Review and prospects of targeted therapies for Spleen tyrosine kinase (SYK)

Discovery of a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity In Vivo in Acute Myeloid Leukemia

(2023) Atsunori Kaneshige et al.   Journal of Medicinal Chemistry

Emerging TACnology: Heterobifunctional Small Molecule Inducers of Targeted Posttranslational Protein Modifications

(2023) Pascal Heitel   MOLECULES

Advancing Strategies for Proteolysis-Targeting Chimera Design

(2023) Minglei Li et al.   Journal of Medicinal Chemistry

Specific targeting of inflammatory osteoclastogenesis by the probiotic yeast S. boulardii CNCM I-745 reduces bone loss in osteoporosis

(2023) Maria-Bernadette Madel et al.   eLife

Spleen tyrosine kinase (SYK) signals are implicated in cardio-cerebrovascular diseases

(2023) Mohan Li et al.   Heliyon

Discovery of 3-(1H-benzo[d]imidazole-2-yl)-1H-pyrazol-4 -amine derivatives as novel and potent syk inhibitors for the treatment of hematological malignancies

(2023) Bingbing Cui et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting MyD88: Therapeutic mechanisms and potential applications of the specific inhibitor ST2825

(2023) Meiqi Liu et al.   INFLAMMATION RESEARCH

A novel association between platelet filamin A and soluble N-ethylmaleimide sensitive factor attachment proteins regulates granule secretion

(2023) Kalyan Golla et al.   Research and Practice in Thrombosis and Haemostasis

Investigational spleen tyrosine kinase (SYK) inhibitors for the treatment of autoimmune diseases

(2022) Su’an Tang et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

The state of the art of PROTAC technologies for drug discovery

(2022) Chao Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos

(2022) Fanye Meng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Asebogenin suppresses thrombus formation via inhibition of Syk phosphorylation

(2022) Li Li et al.   BRITISH JOURNAL OF PHARMACOLOGY

Systemic lupus erythematosus-complicating immune thrombocytopenia: From pathogenesis to treatment

(2022) Ying Jiang et al.   JOURNAL OF AUTOIMMUNITY

Protein Phosphatase 5-Recruiting Chimeras for Accelerating Apoptosis-Signal-Regulated Kinase 1 Dephosphorylation with Antiproliferative Activity

(2022) Qiuyue Zhang et al.   Journal of the American Chemical Society

Entospletinib and obinutuzumab in patients with relapsed/refractory chronic lymphocytic leukemia and B-cell malignancies

(2021) Adam S. Kittai et al.   HAEMATOLOGICA

The sickening consequences of too much SYK signaling

(2021) Ivona Aksentijevich   NATURE GENETICS

STING-mediated Syk Signaling Attenuates Tumorigenesis of Colitis‑associated Colorectal Cancer Through Enhancing Intestinal Epithelium Pyroptosis

(2021) Wenbin Gong et al.   INFLAMMATORY BOWEL DISEASES

Progress in the development of small molecular inhibitors of the Bruton’s tyrosine kinase (BTK) as a promising cancer therapy

(2021) Xiu-Juan Liu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Regulatory interplay between Vav1, Syk and β-catenin occurs in lung cancer cells

(2021) Rofia Boudria et al.   CELLULAR SIGNALLING

Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors

(2021) Xiaoyun Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of SYK kinase does not confer a pro-proliferative or pro-invasive phenotype in breast epithelium or breast cancer cells

(2020) David J. Lamb et al.   Oncotarget

Phosphorylation-Inducing Chimeric Small Molecules

(2020) Sachini U. Siriwardena et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Mincle/Syk/NF-κB Signaling Circuit Is Essential for Maintaining the Protumoral Activities of Tumor-Associated Macrophages

(2020) Chunjie Li et al.   Cancer Immunology Research

Kinase inhibition in autoimmunity and inflammation

(2020) Ali A. Zarrin et al.   NATURE REVIEWS DRUG DISCOVERY

Recent advance of spleen tyrosine kinase in diseases and drugs

(2020) Yuxin Shao et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Strategies for Targeting the NLRP3 Inflammasome in the Clinical and Preclinical Space

(2020) Adam G. Schwaid et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting SYK signaling in myeloid cells protects against liver fibrosis and hepatocarcinogenesis

(2019) Alejandro Torres-Hernandez et al.   ONCOGENE

Fostamatinib for the treatment of chronic immune thrombocytopenia

(2019) Nathan T. Connell et al.   BLOOD

Spleen tyrosine kinase (SYK) blocks autophagic Tau degradation in vitro and in vivo

(2019) Jonas Elias Schweig et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Global, regional and national burden of rheumatoid arthritis 1990–2017: a systematic analysis of the Global Burden of Disease study 2017

(2019) Saeid Safiri et al.   ANNALS OF THE RHEUMATIC DISEASES

IL-17A Increases Multiple Myeloma Cell Viability by Positively Regulating Syk Expression

(2019) Shunye Wang et al.   Translational Oncology

Immune thrombocytopenia (ITP): Pathophysiology update and diagnostic dilemmas

(2019) Dana N. LeVine et al.   VETERINARY CLINICAL PATHOLOGY

PROTAC-Mediated Degradation of KRAS Protein for Anticancer Therapeutics

(2019) Robert B. Kargbo   ACS Medicinal Chemistry Letters

Fostamatinib for the treatment of adult persistent and chronic immune thrombocytopenia: Results of two phase 3, randomized, placebo-controlled trials

(2018) James Bussel et al.   AMERICAN JOURNAL OF HEMATOLOGY

Fostamatinib: First Global Approval

(2018) Anthony Markham   DRUGS

Splenic tyrosine kinase (SYK) inhibitors and their possible use in acute myeloid leukemia

(2018) Sushma Bartaula-Brevik et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Fostamatinib for persistent/chronic adult immune thrombocytopenia

(2018) Adrian Newland et al.   Immunotherapy

Spleen Tyrosine Kinase Inhibitor TAK-659 Prevents Splenomegaly and Tumor Development in a Murine Model of Epstein-Barr Virus-Associated Lymphoma

(2018) Osman Cen et al.   mSphere

Inhibition of spleen tyrosine kinase attenuates psoriasis-like inflammation in mice through blockade of dendritic cell-Th17 inflammation axis

(2018) Khalid S. Alzahrani et al.   BIOMEDICINE & PHARMACOTHERAPY

TAK-659, AN INVESTIGATIONAL REVERSIBLE DUAL SYK/FLT-3 INHIBITOR, IN PATIENTS WITH LYMPHOMA: UPDATED RESULTS FROM DOSE-ESCALATION AND EXPANSION COHORTS OF a PHASE 1 STUDY

(2017) J. Kaplan et al.   HEMATOLOGICAL ONCOLOGY

Syk inhibitors in clinical development for hematological malignancies

(2017) Delong Liu et al.   Journal of Hematology & Oncology

Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK)

(2016) Betty Lam et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pharmacokinetics, Pharmacodynamics, and Safety of Entospletinib, a Novel pSYK Inhibitor, Following Single and Multiple Oral Dosing in Healthy Volunteers

(2016) Srini Ramanathan et al.   CLINICAL DRUG INVESTIGATION

The diagnosis and management of the haematologic manifestations of lupus

(2016) Alba Velo-García et al.   JOURNAL OF AUTOIMMUNITY

Rheumatoid arthritis

(2016) Josef S Smolen et al.   LANCET

Inhibition of BCR signaling using the Syk inhibitor TAK-659 prevents stroma-mediated signaling in chronic lymphocytic leukemia cells

(2016) Noelia Purroy et al.   Oncotarget

An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia

(2015) J. Sharman et al.   BLOOD

Human autoimmune diseases: a comprehensive update

(2015) Lifeng Wang et al.   JOURNAL OF INTERNAL MEDICINE

Immunogenicity of Antibody Drug Conjugates: Bioanalytical Methods and Monitoring Strategy for a Novel Therapeutic Modality

(2014) M. Benjamin Hock et al.   AAPS Journal

SYK Is a Candidate Kinase Target for the Treatment of Advanced Prostate Cancer

(2014) V. P. S. Ghotra et al.   CANCER RESEARCH

Discovery of GS-9973, a Selective and Orally Efficacious Inhibitor of Spleen Tyrosine Kinase

(2014) Kevin S. Currie et al.   JOURNAL OF MEDICINAL CHEMISTRY

Getting Syk: spleen tyrosine kinase as a therapeutic target

(2014) Robert L. Geahlen   TRENDS IN PHARMACOLOGICAL SCIENCES

Inhibitors of switch kinase ‘spleen tyrosine kinase’ in inflammation and immune-mediated disorders: A review

(2013) Maninder Kaur et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel small molecule therapeutics in rheumatoid arthritis

(2013) V. Kelly et al.   RHEUMATOLOGY

Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders

(2012) Tadeusz Robak et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Discovery and Development of Spleen Tyrosine Kinase (SYK) Inhibitors

(2012) Rajinder Singh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Genetic deficiency of Syk protects mice from autoantibody-induced arthritis

(2010) Zoltán Jakus et al.   ARTHRITIS AND RHEUMATISM

Inhibition of spleen tyrosine kinase suppresses skin and kidney disease in lupus prone mice

(2010) Guo-Min Deng et al.   ARTHRITIS AND RHEUMATISM

The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the E - TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling

(2010) M. Suljagic et al.   BLOOD

Spleen tyrosine kinases: biology, therapeutic targets and drugs

(2010) Mauro Riccaboni et al.   DRUG DISCOVERY TODAY

Mast cell signaling: The role of protein tyrosine kinase Syk, its activation and screening methods for new pathway participants

(2010) Reuben P. Siraganian et al.   FEBS LETTERS

Src-family and Syk Kinases in Activating and Inhibitory Pathways in Innate Immune Cells: Signaling Cross Talk

(2010) C. A. Lowell   Cold Spring Harbor Perspectives in Biology

Spleen tyrosine kinase: An Src family of non-receptor kinase has multiple functions and represents a valuable therapeutic target in the treatment of autoimmune and inflammatory diseases

(2009) Debjani Ghosh et al.   AUTOIMMUNITY

Syk and pTyr'd: Signaling through the B cell antigen receptor

(2009) Robert L. Geahlen   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Therapeutic prospect of Syk inhibitors

(2009) Paolo Ruzza et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Autoinhibition and adapter function of Syk

(2009) Yogesh Kulathu et al.   IMMUNOLOGICAL REVIEWS

The tyrosine kinase network regulating mast cell activation

(2009) Alasdair M. Gilfillan et al.   IMMUNOLOGICAL REVIEWS

A Spleen Tyrosine Kinase Inhibitor Reduces the Severity of Established Glomerulonephritis

(2009) J. Smith et al.   JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY

Of mice and men: an open-label pilot study for treatment of immune thrombocytopenic purpura by an inhibitor of Syk

(2008) A. Podolanczuk et al.   BLOOD

The development of allergic inflammation

(2008) Stephen J. Galli et al.   NATURE

Tyr130 phosphorylation triggers Syk release from antigen receptor by long-distance conformational uncoupling

(2008) Y. Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Akt/Mcl-1 pathway plays a prominent role in mediating antiapoptotic signals downstream of the B-cell receptor in chronic lymphocytic leukemia B cells

(2007) P. G. Longo et al.   BLOOD