skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: Development of Potent and Selective Janus Kinase 2/3 Directing PG?PROTACs

Journal Article · · ACS Med. Chem. Lett.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; NCI; OTHER
OSTI ID:
1856384
Journal Information:
ACS Med. Chem. Lett., Vol. 13, Issue (3)
Country of Publication:
United States
Language:
ENGLISH

References (25)

Targetable Kinase-Activating Lesions in Ph-like Acute Lymphoblastic Leukemia journal September 2014
Genetic Alterations Activating Kinase and Cytokine Receptor Signaling in High-Risk Acute Lymphoblastic Leukemia journal August 2012
Functional screening identifies CRLF2 in precursor B-cell acute lymphoblastic leukemia journal December 2009
Deregulated expression of cytokine receptor gene, CRLF2, is involved in lymphoid transformation in B-cell precursor acute lymphoblastic leukemia journal September 2009
Rearrangement of CRLF2 in B-progenitor– and Down syndrome–associated acute lymphoblastic leukemia journal October 2009
High Frequency and Poor Outcome of Philadelphia Chromosome–Like Acute Lymphoblastic Leukemia in Adults journal February 2017
Aberrant STAT5 and PI3K/mTOR pathway signaling occurs in human CRLF2-rearranged B-precursor acute lymphoblastic leukemia journal July 2012
Heterodimeric JAK–STAT activation as a mechanism of persistence to JAK2 inhibitor therapy journal July 2012
New Chemical Modalities and Strategic Thinking in Early Drug Discovery journal January 2020
E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones journal April 2021
Degradation of Janus kinases in CRLF2 -rearranged acute lymphoblastic leukemia journal December 2021
A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase journal June 2016
Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders journal January 2018
Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators journal May 2021
Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs journal March 2020
Phenyl‐Glutarimides: Alternative Cereblon Binders for the Design of PROTACs journal November 2021
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof journal February 2021
Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders journal September 2019
De-Novo Design of Cereblon (CRBN) Effectors Guided by Natural Hydrolysis Products of Thalidomide Derivatives journal June 2019
Thalidomide mimics uridine binding to an aromatic cage in cereblon journal December 2014
LigPlot+: Multiple Ligand–Protein Interaction Diagrams for Drug Discovery journal October 2011
A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos journal April 2017
Copy number abnormality of acute lymphoblastic leukemia cell lines based on their genetic subtypes journal May 2018
JAK2 is dispensable for maintenance of JAK2 mutant B-cell acute lymphoblastic leukemias journal June 2018
Combination efficacy of ruxolitinib with standard-of-care drugs in CRLF2-rearranged Ph-like acute lymphoblastic leukemia journal April 2021