Xiaozheng Dou Email & Phone Number

St Louis, Missouri, United States

Lead a small molecule drug discovery project to PCC

Blagg Lab

•Performed gram-scale (>100 g) stereoselective syntheses to conduct structure-activity relationship studies of cruentaren A, a 12-membered macrocyclic lactone containing 8 stereocenters and an N-acyl allylamine side chain.•Initiated collaborations with the Rubinstein Lab at the University of Toronto to obtain a cryo-EM structure of cruentaren A bound to ATP synthase.•Synthesized >50 cruentaren A analogues via total synthesis and late-stage modification, which… Show more •Performed gram-scale (>100 g) stereoselective syntheses to conduct structure-activity relationship studies of cruentaren A, a 12-membered macrocyclic lactone containing 8 stereocenters and an N-acyl allylamine side chain.•Initiated collaborations with the Rubinstein Lab at the University of Toronto to obtain a cryo-EM structure of cruentaren A bound to ATP synthase.•Synthesized >50 cruentaren A analogues via total synthesis and late-stage modification, which resulted in a series of analogues with nanomolar activity and 2 manuscripts.•Developed isoform-selective Hsp90 inhibitors via strategies, which include structure-based drug design and photochemistry, to construct a library of complex, three-dimensional compounds with>800-fold selectivity and >100-fold improved solubility.•Designed small molecules via in-silico methods and evaluated them in fluorescence polarization assays. Show less

Norman, Oklahoma

Duerfeldt Lab

•Designed, synthesized, and evaluated more than 200peroxisomeproliferator-activated receptor alpha agonists that improved potency to 50 nM with >2700-fold isoform selectivity and resulted in a pipeline of candidates with in vivo efficacy and good pharmacokinetic properties, which leads to 3 publications, 2 patents, and an SBIR-funded start-up.•Designed and optimized of small molecules using in-silico methods and evaluated compounds in cell-based and protein-based assays… Show more •Designed, synthesized, and evaluated more than 200peroxisomeproliferator-activated receptor alpha agonists that improved potency to 50 nM with >2700-fold isoform selectivity and resulted in a pipeline of candidates with in vivo efficacy and good pharmacokinetic properties, which leads to 3 publications, 2 patents, and an SBIR-funded start-up.•Designed and optimized of small molecules using in-silico methods and evaluated compounds in cell-based and protein-based assays, such as luciferase assay, thermal shift assay, and isothermal titration calorimetry assay.•Probed >50 conditions to synthesize a key intermediate to complete a15-step total synthesis of an acyldepsipeptide derivative in 6 months.•Applied new methodologies to synthesize boronic-acid bioisosteres as covalent drugs •Probed methodologies to synthesize saturated bicyclic compounds. Show less

Norman, Oklahoma

Doctor Of Philosophy - Phd, Chemistry

Master Of Science - Ms, Organic Chemistry

Bachelor Of Engineering - Be, Chemical Engineering