Abstract Results 2: Results 4: Dimethyl Fumarate (DMF) α ... DOCS/Systems Biology Presenta… ·...
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α β β β α β β α Results 1 : α-NETA Selectively Inhibits CMKLR1 Signaling Results 4 : α-NETA Suppresses Clinical and Histological EAE: comparison with FDA-approved Dimethyl Fumarate Conclusions α α α α β α α α α Results 2 : α-NETA Stability, Potential Bioactive Degradation Products, and Structure- Activity Relationships Results 3 : α-NETA Selectivity α- CHO cells CMKLR1 β-arrestin:β-gal1 chemerin b-arrestin:b-gal1 Chemilluminescent Signal Substrate b-gal2 b-gal2 α α α α α Proposed Degradation Pathway of α-NETA β μ μ α-NETA 242 Da electrophile Dimethyl Fumarate (DMF) 144 Da electrophile Graham et al, PLoS One 2014 Schilling et al, Clin and Expt Immunol 2006 β α β α α α α α (A) Proposed Degradation Pathway of α-NETA (supported by MS-TOF data). (B) α-NETA stability. α-NETA was spiked into 10% mouse plasma and incubated at the indicated temperatures. At the indicated times, the samples were quenched and analyzed by mass spectrometry. The stability of Benfluorex (positive control compound) was also determined. Mean ± SD of triplicate wells for each point is displayed. (C) α α α α Abstract
Transcript of Abstract Results 2: Results 4: Dimethyl Fumarate (DMF) α ... DOCS/Systems Biology Presenta… ·...
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β β
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βα
Results 1:α-NETA Selectively Inhibits CMKLR1 Signaling
Results 4:α-NETA Suppresses Clinical and
Histological EAE: comparison with FDA-approved Dimethyl Fumarate
Conclusions
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αα
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α
αα
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Results 2:α-NETA Stability, Potential Bioactive
Degradation Products, and Structure-Activity Relationships
Results 3: α-NETA Selectivity
α-
CHO cells
CMKLR1
β-arrestin:β-gal1
chemerin
b-arrestin:b-gal1
ChemilluminescentSignal
Substrate
b-gal2
b-ga
l2
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α
α
α
α
Proposed Degradation Pathway of α-NETA
βμ
μ
α-NETA
242 Da electrophile
Dimethyl Fumarate (DMF)
144 Da electrophile
Graham et al, PLoS One 2014 Schilling et al, Clin and Expt Immunol 2006
β αβ
α
αα
α
α
(A) Proposed Degradation Pathway of α-NETA (supported by MS-TOF data). (B) α-NETA stability. α-NETA was spiked into 10% mouse plasma and incubated at the indicated temperatures. At the indicated times, the samples were quenched and analyzed by mass spectrometry. The stability of Benfluorex (positive control compound) was also determined. Mean ± SD of triplicate wells for each point is displayed. (C)
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α α
Abstract
