C. Smith, Dominic J. Reynolds, Mark Zak, Yen-Ching Ho, Bingsong Han
Publikováno v:
Journal of medicinal chemistry. 56(12)
Nicotinamide phosphoribosyltransferase (Nampt) is a promising anticancer target. Virtual screening identified a thiourea analogue, compound 5, as a novel highly potent Nampt inhibitor. Guided by the cocrystal structure of 5, SAR exploration revealed
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::94f830702c785982553738f36d808da4
https://pubmed.ncbi.nlm.nih.gov/23617784
https://pubmed.ncbi.nlm.nih.gov/23617784
Autor:
Zhenyu Yue, Hilda Solanoy, Janet Gunzner-Toste, Claire E. Le Pichon, Xiao Ding, Anthony A. Estrada, Marcel P. van der Brug, Jason Drummond, Qinghua Song, John Moffat, Huifen Chen, Haitao Zhu, Donald S. Kirkpatrick, Xingrong Liu, Xiaolin Zhang, Zachary Kevin Sweeney, Shuo Zhang, Zejuan Sheng, Daniel J. Burdick, Xianting Li, Sara L. Dominguez, Tracy Kleinheinz, Daisy Bustos, Fang Cai, Kimberly Scearce-Levie
Publikováno v:
Science Translational Medicine. 4
Mutations in the leucine-rich repeat kinase 2 (LRRK2) gene are the most common cause of familial Parkinson's disease (PD). Although biochemical studies have shown that certain PD mutations confer elevated kinase activity in vitro on LRRK2, there are
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc635028b28e63b821c120ddee2478f2
https://doi.org/10.1126/scitranslmed.3004485
https://doi.org/10.1126/scitranslmed.3004485