A Novel Selective JAK2 Inhibitor Identified Using Pharmacological Interactions

A whole-animal platform to advance a clinical kinase inhibitor into new disease space

(2018) Masahiro Sonoshita et al.   Nature Chemical Biology

CASTp 3.0: computed atlas of surface topography of proteins

(2018) Wei Tian et al.   NUCLEIC ACIDS RESEARCH

Human colorectal cancer-derived mesenchymal stem cells promote colorectal cancer progression through IL-6/JAK2/STAT3 signaling

(2018) Xiaochao Zhang et al.   Cell Death & Disease

No evidence for JAK2 V617F mutation in colorectal cancer

(2018) M. Herreros-Villanueva et al.   BRITISH JOURNAL OF BIOMEDICAL SCIENCE

Rethinking JAK2 inhibition: towards novel strategies of more specific and versatile janus kinase inhibition

(2017) E Leroy et al.   LEUKEMIA

JAK inhibition as a therapeutic strategy for immune and inflammatory diseases

(2017) Daniella M. Schwartz et al.   NATURE REVIEWS DRUG DISCOVERY

Identification of 8-Hydroxyquinoline Derivatives Active Against Somatic V658F Mutant JAK1-Dependent Cells

(2016) Róbert Kiss et al.   ARCHIV DER PHARMAZIE

Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors

(2016) Vladimir Simov et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cancer treatment and survivorship statistics, 2016

(2016) Kimberly D. Miller et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Insights into the Structural Features Essential for JAK2 Inhibition and Selectivity

(2016) Chao Zhao et al.   CURRENT MEDICINAL CHEMISTRY

Targeting JAK kinase in solid tumors: emerging opportunities and challenges

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FDA-approved small-molecule kinase inhibitors

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JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model

(2014) S. Degryse et al.   BLOOD

S-Phase Cell Cycle Arrest, Apoptosis, and Molecular Mechanisms of Aplasia Ras homolog Member I–Induced Human Ovarian Cancer SKOV3 Cell Lines

(2014) Qiaoying Zhu et al.   INTERNATIONAL JOURNAL OF GYNECOLOGICAL CANCER

Considering the impact drug-like properties have on the chance of success

(2013) Iskander Yusof et al.   DRUG DISCOVERY TODAY

Specificity and mechanism-of-action of the JAK2 tyrosine kinase inhibitors ruxolitinib and SAR302503 (TG101348)

(2013) T Zhou et al.   LEUKEMIA

JAKs and STATs in Immunity, Immunodeficiency, and Cancer

(2013) John J. O'Shea et al.   NEW ENGLAND JOURNAL OF MEDICINE

STAT3 suppresses transcription of proapoptotic genes in cancer cells with the involvement of its N-terminal domain

(2013) Olga A. Timofeeva et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure-Based Virtual Screening for Drug Discovery: a Problem-Centric Review

(2012) Tiejun Cheng et al.   AAPS Journal

Molecular Docking: A Powerful Approach for Structure-Based Drug Discovery

(2012) Xuan-Yu Meng et al.   Current Computer-Aided Drug Design

Biology and Clinical Management of Myeloproliferative Neoplasms and Development of the JAK Inhibitor Ruxolitinib

(2012) J. Mascarenhas et al.   CURRENT MEDICINAL CHEMISTRY

JAK2 inhibition for the treatment of hematologic and solid malignancies

(2012) Brian L Harry et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Quantifying the chemical beauty of drugs

(2012) G. Richard Bickerton et al.   Nature Chemistry

Ruxolitinib

(2012) Ruben A. Mesa et al.   NATURE REVIEWS DRUG DISCOVERY

JAK/STAT signaling in hematological malignancies

(2012) W Vainchenker et al.   ONCOGENE

iGEMDOCK: a graphical environment of enhancing GEMDOCK using pharmacological interactions and post-screening analysis

(2011) Kai-Cheng Hsu et al.   BMC BIOINFORMATICS

STAT3 Is Necessary for Proliferation and Survival in Colon Cancer-Initiating Cells

(2011) L. Lin et al.   CANCER RESEARCH

The Use of Structural Biology in Janus Kinase Targeted Drug Discovery

(2011) Nilda L. Alicea-Velazquez et al.   CURRENT DRUG TARGETS

Inhibition of JAK2/STAT3 signalling induces colorectal cancer cell apoptosis via mitochondrial pathway

(2011) Wan Du et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Discovery of 1-Amino-5H-pyrido[4,3-b]indol-4-carboxamide Inhibitors of Janus Kinase 2 (JAK2) for the Treatment of Myeloproliferative Disorders

(2011) Jongwon Lim et al.   JOURNAL OF MEDICINAL CHEMISTRY

Trichostatin A, a histone deacetylase inhibitor, suppresses JAK2/STAT3 signaling via inducing the promoter-associated histone acetylation of SOCS1 and SOCS3 in human colorectal cancer cells

(2011) Hua Xiong et al.   MOLECULAR CARCINOGENESIS

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

JAK2 inhibitors: What's the true therapeutic potential?

(2010) Fabio P.S. Santos et al.   BLOOD REVIEWS

The current status and the future of JAK2 inhibitors for the treatment of myeloproliferative diseases

(2010) Yasumichi Hitoshi et al.   INTERNATIONAL JOURNAL OF HEMATOLOGY

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY

2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2

(2009) Mark W. Ledeboer et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening

(2009) Róbert Kiss et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Janus Kinase 2 Inhibitors. Synthesis and Characterization of a Novel Polycyclic Azaindole

(2009) Tiansheng Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lestaurtinib: a multi-targeted FLT3 inhibitor

(2009) Amir T Fathi et al.   Expert Review of Hematology

Absence of JH2 domain mutation of the tyrosine kinase JAK2 in renal cell carcinomas

(2008) Jianming Zhao et al.   ACTA ONCOLOGICA