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Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity
Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity
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Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity

Maurer, Till ; Garrenton, Lindsay S ; Oh, Angela ; Pitts, Keith ; Anderson, Daniel J ; Skelton, Nicholas J ; Fauber, Benjamin P ; Pan, Borlan ; Malek, Shiva ; Stokoe, David ; Ludlam, Mary J. C ; Bowman, Krista K ; Wu, Jiansheng ; Giannetti, Anthony M ; Starovasnik, Melissa A ; Mellman, Ira ; Jackson, Peter K ; Rudolph, Joachim ; Wang, Weiru ; Fang, Guowei

Proceedings of the National Academy of Sciences - PNAS, 2012-04, Vol.109 (14), p.5299-5304 [Periódico revisado por pares]

United States: National Academy of Sciences

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2
Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2
Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2
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Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2

Foster, Scott A. ; Whalen, Daniel M. ; Özen, Ayşegül ; Wongchenko, Matthew J. ; Yin, JianPing ; Yen, Ivana ; Schaefer, Gabriele ; Mayfield, John D. ; Chmielecki, Juliann ; Stephens, Philip J. ; Albacker, Lee A. ; Yan, Yibing ; Song, Kyung ; Hatzivassiliou, Georgia ; Eigenbrot, Charles ; Yu, Christine ; Shaw, Andrey S. ; Manning, Gerard ; Skelton, Nicholas J. ; Hymowitz, Sarah G. ; Malek, Shiva

Cancer cell, 2016-04, Vol.29 (4), p.477-493 [Periódico revisado por pares]

United States: Elsevier Inc

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3
Identification of a Small Peptide That Inhibits PCSK9 Protein Binding to the Low Density Lipoprotein Receptor
Identification of a Small Peptide That Inhibits PCSK9 Protein Binding to the Low Density Lipoprotein Receptor
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Identification of a Small Peptide That Inhibits PCSK9 Protein Binding to the Low Density Lipoprotein Receptor

Zhang, Yingnan ; Eigenbrot, Charles ; Zhou, Lijuan ; Shia, Steven ; Li, Wei ; Quan, Clifford ; Tom, Jeffrey ; Moran, Paul ; Di Lello, Paola ; Skelton, Nicholas J. ; Kong-Beltran, Monica ; Peterson, Andrew ; Kirchhofer, Daniel

The Journal of biological chemistry, 2014-01, Vol.289 (2), p.942-955 [Periódico revisado por pares]

United States: Elsevier Inc

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4
Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists
Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists
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Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists

Zhang, Yingnan ; Ultsch, Mark ; Skelton, Nicholas J ; Burdick, Daniel J ; Beresini, Maureen H ; Li, Wei ; Kong-Beltran, Monica ; Peterson, Andrew ; Quinn, John ; Chiu, Cecilia ; Wu, Yan ; Shia, Steven ; Moran, Paul ; Di Lello, Paola ; Eigenbrot, Charles ; Kirchhofer, Daniel

Nature structural & molecular biology, 2017-10, Vol.24 (10), p.848-856 [Periódico revisado por pares]

United States: Nature Publishing Group

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5
Regions of conformational flexibility in the proprotein convertase PCSK9 and design of antagonists for LDL cholesterol lowering
Regions of conformational flexibility in the proprotein convertase PCSK9 and design of antagonists for LDL cholesterol lowering
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Regions of conformational flexibility in the proprotein convertase PCSK9 and design of antagonists for LDL cholesterol lowering

Kirchhofer, Daniel ; Burdick, Daniel J. ; Skelton, Nicholas J. ; Zhang, Yingnan ; Ultsch, Mark

Biochemical Society transactions, 2020-08, Vol.48 (4), p.1323-1336 [Periódico revisado por pares]

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6
Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models
Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models
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Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models

JIE LIN ; SAMPATH, Deepak ; LEE, Leslie B ; RISOM, Tyler ; GROSS, Stefan ; LIEDERER, Bianca M ; KOEPPEN, Hartmut ; SKELTON, Nicholas J ; WALLIN, Jeffrey J ; BELVIN, Marcia ; PUNNOOSE, Elizabeth ; FRIEDMAN, Lori S ; NANNINI, Michelle A ; KUI LIN ; LEE, Brian B ; DEGTYAREV, Michael ; OEH, Jason ; SAVAGE, Heidi ; ZHENGYU GUAN ; HONG, Rebecca ; KASSEES, Robert

