Synthesis and characterization of a BODIPY-labeled derivative of Soraphen A that binds to acetyl-CoA carboxylase.
BODIPY-labeled Soraphen A derivative 4 was synthesized and characterized as an acetyl-CoA carboxylase (ACC) binder. Biophysical measurements indicate that the molecule binds in the biotin carboxylase domain where Soraphen A has been shown to bind. The fluorescent label of the BODIPY can be used to biophysically identify a compound that binds to the Soraphen A site of the biotin carboxylase domain versus the carboxytransferase domain of ACC.
Novartis Institutes for BioMedical Research, Cambridge, MA 02139, United States. brian.raymer@novartis.com
Brian
B
Raymer
Michael
M
Kavana
Allen
A
Price
Bing
B
Wang
Lisa
L
Corcoran
Raviraj
R
Kulathila
James
J
Groarke
Theirry
T
Mann
D000103:Acetyl-CoA Carboxylase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D001665:Binding Sites; D001896:Boron Compounds / Q000138:chemical synthesis / Q000737:chemistry*; D018360:Crystallography, X-Ray; D018942:Macrolides / Q000138:chemical synthesis / Q000737:chemistry*; D017434:Protein Structure, Tertiary
C095489:4,4-difluoro-4-bora-3a,4a-diaza-s-indacene; D001896:Boron Compounds; D018942:Macrolides; C086151:soraphen A; D000103:Acetyl-CoA Carboxylase