Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Tom Emm"'
Autor:
Yue Zou, Srijita Dhar, Kirsten Gallagher, Andrew Buesking, Sarah Pawley, Ryan Holmes, Xiaowei Wu, Katarina Rohlfing, Min Wang, Joseph Rager, Tom Emm, Stefan Ruepp, Miles Cowart, Jing Ni, Jean Zhao, Bruce Ruggeri, Andrew Combs, Kris Vaddi, Sandy Geeganage, Ashish Juvekar, Sang Hyun Lee, Peggy Scherle
Publikováno v:
Cancer Research. 83:5973-5973
Cell cycle deregulation is a hallmark of cancer and the hyperactivation and overexpression of CDKs are often drivers of cancer pathogenesis. Cyclin-dependent kinase 4 and 6 (CDK4)/(CDK6) are critical mediators of cellular transition into S phase and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5fe20e98999d400271cbbc5365025a3f
https://doi.org/10.1158/1538-7445.am2023-5973
https://doi.org/10.1158/1538-7445.am2023-5973
Autor:
Brian M. Glass, Padmaja Polam, Tom Emm, Kevin Bowman, Jordan S. Fridman, Holly Koblish, Richard Wynn, Michael Hansbury, Yanlong Li, Eddy W. Yue, Brian Metcalf, Michael J. Bower, Min Wei, Richard B. Sparks, Peggy Scherle, Xiangdong Liu, Andrew P. Combs, Timothy Burn, Dilip P. Modi, Brian Wayland, Qian Wang, Lynn Leffet, Brent Douty, Wenyu Zhu, Amy Takvorian, Joseph Glenn
Publikováno v:
ACS Medicinal Chemistry Letters
A data-centric medicinal chemistry approach led to the invention of a potent and selective IDO1 inhibitor 4f, INCB24360 (epacadostat). The molecular structure of INCB24360 contains several previously unknown or underutilized functional groups in drug
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c5e3f5ea28d700b9b9ea48bc68260b0
http://europepmc.org/articles/PMC5430407
http://europepmc.org/articles/PMC5430407
Autor:
Kris Vaddi, Bruce Ruggeri, Hong Lin, Dave Rominger, Juan Luengo, Michael Hawkins, Peggy Scherle, Yang Zhang, Tom Emm, Dimitrios Angelis, Min Wang
Publikováno v:
Cancer Research. 80:2919-2919
Protein arginine methyltransferase 5 (PRMT5) is the major type II PRMT that catalyzes the formation of symmetrical dimethyl arginine (SDMA) on protein substrates and plays important roles in regulating RNA splicing as well as transcription and activi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6ef8d072e00ea6c6d6d8c96a0bae09e0
https://doi.org/10.1158/1538-7445.am2020-2919
https://doi.org/10.1158/1538-7445.am2020-2919
Autor:
Srdan Verstovsek, Yang Zhang, Ross L. Levine, Alexander Grego, William Gowen-MacDonald, Taghi Manshouri, Dimitrios Angelis, Hong Lin, Peggy Scherle, Juan Luengo, Min Wang, Kris Vaddi, Neha Bhagwat, Dave Rominger, Tom Emm, Bruce Ruggeri, Raul A. Leal, Rupa Shetty, Friederike Pastore, Divya Chugani-Mahtani
Publikováno v:
Cancer Research. 80:2915-2915
Protein arginine methyltransferase 5 (PRMT5) is the major type II PRMT that catalyzes the formation of symmetrical dimethyl arginine (SDMA) on protein substrates and plays important roles in various cellular pathways including tumorigenesis. PRMT5 ca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d22259afd761bc23c7d8f64650167a2b
https://doi.org/10.1158/1538-7445.am2020-2915
https://doi.org/10.1158/1538-7445.am2020-2915
Autor:
Brian Metcalf, Sharon Diamond, Taisheng Huang, Lixin Shao, Swamy Yeleswaram, D. Joseph Rogier, Greg Hollis, Michael Xia, Ke Zhang, Ganfeng Cao, Nancy Contel, Lingquan Kong, Peggy Scherle, Maryanne Covington, Tom Emm, Robert Hughes, Joseph Glenn, Robert C. Newton, Kris Vaddi, Changsheng Zheng, Lou Storace, Chu-Biao Xue, Rajan Anand, Hao Feng, Meloni David, Anlai Wang, Mei Li, Philip A. Morton, Robinson Darius J, Qi Han, Rajesh V. Devraj, Yingxin Zhang
Publikováno v:
ACS Medicinal Chemistry Letters. 2:913-918
We report the discovery of a new (S)-3-aminopyrrolidine series of CCR2 antagonists. Structure-activity relationship studies on this new series led to the identification of 17 (INCB8761/PF-4136309) that exhibited potent CCR2 antagonistic activity, hig
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d2a792b5ba70daa3c854d4e609b3ad5
https://doi.org/10.1021/ml200199c
https://doi.org/10.1021/ml200199c
Autor:
Karen Gallagher, Timothy V Olah, Romas Geleziunas, Steve Unger, Guoen Shi, Yu Li, Tom Emm, Jing-Tao Wu
Publikováno v:
Rapid Communications in Mass Spectrometry. 16:1092-1099
A novel analytical method has been developed for direct quantification of intracellular nucleoside triphosphates (NTPs). Lysates of human peripheral blood mononuclear cells (PBMCs) were extracted by protein precipitation, and the filtered extracts we
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1a60ffcc31433686351c8c9ee805e90
https://doi.org/10.1002/rcm.684
https://doi.org/10.1002/rcm.684
Autor:
Greg Hollis, Changsheng Zheng, Hao Feng, Mei Li, Peggy Scherle, Taisheng Huang, Joseph Glenn, Chu-Biao Xue, Kris Vaddi, Lixin Shao, Brian Metcalf, Tom Emm, Nancy Contel, Ke Zhang, Ganfeng Cao, Dilip P. Modi, Lou Storace, Anlai Wang, Sharon Diamond, Robert C. Newton, Chen Lihua, Steven Friedman, Rajan Anand, Vaqar Sharief, Lingquan Kong, Hiroyuki Tanaka, Meloni David, Maryanne Covington, Michael Xia, Laurine G. Galya, Robinson Darius J, Qi Han, Swamy Yeleswaram, Yingxin Zhang
Publikováno v:
ACS medicinal chemistry letters. 2(6)
We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2cdd928778e1596e752bde06658b5662
https://pubmed.ncbi.nlm.nih.gov/24900329
https://pubmed.ncbi.nlm.nih.gov/24900329
Autor:
Gregory Hollis, Tom Emm, Joseph Glenn, Kris Vaddi, Rajan Anand, Brian Metcalf, Douglas Keller, Peggy Scherle, Chen Lihua, Ke Zhang, Ganfeng Cao, Taisheng Huang, Sharon Diamond, Kim Solomon, Robert C. Newton, Chu-Biao Xue, Jiacheng Zhou, Meloni David, Steven Friedman, Nancy Contel, Anlai Wang, Changsheng Zheng, Bitao Zhao, Swamy Yeleswaram, Hao Feng, Ling Kong, Laurine G. Galya, Fredric Baribaud, Michael Xia, Niu Shin, Mei Li
To identify a CCR5 antagonist as an HIV-1 entry inhibitor, we designed a novel series of indane derivatives based on conformational considerations. Modification on the indane ring led to the discovery of compound 22a (INCB9471) that exhibited high af
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0734e1759782a0457a497299b8c836bd
https://europepmc.org/articles/PMC4007949/
https://europepmc.org/articles/PMC4007949/
Autor:
Steve Friedman, Robert C. Newton, Wenqing Yao, D. Raghunadharao, Tom Emm, William M. Garrett, Shailesh Arjun Bondarde, Peggy Scherle, Dinesh Chandra Doval, Richard S. Levy, Swamy Yeleswaram, Shona Nag, TP Sahoo, G. Bhattacharyya, Pramod Kumar Julka, M. Walia, K. Kumar, K. T. Shenoy, P. Mohan, R. Nagarkar, D. Lokanatha, N. Narang, Jingwei Li
Publikováno v:
Cancer Research. 69:5056-5056
Background: In HER2 over-expressing breast cancer cells, the HER2 protein can be cleaved by a metalloproteinase, ADAM10. While the extracellular domain (ECD) of HER2 is released into the serum, the truncated HER2 receptor fragment, termed p95, remain
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::aad2fe07ef2b2a80a3ff15e07638d307
https://doi.org/10.1158/0008-5472.sabcs-09-5056
https://doi.org/10.1158/0008-5472.sabcs-09-5056
Publikováno v:
Pharmacology Biochemistry and Behavior. 26:313-319
Experiments were conducted in young (3–4 months) and old (24–25 months) male Fischer 344 rats to assess the effects of amitriptyline, scopolamine, and zimelidine on short term memory using an eight arm radial maze paradigm. Kinetic analyses emplo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3dc7a937665c8715cc6382b13b87d181
https://doi.org/10.1016/0091-3057(87)90124-9
https://doi.org/10.1016/0091-3057(87)90124-9