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Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Tr

Journal Article · · J. Med. Chem.
Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
DOE Contract Number:
NONE;
OSTI ID:
1869980
Journal Information:
J. Med. Chem., Journal Name: J. Med. Chem. Journal Issue: (7) Vol. 65
Country of Publication:
United States
Language:
ENGLISH

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Evaluation of fluorescence-based thermal shift assays for hit identification in drug discovery journal September 2004
Cyclic [G(2′,5′)pA(3′,5′)p] Is the Metazoan Second Messenger Produced by DNA-Activated Cyclic GMP-AMP Synthase journal May 2013
Direct Activation of STING in the Tumor Microenvironment Leads to Potent and Systemic Tumor Regression and Immunity journal May 2015
STING-Dependent Cytosolic DNA Sensing Promotes Radiation-Induced Type I Interferon-Dependent Antitumor Immunity in Immunogenic Tumors journal November 2014
Cyclic GMP-AMP Containing Mixed Phosphodiester Linkages Is An Endogenous High-Affinity Ligand for STING journal July 2013
Targeting Stimulator of Interferon Genes (STING): A Medicinal Chemistry Perspective journal December 2019
Discovery of a Novel cGAMP Competitive Ligand of the Inactive Form of STING journal December 2018
Novel Applications of Biocatalysis to Stereochemistry Determination of 2′3′-cGAMP Bisphosphorothioate (2′3′-cG S A S MP) journal June 2020
Thermodynamic Stability of Carbonic Anhydrase:  Measurements of Binding Affinity and Stoichiometry Using ThermoFluor journal April 2005
Accurate and Reliable Prediction of Relative Ligand Binding Potency in Prospective Drug Discovery by Way of a Modern Free-Energy Calculation Protocol and Force Field journal February 2015
One-Flask Syntheses of c-di-GMP and the [ R p , R p ] and [ R p , S p ] Thiophosphate Analogues journal July 2010
Combinations take centre stage in PD1/PDL1 inhibitor clinical trials journal November 2020
Hydrolysis of 2′3′-cGAMP by ENPP1 and design of nonhydrolyzable analogs journal October 2014
Regulation and function of the cGAS–STING pathway of cytosolic DNA sensing journal September 2016
STING: infection, inflammation and cancer journal November 2015
STING signaling and host defense against microbial infection journal December 2019
Approaches to treat immune hot, altered and cold tumours with combination immunotherapies journal January 2019
A kinase-cGAS cascade to synthesize a therapeutic STING activator journal March 2022
Comprehensive analysis of the clinical immuno-oncology landscape journal January 2018
An orally available non-nucleotide STING agonist with antitumor activity journal August 2020
Immunotherapy with a sting journal August 2020
2′F-Arabinonucleic acids (2′F-ANA) — History, properties, and new frontiers journal July 2008

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