George S. Sheppard - Publications, H-index & Citations

George S. Sheppard

AbbVie

28H指数

157论文数

3.6K被引数

收录论文 27

发表时间

Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2020-04-23

PREAI

Sheppard, George S.; Wang, Le; Fidanze, Steven D.; Hasvold, Lisa A.; Liu, Dachun; Pratt, John K.; Park, Chang H.; Longenecker, Kenton; Qiu, Wei; Torrent, Maricel; Kovar, Peter J.; Bui, Mai; Faivre, Emily; Huang, Xiaoli; Lin, Xiaoyu; Wilcox, Denise; Zhang, Lu; Shen, Yu; Albert, Daniel H.; Magoc, Terrance J.; Rajaraman, Ganesh; Kati, Warren M.; McDaniel, Keith F.

Discovery of ABBV-744, a first-in-class highly BDII-selective BET bromodomain inhibitor

CANCER RESEARCH

IF16.6

2018-07-01

PREAI

Sheppard, George S.; Wang, Le; Fidanze, Steven D.; Hasvold, Lisa A.; Liu, Dachun; Pratt, John K.; Park, Chang H.; Bui, Mai-Ha; Faivre, Emily J.; Huang, Xiaoli; Lin, Xiaoyu; Wilcox, Denise M.; Shen, Yu; Albert, Daniel H.; Magoc, Terrance J.; Rajaraman, Ganesh; Kati, Warren M.; McDaniel, Keith F.

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2017-10-12

125

PREAI

McDaniel, Keith F.; Wang, Le; Soltwedel, Todd; Fidanze, Steven D.; Hasvold, Lisa A.; Liu, Dachun; Mantei, Robert A.; Pratt, John K.; Sheppard, George S.; Bui, Mai H.; Faivre, Emily J.; Huang, Xiaoli; Li, Leiming; Lin, Xiaoyu; Wang, Rongqi; Warder, Scott E.; Wilcox, Denise; Albert, Daniel H.; Magoc, Terrance J.; Rajaraman, Ganesh; Park, Chang H.; Hutchins, Charles W.; Shen, Jianwei J.; Edalji, Rohinton P.; Sun, Chaohong C.; Martin, Ruth; Gao, Wenqing; Wong, Shekman; Fang, Guowei; Elmore, Steven W.; Shen, Yu; Kati, Warren M.

Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

CANCER RESEARCH

IF16.6

2017-05-31

113

OAAI

Bui, Mai H.; Lin, Xiaoyu; Albert, Daniel H.; Li, Leiming; Lam, Lloyd T.; Faivre, Emily J.; Warder, Scott E.; Huang, Xiaoli; Wilcox, Denise; Donawho, Cherrie K.; Sheppard, George S.; Wang, Le; Fidanze, Steve; Pratt, John K.; Liu, Dachun; Hasvold, Lisa; Uziel, Tamar; Lu, Xin; Kohlhapp, Fred; Fang, Guowei; Elmore, Steven W.; Rosenberg, Saul H.; McDaniel, Keith F.; Kati, Warren M.; Shen, Yu

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2017-04-21

OAAI

Wang, Le; Pratt, John K.; Soltwedel, Todd; Sheppard, George S.; Fidanze, Steven D.; Liu, Dachun; Hasvold, Lisa A.; Mantei, Robert A.; Holms, James H.; McClellan, William J.; Wendt, Michael D.; Wada, Carol; Frey, Robin; Hansen, T. Matthew; Hubbard, Robert; Park, Chang H.; Li, Leiming; Magoc, Terrance J.; Albert, Daniel H.; Lin, Xiaoyu; Warder, Scott E.; Kovar, Peter; Huang, Xiaoli; Wilcox, Denise; Wang, Rongqi; Rajaraman, Ganesh; Petros, Andrew M.; Hutchins, Charles W.; Panchal, Sanjay C.; Sun, Chaohong; Elmore, Steven W.; Shen, Yu; Kati, Warren M.; McDaniel, Keith F.