Clinical cancer research, 2013-04, Vol.19 (7), p.1760-1772 [Periódico revisado por pares]

Philadelphia, PA: American Association for Cancer Research

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7
Cyanopyrrolidine Inhibitors of Ubiquitin Specific Protease 7 Mediate Desulfhydration of the Active-Site Cysteine
Cyanopyrrolidine Inhibitors of Ubiquitin Specific Protease 7 Mediate Desulfhydration of the Active-Site Cysteine
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Cyanopyrrolidine Inhibitors of Ubiquitin Specific Protease 7 Mediate Desulfhydration of the Active-Site Cysteine

Bashore, Charlene ; Jaishankar, Priyadarshini ; Skelton, Nicholas J ; Fuhrmann, Jakob ; Hearn, Brian R ; Liu, Peter S ; Renslo, Adam R ; Dueber, Erin C

ACS chemical biology, 2020-06, Vol.15 (6), p.1392-1400 [Periódico revisado por pares]

United States

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8
A Novel Inhibitor of the LolCDE ABC Transporter Essential for Lipoprotein Trafficking in Gram-Negative Bacteria
A Novel Inhibitor of the LolCDE ABC Transporter Essential for Lipoprotein Trafficking in Gram-Negative Bacteria
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A Novel Inhibitor of the LolCDE ABC Transporter Essential for Lipoprotein Trafficking in Gram-Negative Bacteria

Nickerson, Nicholas N ; Jao, Christine C ; Xu, Yiming ; Quinn, John ; Skippington, Elizabeth ; Alexander, Mary Kate ; Miu, Anh ; Skelton, Nicholas ; Hankins, Jessica V ; Lopez, Michael S ; Koth, Christopher M ; Rutherford, Steven ; Nishiyama, Mireille

Antimicrobial agents and chemotherapy, 2018-04, Vol.62 (4) [Periódico revisado por pares]

United States: American Society for Microbiology

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9
Disruption of PH–kinase domain interactions leads to oncogenic activation of AKT in human cancers
Disruption of PH–kinase domain interactions leads to oncogenic activation of AKT in human cancers
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Disruption of PH–kinase domain interactions leads to oncogenic activation of AKT in human cancers

Parikh, Chaitali ; Janakiraman, Vasantharajan ; Wu, Wen-I ; Foo, Catherine K ; Kljavin, Noelyn M ; Chaudhuri, Subhra ; Stawiski, Eric ; Lee, Brian ; Lin, Jie ; Li, Hong ; Lorenzo, Maria N ; Yuan, Wenlin ; Guillory, Joseph ; Jackson, Marlena ; Rondon, Jesus ; Franke, Yvonne ; Bowman, Krista K ; Sagolla, Meredith ; Stinson, Jeremy ; Wu, Thomas D ; Wu, Jiansheng ; Stokoe, David ; Stern, Howard M ; Brandhuber, Barbara J ; Lin, Kui ; Skelton, Nicholas J ; Seshagiri, Somasekar

Proceedings of the National Academy of Sciences - PNAS, 2012-11, Vol.109 (47), p.19368-19373 [Periódico revisado por pares]

United States: National Academy of Sciences

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10
Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors
Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors
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Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors

Blake, James F ; Xu, Rui ; Bencsik, Josef R ; Xiao, Dengming ; Kallan, Nicholas C ; Schlachter, Stephen ; Mitchell, Ian S ; Spencer, Keith L ; Banka, Anna L ; Wallace, Eli M ; Gloor, Susan L ; Martinson, Matthew ; Woessner, Richard D ; Vigers, Guy P.A ; Brandhuber, Barbara J ; Liang, Jun ; Safina, Brian S ; Li, Jun ; Zhang, Birong ; Chabot, Christine ; Do, Steven ; Lee, Leslie ; Oeh, Jason ; Sampath, Deepak ; Lee, Brian B ; Lin, Kui ; Liederer, Bianca M ; Skelton, Nicholas J

Journal of medicinal chemistry, 2012-09, Vol.55 (18), p.8110-8127 [Periódico revisado por pares]

United States: American Chemical Society

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