Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties

Michael J.  Soth; Kang  Le; Maria Emilia  Di FrancescoMatthew M.  HamiltonGang  LiuJason P.  BurkeChris L.  CarrollJeffrey J.  KovacsJennifer P.  BardenhagenChristopher A.  BristowMario  CardozoBarbara  CzakoElisa  de StanchinaNingping  FengJill R.  GarveyJason P.  GayMary K. Geck  DoJennifer  GreerMichelle  HanAngela  HarrisZachary  HerreraSha  HuangVirginia  GiulianiYongying  JiangSarah B.  JohnsonTroy A.  JohnsonZhijun  KangPaul G.  LeonardZhen  LiuTimothy  McAfoosMeredith  MillerPietro  MorlacchiRobert A.  MullinaxWylie S.  PalmerJihai  PangNorma  RogersCharles M.  RudinHannah E.  ShepardNakia D.  SpencerJay  TheroffQi  WuAlan  XuJu Anne  YauGiulio  DraettaCarlo  ToniattiTimothy P.  HeffernanPhilip  Jones

首页> 外文期刊>Journal of Medicinal Chemistry >Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties

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Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties

机译：Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties

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Inhibition of glutaminase-1 (GLS-1) hampers the proliferation of tumor cells reliant on glutamine. Known glutaminase inhibitors have potential limitations, and in vivo exposures are potentially limited due to poor physicochemical properties. We initiated a GLS-1 inhibitor discovery program focused on optimizing physicochemical and pharmacokinetic properties, and have developed a new selective inhibitor, compound 27 (IPN60090), which is currently in phase 1 clinical trials. Compound 27 attains high oral exposures in preclinical species, with strong in vivo target engagement, and should robustly inhibit glutaminase in humans.

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《Journal of Medicinal Chemistry》 |2020年第21期|12957-12977|共21页
作者
Michael J. Soth; Kang Le; Maria Emilia Di FrancescoMatthew M. HamiltonGang LiuJason P. BurkeChris L. CarrollJeffrey J. KovacsJennifer P. BardenhagenChristopher A. BristowMario CardozoBarbara CzakoElisa de StanchinaNingping FengJill R. GarveyJason P. GayMary K. Geck DoJennifer GreerMichelle HanAngela HarrisZachary HerreraSha HuangVirginia GiulianiYongying JiangSarah B. JohnsonTroy A. JohnsonZhijun KangPaul G. LeonardZhen LiuTimothy McAfoosMeredith MillerPietro MorlacchiRobert A. MullinaxWylie S. PalmerJihai PangNorma RogersCharles M. RudinHannah E. ShepardNakia D. SpencerJay TheroffQi WuAlan XuJu Anne YauGiulio DraettaCarlo ToniattiTimothy P. HeffernanPhilip Jones;
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作者单位

Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center;

Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center;

Antitumor Assessment Core Facility—Molecular Pharmacology Program, Memorial Sloan Kettering Cancer CenterDrunkenmiller Center for Lung Cancer Research, Memorial Sloan Kettering Cancer Center;

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Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties

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