ABBV-075, a novel BET family bromodomain inhibitor, represents a promising therapeutic agent for a broad spectrum of cancer indications

CANCER RESEARCH

IF16.6

2016-07-15

PREAI

Sarthy, Aparna; Li, Leiming; Albert, Daniel H.; Lin, Xiaoyu; Scott, Warder; Faivre, Emily; Bui, Mai H.; Huang, Xiaoli; Wilcox, Denise M.; Magoc, Terry; Buchanan, Fritz G.; Tapang, Paul; Sheppard, George S.; Le Wang; Fidanze, Steve D.; Pratt, John; Liu, Dachun; Hasvold, Lisa; Hessler, Paul; Uziel, Tamar; Lam, Lloyd; Rajaraman, Ganesh; Fang, Guowei; Elmore, Steven W.; Rosenberg, Saul H.; McDaniel, Keith; Kati, Warren; Shen, Yu

Functional group elaboration of a low molecular weight fragment to yield the novel BET family bromodomain inhibitor ABBV-075

CANCER RESEARCH

IF16.6

2016-07-15

PREAI

McDaniel, Keith; Le Wang; Sheppard, George; Fidanze, Steve; Pratt, John; Liu, Dachun; Hasvold, Lisa; Mantei, Robert; Park, Chang; Sarthy, Aparna; Li, Leiming; Albert, Daniel H.; Lin, Xiaoyu; Warder, Scott; Faivre, Emily; Bui, Mai H.; Huang, Xiaoli; Wilcox, Denise; Wang, Rongqi; Magoc, Terry; Rajaraman, Ganesh; Petros, Andrew; Panchal, Sanjay; Sun, Chaohong; Fang, Guowei; Elmore, Steven W.; Rosenberg, Saul; Shen, Yu; Kati, Warren

MCL-1 Is a Key Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency Utilizing a Highly Selective Small Molecule Inhibitor

MOLECULAR CANCER THERAPEUTICS

IF5.5

2015-08-05

107

OAAI

Xiao, Yu; Nimmer, Paul; Sheppard, George S.; Bruncko, Milan; Hessler, Paul; Lu, Xin; Roberts-Rapp, Lisa; Pappano, William N.; Elmore, Steven W.; Souers, Andrew J.; Leverson, Joel D.; Phillips, Darren C.

Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity (vol 58, pg 2180, 2015)

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2015-05-01

PREAI

Bruncko, Milan; Wang, Le; Sheppard, George S.; Phillips, Darren C.; Tahir, Stephen K.; Xue, John; Erickson, Scott; Fidanze, Steve; Fry, Elizabeth; Hasvold, Lisa; Jenkins, Gary J.; Jin, Sha; Judge, Russell A.; Kovar, Peter J.; Madar, David; Nimmer, Paul; Park, Chang; Petros, Andrew M.; Rosenberg, Saul H.; Smith, Morey L.; Song, Xiaohong; Sun, Chaohong; Tao, Zhi-Fu; Wang, Xilu; Xiao, Yu; Zhang, Haichao; Tse, Chris; Leverson, Joel D.; Elmore, Steven W.; Souers, Andrew J.

Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2015-02-26

158

PREAI

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax)

CELL DEATH & DISEASE

IF9.6

2015-01-15

431

OAAI

Leverson, J. D.; Zhang, H.; Chen, J.; Tahir, S. K.; Phillips, D. C.; Xue, J.; Nimmer, P.; Jin, S.; Smith, M.; Xiao, Y.; Kovar, P.; Tanaka, A.; Bruncko, M.; Sheppard, G. S.; Wang, L.; Gierke, S.; Kategaya, L.; Anderson, D. J.; Wong, C.; Eastham-Anderson, J.; Ludlam, M. J. C.; Sampath, D.; Fairbrother, W. J.; Wertz, I.; Rosenberg, S. H.; Tse, C.; Elmore, S. W.; Souers, A. J.

A Selective Small Molecule Inhibitor of Mcl-1 Induces Bak Dependent Apoptosis in Cancer Cell Lines

EUROPEAN JOURNAL OF CANCER

IF7.1

2012-11-01

PREAI

Phillips, D. C.; Xiao, Y.; Bruncko, M.; Park, C.; Zhang, H.; Wang, L.; Sheppard, G. S.; Elmore, S. W.; Leverson, J.; Souers, A.

Imidazo[2,1-b]thiazole and imidazo[1,2-a]pyridine amides as novel inhibitors of the insulin-like growth factor (IGF1R) and members of the epidermal growth factor family of tyrosine kinases

MOLECULAR CANCER THERAPEUTICS

IF5.5

2009-12-01

PREAI

Fidanze, Steve D.; Erickson, Scott A.; Hubbard, Robert D.; Wang, Gary T.; Mantei, Robert A.; BaMaung, Nwe Y.; Clark, Richard F.; Sorensen, Bryan K.; Koval-, Peter; Pappano, William; Zhang, Qian; Wilsbacher, Julie L.; Hu, Xiaoming; Tucker, Lora A.; Cheng, Min; Swinger, Kerren K.; Stewart, Kent D.; Wang, Jieyi; Bell, Randy L.; Davidsen, Steven K.; Sheppard, George S.

Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multitargeted inhibitors targeting insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor tyrosine kinases

MOLECULAR CANCER THERAPEUTICS

IF5.5

2009-12-01

PREAI

Wang, Gary T.; Mantel, Robert A.; Hubbard, Robert D.; Wilsbacher, Julie L.; Zhang, Qian; Tucker, Lora; Hu, Xiaoming; Kovar, Peter; Johson, Erick F.; Osterling, Donald J.; Bouska, Jennifer; Wang, Jieyi; Bell, Randy L.; Davidsen, Steven K.; Sheppard, George S.

Reversal of oncogene transformation and suppression of tumor growth by the novel IGF1R kinase inhibitor A-928605

BMC CANCER

IF3.4

2009-09-04

OAAI

Pappano, William N.; Jung, Paul M.; Meulbroek, Jonathan A.; Wang, Yi-Chun; Hubbard, Robert D.; Zhang, Qian; Grudzien, Meagan M.; Soni, Niru B.; Johnson, Eric F.; Sheppard, George S.; Donawho, Cherrie; Buchanan, Fritz G.; Davidsen, Steven K.; Bell, Randy L.; Wang, Jieyi

Discovery, Identification, and Characterization of Candidate Pharmacodynamic Markers of Methionine Aminopeptidase-2 Inhibition

JOURNAL OF PROTEOME RESEARCH

IF3.6

2008-10-02

PREAI

Warder, Scott E.; Tucker, Lora A.; McLoughlin, Shaun M.; Strelitzer, Tamara J.; Meuth, Joseph L.; Zhang, Qian; Sheppard, George S.; Richardson, Paul L.; Lesniewski, Rick; Davidsen, Steven K.; Bell, Randy L.; Rogers, John C.; Wang, Jieyi

Insulin-like growth factor-1 receptor and ErbB kinase inhibitor combinations block proliferation and induce apoptosis through cyclin D1 reduction and Bax activation

JOURNAL OF BIOLOGICAL CHEMISTRY

IF3.9

2008-08-01

OAAI

Wilsbacher, Julie L.; Zhang, Qian; Tucker, Lora A.; Hubbard, Robert D.; Sheppard, George S.; Bamaung, Nwe Y.; Fidanze, Steve D.; Wang, Gary T.; Hu, Xiaoming; Davidsen, Steven K.; Bell, Randy L.; Wang, Jieyi

Correlation of tumor growth suppression and methionine aminopetidase-2 activity blockade using an orally active inhibitor

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

IF9.1

2008-02-12

OAAI

Wang, Jieyi; Tucker, Lora A.; Stavropoulos, Jason; Zhang, Qian; Wang, Yi-Chun; Bukofzer, Gail; Niquette, Amanda; Meulbroek, Jonathan A.; Barnes, David M.; Shen, Jianwei; Bouska, Jennifer; Donawho, Cherrie; Sheppard, George S.; Bell, Randy L.

Ectopic expression of methionine aminopeptidase-2 causes cell transformation and stimulates proliferation

ONCOGENE

IF7.3

2008-02-11

PREAI

Tucker, L. A.; Zhang, Q.; Sheppard, G. S.; Lou, P.; Jiang, F.; McKeegan, E.; Lesniewski, R.; Davidsen, S. K.; Bell, R. L.; Wang, J.

Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: A structural basis for the reduction of albumin binding

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2006-06-08

PREAI

Sheppard, George S.; Wang, Jieyi; Kawai, Megumi; Fidanze, Steve D.; BaMaung, Nwe Y.; Erickson, Scott A.; Barnes, David M.; Tedrow, Jason S.; Kolaczkowski, Lawrence; Vasudevan, Anil; Park, David C.; Wang, Gary T.; Sanders, William J.; Mantei, Robert A.; Palazzo, Fabio; Tucker-Garcia, Lora; Lou, Pingping; Zhang, Qian; Park, Chang H.; Kim, Ki H.; Petros, Andrew; Olejniczak, Edward; Nettesheim, David; Hajduk, Phillip; Henkin, Jack; Lesniewski, Richard; Davidsen, Steven K.; Bell, Randy L.

研究方向