Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis

Journal of Medicinal Chemistry

Volumn 61, Issue 17, 2018, Pages 7862-7876

  Miller, Mark ^a   Pal, Arindom ^a   Albusairi, Wabel ^a   Joo, Hyun ^a   Pappas, Beverly ^a   Haque Tuhin, Md Tariqul ^a   Liang, Dengpan ^a   Jampala, Raghavendra ^a   Liu, Fang ^a   Khan, Jared ^a   Faaij, Marjon ^a   Park, Miki ^a   Chan, William ^a   Graef, Isabella ^b   Zamboni, Robert ^c   Kumar, Neil ^c   Fox, Jonathan ^c   Sinha, Uma ^c   Alhamadsheh, Mamoun ^a  

^a UNIVERSITY OF THE PACIFIC   (United States)

^b STANFORD UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c Eidos Therapeutics Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AG10; PROTEIN INHIBITOR; TRANSTHYRETIN; UNCLASSIFIED DRUG; 3-(3-(3,5-DIMETHYL-1H-PYRAZOL-4-YL)PROPOXY)-4-FLUOROBENZOIC ACID; BENZOIC ACID; HUMAN SERUM ALBUMIN; PYRAZOLE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; ATTR AMYLOIDOSIS; BEAGLE; BINDING AFFINITY; CRYSTAL STRUCTURE; ENTHALPY; FEMALE; GENETIC VARIABILITY; HYDROGEN BOND; IN VIVO STUDY; ISOTHERMAL TITRATION CALORIMETRY; MALE; MAXIMUM CONCENTRATION; MOLECULAR INTERACTION; NONHUMAN; PHARMACODYNAMICS; PROTEIN STABILITY; SERUM; SYNTHESIS; THERMODYNAMICS; TROUGH CONCENTRATION; ANIMAL; BIOMIMETICS; CHEMISTRY; DOG; ENTROPY; FAMILIAL AMYLOID POLYNEUROPATHY; GENETICS; HUMAN; METABOLISM; MOLECULAR MODEL; MUTATION; ORAL DRUG ADMINISTRATION; PATHOLOGY; PROTEIN CONFORMATION;

ADMINISTRATION, ORAL; AMYLOID NEUROPATHIES, FAMILIAL; ANIMALS; BENZOATES; BIOMIMETICS; DOGS; ENTROPY; FEMALE; HUMANS; MALE; MODELS, MOLECULAR; MUTATION; PREALBUMIN; PROTEIN CONFORMATION; PROTEIN STABILITY; PYRAZOLES; SERUM ALBUMIN, HUMAN; THERMODYNAMICS;

EID: 85052958825     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.8b00817     Document Type: Article

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