Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay

PLoS ONE

Volumn 12, Issue 9, 2017, Pages

  Hall, Justin ^a   Brault, Amy ^a   Vincent, Fabien ^a   Weng, Shawn ^a   Wang, Hong ^a   Dumlao, Darren ^a   Aulabaugh, Ann ^a   Aivazian, Dikran ^a   Castro, Dana ^a   Chen, Ming ^a   Culp, Jeffrey ^a   Dower, Ken ^a   Gardner, Joseph ^a   Hawrylik, Steven ^a   Golenbock, Douglas ^b   Hepworth, David ^a   Horn, Mark ^a   Jones, Lyn ^a   Jones, Peter ^a   Latz, Eicke ^b,c   Li, Jing ^a   Lin, Lih Ling ^a   Lin, Wen ^a   Lin, David ^a   Lovering, Frank ^a   Niljanskul, Nootaree ^a   Nistler, Ryan ^a   Pierce, Betsy ^a   Plotnikova, Olga ^a   Schmitt, Daniel ^a   Shanker, Suman ^a   Smith, James ^a   Snyder, William ^a   Subashi, Timothy ^a   Trujillo, John ^a   Tyminski, Edyta ^a   Wang, Guoxing ^a   Wong, Jimson ^a   Lefker, Bruce ^a   Dakin, Leslie ^a   Leach, Karen ^a   more..

^a PFIZER INC   (United States)

^b UNIVERSITY OF MASSACHUSETTS MEDICAL SCHOOL   (United States)

^c UNIVERSITY HOSPITAL BONN   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIC GMP; CYCLIC GMP AMPA SYNTHASE; MONOCLONAL ANTIBODY; PF 06928215; UNCLASSIFIED DRUG; ANTIBODY; CYCLIC GUANOSINE MONOPHOSPHATE-ADENOSINE MONOPHOSPHATE; CYCLIC NUCLEOTIDE; ENZYME INHIBITOR; MB21D1 PROTEIN, HUMAN; NONSTEROID ANTIINFLAMMATORY AGENT; NUCLEOTIDYLTRANSFERASE; PF-06928215; PROTEIN BINDING; PYRAZOLE DERIVATIVE; PYRIMIDINE DERIVATIVE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANTIBODY AFFINITY; ANTIBODY TITER; ARTICLE; BINDING AFFINITY; CELL VIABILITY; CONCENTRATION RESPONSE; CROSS REACTION; DRUG CYTOTOXICITY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME BINDING; ENZYME SUBSTRATE; FLUORESCENCE POLARIZATION; HYDROPHOBICITY; IC50; IMMUNE RESPONSE; INNATE IMMUNITY; MASS SPECTROMETRY; MOUSE; NONHUMAN; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; DRUG DEVELOPMENT; ENZYME LINKED IMMUNOSORBENT ASSAY; HUMAN; IMMUNOLOGY; METABOLISM; MOLECULAR MODEL; SYNTHESIS;

ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; ANTIBODIES; DRUG DISCOVERY; ENZYME INHIBITORS; ENZYME-LINKED IMMUNOSORBENT ASSAY; FLUORESCENCE POLARIZATION; HUMANS; MASS SPECTROMETRY; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NUCLEOTIDES, CYCLIC; NUCLEOTIDYLTRANSFERASES; PROTEIN BINDING; PYRAZOLES; PYRIMIDINES;

EID: 85029726822     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0184843     Document Type: Article

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