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1.
Chembiochem ; 22(4): 705-711, 2021 02 15.
Article in English | MEDLINE | ID: mdl-32991036

ABSTRACT

A method for producing buta-1,3-diene (1,3-BD) by an amalgamation of chemical and biological approaches with syngas as the carbon source is proposed. Syngas is converted to the central intermediate, acetyl-CoA, by microorganisms through a tetrahydrofolate metabolism pathway. Acetyl-CoA is subsequently converted to malonyl-CoA using a carbonyl donor in the presence of a carboxylase enzyme. A decarboxylative Claisen condensation of malonyl-CoA and acetaldehyde ensues in the presence of acyltransferases to form 3-hydroxybutyryl-CoA, which is subsequently reduced by aldehyde reductase to give butane-1,3-diol (1,3-BDO). An ensuing dehydration step converts 1,3-BDO to 1,3-BD in the presence of a chemical dehydrating reagent.


Subject(s)
Acyltransferases/metabolism , Biomass , Butadienes/chemical synthesis , Carbon/chemistry , Gases/chemistry , Zeolites/chemistry , Decarboxylation , Dehydration , Kinetics
2.
Beilstein J Org Chem ; 16: 628-637, 2020.
Article in English | MEDLINE | ID: mdl-32318119

ABSTRACT

Guided by computational analysis, herein we report the design, synthesis and evaluation of four novel diazine-based histone deacetylase inhibitors (HDACis). The targets of interest (TOI) are analogues of panobinostat, one of the most potent and versatile HDACi reported. By simply replacing the phenyl core of panobinostat with that of a diazine derivative, docking studies against HDAC2 and HDAC8 revealed that the four analogues exhibit inhibition activities comparable to that of panobinostat. Multistep syntheses afforded the visualized targets TOI1, TOI2, TOI3-rev and TOI4 whose biological evaluation confirmed the strength of HDAC8 inhibition with TOI4 displaying the greatest efficacy at varying concentrations. The results of this study lay the foundation for future design strategies toward more potent HDACis for HDAC8 isozymes and further therapeutic applications for neuroblastoma.

3.
Nat Commun ; 10(1): 1111, 2019 03 07.
Article in English | MEDLINE | ID: mdl-30846702

ABSTRACT

Activated macrophages have the potential to be ideal targets for imaging inflammation. However, probe selectivity over non-activated macrophages and probe delivery to target tissue have been challenging. Here, we report a small molecule probe specific for activated macrophages, called CDg16, and demonstrate its application to visualizing inflammatory atherosclerotic plaques in vivo. Through a systematic transporter screen using a CRISPR activation library, we identify the orphan transporter Slc18b1/SLC18B1 as the gating target of CDg16.


Subject(s)
Cation Transport Proteins/metabolism , Inflammation/diagnostic imaging , Inflammation/immunology , Macrophage Activation , Acridines , Animals , CRISPR-Cas Systems , HeLa Cells , Humans , Inflammation/metabolism , Mice , Mice, Knockout, ApoE , Molecular Probe Techniques , Molecular Probes , Plaque, Atherosclerotic/diagnostic imaging , Plaque, Atherosclerotic/immunology , Plaque, Atherosclerotic/metabolism , RAW 264.7 Cells
4.
Carbohydr Res ; 358: 23-30, 2012 Sep 01.
Article in English | MEDLINE | ID: mdl-22863364

ABSTRACT

D-gluco-configured building block derived from D-(+)-gluconolactone has served as a common chiral template for the synthesis of enantiopure D- and L-xylo-configured 1,2,3,4-alkane tetrols. This has enabled synthesis of medicinally important guggultetrols and their enantiomers from a common starting point. Wittig and Grignard reactions are the key steps used for the incorporation of lipophilic chain.


Subject(s)
Gluconates/chemistry , Lactones/chemistry , Sugar Alcohols/chemistry , Sugar Alcohols/chemical synthesis , Molecular Structure , Stereoisomerism
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