Lei Yang, PhD
Cards
About
Research
Publications
2024
Development of an Orally Bioavailable LCK PROTAC Degrader as a Potential Therapeutic Approach to T‑Cell Acute Lymphoblastic Leukemia
Jarusiewicz J, Yoshimura S, Actis M, Li Y, Fu X, Yang L, Narina S, Pruett-Miller S, Zhou S, Wang X, High A, Nishiguchi G, Yang J, Rankovic Z. Development of an Orally Bioavailable LCK PROTAC Degrader as a Potential Therapeutic Approach to T‑Cell Acute Lymphoblastic Leukemia. Journal Of Medicinal Chemistry 2024 PMID: 38973320, DOI: 10.1021/acs.jmedchem.4c00481.Peer-Reviewed Original ResearchAntitrypanosomal Chloronitrobenzamides
Carrillo A, Kadayat T, Hwang J, Chen Y, Zhu F, Holbrook G, Gillingwater K, Connelly M, Yang L, Kaiser M, Guy R. Antitrypanosomal Chloronitrobenzamides. Journal Of Medicinal Chemistry 2024, 67: 3437-3447. PMID: 38363074, DOI: 10.1021/acs.jmedchem.3c01680.Peer-Reviewed Original ResearchDevelopment of 2nd generation aminomethyl spectinomycins that overcome native efflux in Mycobacterium abscessus
Phelps G, Cheramie M, Fernando D, Selchow P, Meyer C, Waidyarachchi S, Dharuman S, Liu J, Meuli M, Dal Molin M, Killam B, Murphy P, Reeve S, Wilt L, Anderson S, Yang L, Lee R, Temrikar Z, Lukka P, Meibohm B, Polikanov Y, Hobbie S, Böttger E, Sander P, Lee R. Development of 2nd generation aminomethyl spectinomycins that overcome native efflux in Mycobacterium abscessus. Proceedings Of The National Academy Of Sciences Of The United States Of America 2024, 121: e2314101120. PMID: 38165935, PMCID: PMC10786304, DOI: 10.1073/pnas.2314101120.Peer-Reviewed Original ResearchConceptsIntrinsic drug resistanceMurine infection modelMechanism of actionAntimycobacterial regimensNontuberculous mycobacterial speciesPoor outcomeNTM infectionTherapy resultsAminomethyl spectinomycinsRobust efficacyPharmacokinetic profileMycobacterium abscessusClinical isolatesDrug resistanceInfection modelEfflux mechanismRibosomal inhibitionCurrent standardMycobacterial strainsIntracellular concentrationSpectinomycinNative effluxEfficacyMycobacterial speciesEfflux
2023
A bromodomain-independent mechanism of gene regulation by the BET inhibitor JQ1: direct activation of nuclear receptor PXR
Huber A, Poudel S, Wu J, Miller D, Lin W, Yang L, Bwayi M, Rimmer M, Gee R, Seetharaman J, Chai S, Chen T. A bromodomain-independent mechanism of gene regulation by the BET inhibitor JQ1: direct activation of nuclear receptor PXR. Nucleic Acids Research 2023, 52: 1661-1676. PMID: 38084912, PMCID: PMC10899790, DOI: 10.1093/nar/gkad1175.Peer-Reviewed Original ResearchConceptsPregnane X receptorGenes encoding drug-metabolizing enzymesMechanisms of gene regulationBET inhibitorsDrug metabolism genesGene regulationCo-crystal structureMetabolic genesNuclear receptor pregnane X receptorBET inhibitor JQ1Liver cell modelDrug-metabolizing enzymesBiological functionsDrug development effortsBET functionNuclear receptorsPXR-dependentInhibitor JQ1JQ1X receptorTranscriptionGenesAgonist of pregnane X receptorCYP3A4 expressionCell modelA high-throughput quality control method for assessing the serial dilution performance of dose–response plates with acoustic ejection mass spectrometry
Rimmer M, Twarog N, Li Y, Shelat A, Rankovic Z, Yang L. A high-throughput quality control method for assessing the serial dilution performance of dose–response plates with acoustic ejection mass spectrometry. SLAS TECHNOLOGY 2023, 29: 100115. PMID: 37925158, DOI: 10.1016/j.slast.2023.10.007.Peer-Reviewed Original Research