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Literature DB >> 35300081

Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.

Lisa J Alcock¹, Yunchao Chang¹, Jamie A Jarusiewicz², Marisa Actis², Stanley Nithianantham², Anand Mayasundari², Jaeki Min², Dylan Maxwell³, Jeremy Hunt³, Brandon Smart³, Jun J Yang³, Gisele Nishiguchi², Marcus Fischer^2,4, Charles G Mullighan^1,5, Zoran Rankovic².

Abstract

Aberrant activation of the JAK-STAT signaling pathway has been implicated in the pathogenesis of a range of hematological malignancies and autoimmune disorders. Here we describe the design, synthesis, and characterization of JAK2/3 PROTACs utilizing a phenyl glutarimide (PG) ligand as the cereblon (CRBN) recruiter. SJ10542 displayed high selectivity over GSPT1 and other members of the JAK family and potency in patient-derived ALL cells containing both JAK2 fusions and CRLF2 rearrangements.

Entities: Chemical

Year: 2022 PMID： 35300081 PMCID： PMC8919382 DOI： 10.1021/acsmedchemlett.1c00650

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

26 in total

1. Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders.

Authors: Jiuling Yang; Yangbing Li; Angelo Aguilar; Zhaomin Liu; Chao-Yie Yang; Shaomeng Wang
Journal: J Med Chem Date: 2019-10-21 Impact factor: 7.446

2. Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs.

Authors: Rishi R Shah; Joanna M Redmond; Andrei Mihut; Malini Menon; John P Evans; John A Murphy; Michelle A Bartholomew; Diane M Coe
Journal: Bioorg Med Chem Date: 2020-01-23 Impact factor: 3.641

3. Oncogenic role and therapeutic targeting of ABL-class and JAK-STAT activating kinase alterations in Ph-like ALL.

Authors: Kathryn G Roberts; Yung-Li Yang; Debbie Payne-Turner; Wenwei Lin; Jacob K Files; Kirsten Dickerson; Zhaohui Gu; Jack Taunton; Laura J Janke; Taosheng Chen; Mignon L Loh; Stephen P Hunger; Charles G Mullighan
Journal: Blood Adv Date: 2017-08-30

4. Genetic alterations activating kinase and cytokine receptor signaling in high-risk acute lymphoblastic leukemia.

Authors: Kathryn G Roberts; Ryan D Morin; Jinghui Zhang; Martin Hirst; Yongjun Zhao; Xiaoping Su; Shann-Ching Chen; Debbie Payne-Turner; Michelle L Churchman; Richard C Harvey; Xiang Chen; Corynn Kasap; Chunhua Yan; Jared Becksfort; Richard P Finney; David T Teachey; Shannon L Maude; Kane Tse; Richard Moore; Steven Jones; Karen Mungall; Inanc Birol; Michael N Edmonson; Ying Hu; Kenneth E Buetow; I-Ming Chen; William L Carroll; Lei Wei; Jing Ma; Maria Kleppe; Ross L Levine; Guillermo Garcia-Manero; Eric Larsen; Neil P Shah; Meenakshi Devidas; Gregory Reaman; Malcolm Smith; Steven W Paugh; William E Evans; Stephan A Grupp; Sima Jeha; Ching-Hon Pui; Daniela S Gerhard; James R Downing; Cheryl L Willman; Mignon Loh; Stephen P Hunger; Marco A Marra; Charles G Mullighan
Journal: Cancer Cell Date: 2012-08-14 Impact factor: 31.743

5. Rearrangement of CRLF2 in B-progenitor- and Down syndrome-associated acute lymphoblastic leukemia.

Authors: Charles G Mullighan; J Racquel Collins-Underwood; Letha A A Phillips; Michael G Loudin; Wei Liu; Jinghui Zhang; Jing Ma; Elaine Coustan-Smith; Richard C Harvey; Cheryl L Willman; Fady M Mikhail; Julia Meyer; Andrew J Carroll; Richard T Williams; Jinjun Cheng; Nyla A Heerema; Giuseppe Basso; Andrea Pession; Ching-Hon Pui; Susana C Raimondi; Stephen P Hunger; James R Downing; William L Carroll; Karen R Rabin
Journal: Nat Genet Date: 2009-10-18 Impact factor: 38.330

6. Deregulated expression of cytokine receptor gene, CRLF2, is involved in lymphoid transformation in B-cell precursor acute lymphoblastic leukemia.

Authors: Lisa J Russell; Melania Capasso; Inga Vater; Takashi Akasaka; Olivier A Bernard; Maria Jose Calasanz; Thiruppavaii Chandrasekaran; Elise Chapiro; Stephan Gesk; Mike Griffiths; David S Guttery; Claudia Haferlach; Lana Harder; Olaf Heidenreich; Julie Irving; Lyndal Kearney; Florence Nguyen-Khac; Lee Machado; Lynne Minto; Aneela Majid; Anthony V Moorman; Heather Morrison; Vikki Rand; Jonathan C Strefford; Claire Schwab; Holger Tönnies; Martin J S Dyer; Reiner Siebert; Christine J Harrison
Journal: Blood Date: 2009-07-29 Impact factor: 22.113

7. Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof.

Authors: Ryan R Davis; Baoli Li; Sang Y Yun; Alice Chan; Pradeep Nareddy; Steven Gunawan; Muhammad Ayaz; Harshani R Lawrence; Gary W Reuther; Nicholas J Lawrence; Ernst Schönbrunn
Journal: J Med Chem Date: 2021-02-11 Impact factor: 7.446

8. Heterodimeric JAK-STAT activation as a mechanism of persistence to JAK2 inhibitor therapy.

Authors: Priya Koppikar; Neha Bhagwat; Outi Kilpivaara; Taghi Manshouri; Mazhar Adli; Todd Hricik; Fan Liu; Lindsay M Saunders; Ann Mullally; Omar Abdel-Wahab; Laura Leung; Abby Weinstein; Sachie Marubayashi; Aviva Goel; Mithat Gönen; Zeev Estrov; Benjamin L Ebert; Gabriela Chiosis; Stephen D Nimer; Bradley E Bernstein; Srdan Verstovsek; Ross L Levine
Journal: Nature Date: 2012-09-06 Impact factor: 49.962