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

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

(2021) Ryan R. Davis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Combination efficacy of ruxolitinib with standard-of-care drugs in CRLF2-rearranged Ph-like acute lymphoblastic leukemia

(2021) Julia W. Bӧhm et al.   LEUKEMIA

Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia

(2021) Yunchao Chang et al.   BLOOD

Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators

(2021) Gisele Nishiguchi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phenyl‐Glutarimides: Alternative Cereblon Binders for the Design of PROTACs

(2021) Jaeki Min et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

(2020) Rishi R. Shah et al.   BIOORGANIC & MEDICINAL CHEMISTRY

New Chemical Modalities and Strategic Thinking in Early Drug Discovery

(2020) Maria-Jesus Blanco et al.   ACS Medicinal Chemistry Letters

De-Novo Design of Cereblon (CRBN) Effectors Guided by Natural Hydrolysis Products of Thalidomide Derivatives

(2019) Christopher Heim et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2019) Jiuling Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders

(2018) Mette Ishoey et al.   ACS Chemical Biology

JAK2 is dispensable for maintenance of JAK2 mutant B-cell acute lymphoblastic leukemias

(2018) Sang-Kyu Kim et al.   GENES & DEVELOPMENT

Copy number abnormality of acute lymphoblastic leukemia cell lines based on their genetic subtypes

(2018) Chihiro Tomoyasu et al.   INTERNATIONAL JOURNAL OF HEMATOLOGY

High Frequency and Poor Outcome of Philadelphia Chromosome–Like Acute Lymphoblastic Leukemia in Adults

(2017) Kathryn G. Roberts et al.   JOURNAL OF CLINICAL ONCOLOGY

A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos

(2017) Mary E. Matyskiela et al.   JOURNAL OF MEDICINAL CHEMISTRY

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

(2016) Mary E. Matyskiela et al.   NATURE

Targetable Kinase-Activating Lesions in Ph-like Acute Lymphoblastic Leukemia

(2015) Kathryn G. Roberts et al.   NEW ENGLAND JOURNAL OF MEDICINE

Thalidomide mimics uridine binding to an aromatic cage in cereblon

(2014) Marcus D. Hartmann et al.   JOURNAL OF STRUCTURAL BIOLOGY

Aberrant STAT5 and PI3K/mTOR pathway signaling occurs in human CRLF2-rearranged B-precursor acute lymphoblastic leukemia

(2012) S. K. Tasian et al.   BLOOD

Genetic Alterations Activating Kinase and Cytokine Receptor Signaling in High-Risk Acute Lymphoblastic Leukemia

(2012) Kathryn G. Roberts et al.   CANCER CELL

Heterodimeric JAK–STAT activation as a mechanism of persistence to JAK2 inhibitor therapy

(2012) Priya Koppikar et al.   NATURE

LigPlot+: Multiple Ligand–Protein Interaction Diagrams for Drug Discovery

(2011) Roman A. Laskowski et al.   Journal of Chemical Information and Modeling

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

(2009) L. J. Russell et al.   BLOOD

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

(2009) Charles G Mullighan et al.   NATURE GENETICS

Functional screening identifies CRLF2 in precursor B-cell acute lymphoblastic leukemia

(2009) A. Yoda et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA