Protein kinase inhibitor ceritinib blocks ectonucleotidase CD39 – a promising target for cancer immunotherapy

Sulfated Polysaccharides from Macroalgae Are Potent Dual Inhibitors of Human ATP-Hydrolyzing Ectonucleotidases NPP1 and CD39

(2021) Vittoria Lopez et al.   Marine Drugs

The ALK inhibitors, alectinib and ceritinib, induce ALK‐independent and STAT3‐dependent glioblastoma cell death

(2021) Daisuke Kawauchi et al.   CANCER SCIENCE

Small-molecule CD73 inhibitors for the immunotherapy of cancer: a patent and literature review (2017–present)

(2021) Alessio Nocentini et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

CD73 facilitates EMT progression and promotes lung metastases in triple-negative breast cancer

(2021) Nataliia Petruk et al.   Scientific Reports

Pharmacological inhibitors of anaplastic lymphoma kinase (ALK) induce immunogenic cell death through on-target effects

(2021) Adriana Petrazzuolo et al.   Cell Death & Disease

A Phase 0 Trial of Ceritinib in Patients with Brain Metastases and Recurrent Glioblastoma

(2021) Shwetal Mehta et al.   CLINICAL CANCER RESEARCH

Lessons from the A2A Adenosine Receptor Antagonist–Enabled Tumor Regression and Survival in Patients with Treatment-Refractory Renal Cell Cancer

(2020) Michail V. Sitkovsky   Cancer Discovery

On the mechanism of anti-CD39 immune checkpoint therapy

(2020) David Allard et al.   Journal for ImmunoTherapy of Cancer

Recombinant expression of ecto-nucleotide pyrophosphatase/phosphodiesterase 4 (NPP4) and development of a luminescence-based assay to identify inhibitors

(2020) Vittoria Lopez et al.   ANALYTICAL BIOCHEMISTRY

Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity

(2020) Alexandra Borodovsky et al.   Journal for ImmunoTherapy of Cancer

Antihypoxic oxygenation agents with respiratory hyperoxia to improve cancer immunotherapy

(2020) Stephen M. Hatfield et al.   JOURNAL OF CLINICAL INVESTIGATION

Nucleotide Analog ARL67156 as a Lead Structure for the Development of CD39 and Dual CD39/CD73 Ectonucleotidase Inhibitors

(2020) Laura Schäkel et al.   Frontiers in Pharmacology

Implications of CD39 in immune-related diseases

(2020) Jianrui Zeng et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Functionalized Oxoindolin Hydrazine Carbothioamide Derivatives as Highly Potent Inhibitors of Nucleoside Triphosphate Diphosphohydrolases

(2020) Saira Afzal et al.   Frontiers in Pharmacology

Serum CD73 is a prognostic factor in patients with metastatic melanoma and is associated with response to anti-PD-1 therapy

(2020) Roberta Turiello et al.   Journal for ImmunoTherapy of Cancer

History of ectonucleotidases and their role in purinergic signaling

(2020) Herbert Zimmermann   BIOCHEMICAL PHARMACOLOGY

Hydrolysis of ATP, ADP, and AMP is increased in blood plasma of prostate cancer patients

(2019) Carla Fernanda Furtado Gardani et al.   Purinergic Signalling

Antisense oligonucleotide targeting CD39 improves anti-tumor T cell immunity

(2019) Abhishek S. Kashyap et al.   Journal for ImmunoTherapy of Cancer

Structure–Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5′-Nucleotidase (CD73) Inhibitors

(2019) Anna Junker et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Purinergic System as a Pharmacological Target for the Treatment of Immune-Mediated Inflammatory Diseases

(2019) Luca Antonioli et al.   PHARMACOLOGICAL REVIEWS

Targeting the Immunomodulatory CD73/Adenosine System to Improve the Therapeutic Gain of Radiotherapy

(2019) Simone de Leve et al.   Frontiers in Immunology

A2B Adenosine Receptor and Cancer

(2019) Zhan-Guo Gao et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Adenosine 2A Receptor Blockade as an Immunotherapy for Treatment-Refractory Renal Cell Cancer

(2019) Lawrence Fong et al.   Cancer Discovery

Targeting the CD73-adenosine axis in immuno-oncology

(2018) David Allard et al.   IMMUNOLOGY LETTERS

Polypharmacology-based ceritinib repurposing using integrated functional proteomics

(2017) Brent M Kuenzi et al.   Nature Chemical Biology

Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors

(2017) Sang-Yong Lee et al.   MedChemComm

Substrate-Dependence of Competitive Nucleotide Pyrophosphatase/Phosphodiesterase1 (NPP1) Inhibitors

(2017) Sang-Yong Lee et al.   Frontiers in Pharmacology

Minor modifications to ceritinib enhance anti-tumor activity in EML4-ALK positive cancer

