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Discovery of a small molecule targeting SET-PP2A interaction to overcome BCR-ABLT315I mutation of chronic myeloid leukemia
It is demonstrated that TGI1002 is a novel SET inhibitor with important therapeutic potential for the treatment of drug-resistant CML. Expand
Chemical Protein Synthesis by Solid Phase Ligation of Unprotected Peptide Segments
In this paper we describe “solid phase chemical ligation” (SPCL), the application of the principles of polymer-supported organic synthesis to the construction of large polypeptide chains for theExpand
Glycyrrhetinic Acid Functionalized Graphene Oxide for Mitochondria Targeting and Cancer Treatment In Vivo.
Glycyrrhetinic acid (GA), a natural product from Glycyrrhiza glabra, is found to be a novel mitochondria targeting ligand, which can improve mitochondrial permeability and enhance the drug uptake of mitochondria. Expand
Enzymatic Preparation of an (S)-Amino Acid from a Racemic Amino Acid
The (S)-amino acid, (S)-2-amino-3-(6-o-tolylpyridin-3-yl)propanoic acid (3), is a key intermediate needed for synthesis of an antidiabetic drug candidate. Three enzymatic routes to 3 were explored.Expand
Preparation of (R)-Amines from Racemic Amines with an (S)-Amine Transaminase from Bacillus megaterium
Screening was carried out to identify strains useful for the preparation of (R)-1-cyclopropylethylamine and (R)-sec-butylamine by resolution of the racemic amines with an (S)-specific transaminase.Expand
Enantioselective synthesis of ethyl (S)-2-hydroxy-4-phenylbutyrate by recombinant diketoreductase
Recombinant diketoreductase showed excellent stereoselectivity in the double reduction of β,δ-diketo esters. To investigate the substrate specificity and to broaden the applications of this newExpand
Integration of a Decrescent Transcriptome and Metabolomics Dataset of Peucedanum praeruptorum to Investigate the CYP450 and MDR Genes Involved in Coumarins Biosynthesis and Transport
This study suggested that integration of a decrescent transcriptome and metabolomics dataset could largely narrow down the number of gene to be investigated and significantly improve the efficiency of functional gene predication. Expand
Oral Delivery of Exenatide via Microspheres Prepared by Cross-Linking of Alginate and Hyaluronate
The present study demonstrated the feasibility of orally delivering exenatide with the new cross-linked biomaterial and formulation, and showed therapeutic potential for clinical applications. Expand
Stereoselective introduction of two chiral centers by a single diketoreductase: an efficient biocatalytic route for the synthesis of statin side chains
Statins, including atorvastatin (Lipitor®), are the top-selling drugs in the world. The biocatalytic production of chiral side chains of statin drugs is of great interest to academia and industry.Expand
Multiple Oxidative Routes towards the Maturation of Nosiheptide
Comparing the coding proteins NosB and NosC with other known P450 enzymes revealed remarkable similarity, including a conserved amino acid sequence, an O2 binding site, and a C-terminal heme-binding domain with the signature cysteine residue for the coordination of heme. Expand