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1 August 2022
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Aryl Hydrocarbon Receptor (AHR) is a transcription factor activated by multiple ligands including the metabolite kynurenine that is produced by IDO1 and TDO2 from the precursor tryptophan. Activated AHR dampens the effector function in multiple immune cells, for example, decreasing effector CD8+ T cells and increasing immune suppressive T regulatory cells and M2 macrophages leading to an overall immunosuppressive tumor microenvironment and facilitating tumor progression. IK-175 is a novel small molecule AHR antagonist that reverses the broad immunosuppressive effects of this pathway in tumors. Read the full article on page 1261. - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
MCT First Disclosures
Discovery and Characterization of a Novel Aryl Hydrocarbon Receptor Inhibitor, IK-175, and Its Inhibitory Activity on Tumor Immune Suppression
Karen McGovern; Alfredo C. Castro; Jill Cavanaugh; Silvia Coma; Meghan Walsh; Jeremy Tchaicha; Sakeena Syed; Prabitha Natarajan; Mark Manfredi; Xiaoyan M. Zhang; Jeffrey Ecsedy
Small Molecule Therapeutics
PLGA–Nano-Encapsulated Disulfiram Inhibits Hypoxia-Induced NF-κB, Cancer Stem Cells, and Targets Glioblastoma In Vitro and In Vivo
Vinodh Kannappan; Ying Liu; Zhipeng Wang; Karim Azar; Sathishkumar Kurusamy; Rajagopal S. Kilari; Angel L. Armesilla; Mark R. Morris; Mohammad Najlah; Peng Liu; Xiu-Wu Bian; Weiguang Wang
Combination of Ribociclib and Gemcitabine for the Treatment of Medulloblastoma
Allison Pribnow; Barbara Jonchere; Jingjing Liu; Kyle S. Smith; Olivia Campagne; Ke Xu; Sarah Robinson; Yogesh Patel; Arzu Onar-Thomas; Gang Wu; Clinton F. Stewart; Paul A. Northcott; Jiyang Yu; Giles W. Robinson; Martine F. Roussel
Trastuzumab Deruxtecan, Antibody–Drug Conjugate Targeting HER2, Is Effective in Pediatric Malignancies: A Report by the Pediatric Preclinical Testing Consortium
Pooja Hingorani; Wendong Zhang; Zhongting Zhang; Zhaohui Xu; Wei-Lien Wang; Michael E. Roth; Yifei Wang; Jonathan B. Gill; Douglas J. Harrison; Beverly A. Teicher; Stephen W. Erickson; Gregory Gatto; Edward A. Kolb; Malcolm A. Smith; Raushan T. Kurmasheva; Peter J. Houghton; Richard Gorlick
Large Molecule Therapeutics
Nonclinical Efficacy and Safety of CX-2029, an Anti-CD71 Probody–Drug Conjugate
Shweta Singh; Laura Serwer; Amy DuPage; Kristi Elkins; Niharika Chauhan; Matthew Ravn; Fritz Buchanan; Leyu Wang; Michael Krimm; Ken Wong; Jason Sagert; Kimberly Tipton; Stephen J. Moore; Yuanhui Huang; Andrew Jang; Eric Ureno; Adam Miller; Sarah Patrick; Shanti Duvur; Shouchun Liu; Olga Vasiljeva; Yingchun Li; Tracy Henriques; Ilaria Badagnani; Shawn Jeffries; Siew Schleyer; Rob Leanna; Claus Krebber; Sridhar Viswanathan; Luc Desnoyers; Jonathan Terrett; Marcia Belvin; Susan Morgan-Lappe; W. Michael Kavanaugh; Jennifer Richardson
Targeting Drug Resistance
GAS6-AXL Inhibition by AVB-500 Overcomes Resistance to Paclitaxel in Endometrial Cancer by Decreasing Tumor Cell Glycolysis
Shaina F. Bruce; Kevin Cho; Hollie Noia; Elena Lomonosova; Elizabeth C. Stock; Alyssa Oplt; Barbara Blachut; Mary M. Mullen; Lindsay M. Kuroki; Andrea R. Hagemann; Carolyn K. McCourt; Premal H. Thaker; Dineo Khabele; Matthew A. Powell; David G. Mutch; Leah P. Shriver; Gary J. Patti; Katherine C. Fuh
Models and Technologies
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