(2016) Chung Hyo Kang et al.   CANCER LETTERS

A2A adenosine receptor antagonists to weaken the hypoxia-HIF-1α driven immunosuppression and improve immunotherapies of cancer

(2016) Stephen M Hatfield et al.   CURRENT OPINION IN PHARMACOLOGY

Immunosuppressive activities of adenosine in cancer

(2016) Bertrand Allard et al.   CURRENT OPINION IN PHARMACOLOGY

Adenosine-generating ovarian cancer cells attract myeloid cells which differentiate into adenosine-generating tumor associated macrophages – a self-amplifying, CD39- and CD73-dependent mechanism for tumor immune escape

(2016) Itsaso Montalbán del Barrio et al.   Journal for ImmunoTherapy of Cancer

Polyoxometalates—Potent and selective ecto-nucleotidase inhibitors

(2015) Sang-Yong Lee et al.   BIOCHEMICAL PHARMACOLOGY

CD39+regulatory T cells attenuate allergic airway inflammation

(2015) P. Li et al.   CLINICAL AND EXPERIMENTAL ALLERGY

FDA Approval: Ceritinib for the Treatment of Metastatic Anaplastic Lymphoma Kinase-Positive Non-Small Cell Lung Cancer

(2015) S. Khozin et al.   CLINICAL CANCER RESEARCH

Extracellular nucleotides as novel, underappreciated pro-metastatic factors that stimulate purinergic signaling in human lung cancer cells

(2015) Gabriela Schneider et al.   Molecular Cancer

Vascular CD39/ENTPD1 Directly Promotes Tumor Cell Growth by Scavenging Extracellular Adenosine Triphosphate

(2015) Lili Feng et al.   NEOPLASIA

Hydrolysis of 2′3′-cGAMP by ENPP1 and design of nonhydrolyzable analogs

(2014) Lingyin Li et al.   Nature Chemical Biology

Ceritinib in ALK-Rearranged Non–Small-Cell Lung Cancer

(2014) Alice T. Shaw et al.   NEW ENGLAND JOURNAL OF MEDICINE

Inhibition of CD39 Enzymatic Function at the Surface of Tumor Cells Alleviates Their Immunosuppressive Activity

(2014) J. Bastid et al.   Cancer Immunology Research

Hostile, Hypoxia-A2-Adenosinergic Tumor Biology as the Next Barrier to Overcome for Tumor Immunologists

(2014) M. V. Sitkovsky et al.   Cancer Immunology Research

A new, sensitive ecto-5′-nucleotidase assay for compound screening

(2013) Marianne Freundlieb et al.   ANALYTICAL BIOCHEMISTRY

8-BuS-ATP derivatives as specific NTPDase1 inhibitors

(2013) Joanna Lecka et al.   BRITISH JOURNAL OF PHARMACOLOGY

A CD38/CD203a/CD73 ectoenzymatic pathway independent of CD39 drives a novel adenosinergic loop in human T lymphocytes

(2013) Alberto L Horenstein et al.   OncoImmunology

Inhibition of ectonucleotidase with ARL67156 prevents the development of calcific aortic valve disease in warfarin-treated rats

(2012) Nancy Côté et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Comparison of Next-Generation Sequencing Systems

(2012) Lin Liu et al.   JOURNAL OF BIOMEDICINE AND BIOTECHNOLOGY

Transcriptional control of adenosine signaling by hypoxia-inducible transcription factors during ischemic or inflammatory disease

(2012) Jens M. Poth et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Cellular function and molecular structure of ecto-nucleotidases

(2012) Herbert Zimmermann et al.   Purinergic Signalling

Crystal Structures of Anaplastic Lymphoma Kinase in Complex with ATP Competitive Inhibitors

(2010) Roberto T. Bossi et al.   BIOCHEMISTRY

Inhibition of vascular ectonucleotidase activities by the pro-drugs ticlopidine and clopidogrel favours platelet aggregation

(2010) Joanna Lecka et al.   BRITISH JOURNAL OF PHARMACOLOGY

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

(2010) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tumor pH and Its Measurement

(2010) X. Zhang et al.   JOURNAL OF NUCLEAR MEDICINE

Therapeutic Protein Kinase Inhibitors

(2008) S. K. Grant   CELLULAR AND MOLECULAR LIFE SCIENCES

A structural basis for the allosteric regulation of non-hydrolysing UDP-GlcNAc 2-epimerases

(2008) Lucas M Velloso et al.   EMBO REPORTS

Structure-activity relationships of anthraquinone derivatives derived from bromaminic acid as inhibitors of ectonucleoside triphosphate diphosphohydrolases (E-NTPDases)

(2008) Younis Baqi et al.   Purinergic Signalling