2023
Development and Pharmacochemical Characterization Discover a Novel Brain-Permeable HDAC11-Selective Inhibitor with Therapeutic Potential by Regulating Neuroinflammation in Mice
Bai P, Liu Y, Yang L, Ding W, Mondal P, Sang N, Liu G, Lu X, Ho T, Zhou Y, Wu R, Birar V, Wilks M, Tanzi R, Lin H, Zhang C, Li W, Shen S, Wang C. Development and Pharmacochemical Characterization Discover a Novel Brain-Permeable HDAC11-Selective Inhibitor with Therapeutic Potential by Regulating Neuroinflammation in Mice. Journal Of Medicinal Chemistry 2023, 66: 16075-16090. PMID: 37972387, DOI: 10.1021/acs.jmedchem.3c01491.Peer-Reviewed Original ResearchConceptsPositron emission tomographyNeuropathic painHDAC11 inhibitorsInhibition of HDAC11Histone deacetylase 11Pharmacokinetic/pharmacodynamic evaluationNeuroimmune functionMouse modelPharmacological inhibitionBrain uptakeEmission tomographyTherapeutic potentialNeurological indicationsPainTherapeutic targetHDAC11Regulating neuroinflammationNeurological disordersDrug developmentMiceInhibitorsHDAC isoformsCarbon-11Metabolic propertiesBrain
2022
A positron emission tomography imaging probe selectively targeting the BD1 bromodomain and extra-terminal domain
Bai P, Yan L, Bagdasarian F, Wilks M, Wey H, Wang C. A positron emission tomography imaging probe selectively targeting the BD1 bromodomain and extra-terminal domain. Chemical Communications 2022, 58: 9654-9657. PMID: 35943085, PMCID: PMC9618257, DOI: 10.1039/d2cc03785h.Peer-Reviewed Original ResearchConceptsPositron emission tomography imaging studiesPositron emission tomographyNon-human primatesModerate brain uptakeImaging studiesBrain uptakePositron emission tomography imaging probeEmission tomographyBrain permeabilityBrainBromodomains of BRD2Clinical translationExtra-terminal domainTranslational potentialInhibitor developmentNeurological diseasesBinding specificity