Progress towards the development of SH2 domain inhibitors

Novel Nonphosphorylated Peptides with Conserved Sequences Selectively Bind to Grb7 SH2 Domain with Affinity Comparable to Its Phosphorylated Ligand

(2012) Dan Zhang et al.   PLoS One

Structurally Modified Curcumin Analogs Inhibit STAT3 Phosphorylation and Promote Apoptosis of Human Renal Cell Carcinoma and Melanoma Cell Lines

(2012) Matthew A. Bill et al.   PLoS One

Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts

(2012) X. Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective Targeting of Disease-Relevant Protein Binding Domains byO-Phosphorylated Natural Product Derivatives

(2011) Martin Gräber et al.   ACS Chemical Biology

Identification of a non-phosphorylated, cell permeable, small molecule ligand for the Stat3 SH2 domain

(2011) Brent D.G. Page et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Antagonism of the Stat3-Stat3 Protein Dimer with Salicylic Acid Based Small Molecules

(2011) Steven Fletcher et al.   ChemMedChem

Fragment-Based Drug Design and Drug Repositioning Using Multiple Ligand Simultaneous Docking (MLSD): Identifying Celecoxib and Template Compounds as Novel Inhibitors of Signal Transducer and Activator of Transcription 3 (STAT3)

(2011) Huameng Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Non-Peptide Ligands of Growth Factor Receptor-Bound Protein 2-Src Homology 2 Domain Using Molecular Modeling and NMR Spectroscopy†

(2011) Ángel L. Orcajo-Rincón et al.   JOURNAL OF MEDICINAL CHEMISTRY

Potent and Selective Phosphopeptide Mimetic Prodrugs Targeted to the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 3

(2011) Pijus K. Mandal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small Molecule STAT5-SH2 Domain Inhibitors Exhibit Potent Antileukemia Activity

(2011) Brent D. G. Page et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Basis of Binding by Cyclic Nonphosphorylated Peptide Antagonists of Grb7 Implicated in Breast Cancer Progression

(2011) Nigus D. Ambaye et al.   JOURNAL OF MOLECULAR BIOLOGY

Interaction of the non-phosphorylated peptide G7-18NATE with Grb7-SH2 domain requires phosphate for enhanced affinity and specificity

(2011) Menachem J. Gunzburg et al.   JOURNAL OF MOLECULAR RECOGNITION

Inhibitors of Stat5 protein signalling

(2011) Abbarna A. Cumaraswamy et al.   MedChemComm

Preparation and crystallization of the Grb7 SH2 domain in complex with the G7-18NATE nonphosphorylated cyclic inhibitor peptide

(2010) Min Y. Yap et al.   Acta Crystallographica Section F-Structural Biology and Crystallization Communications

An oral Syk kinase inhibitor in the treatment of rheumatoid arthritis: A three-month randomized, placebo-controlled, phase II study in patients with active rheumatoid arthritis that did not respond to biologic agents

(2010) Mark C. Genovese et al.   ARTHRITIS AND RHEUMATISM

A novel small-molecule disrupts Stat3 SH2 domain–phosphotyrosine interactions and Stat3-dependent tumor processes

(2010) Xiaolei Zhang et al.   BIOCHEMICAL PHARMACOLOGY

Benzopyrazine derivatives: A novel class of growth factor receptor bound protein 7 antagonists

(2010) Nigus D. Ambaye et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Uptake of a cell permeable G7-18NATE construct into cells and binding with the Grb7-SH2 domain

(2010) Nigus D. Ambaye et al.   BIOPOLYMERS

Novel STAT3 Phosphorylation Inhibitors Exhibit Potent Growth-Suppressive Activity in Pancreatic and Breast Cancer Cells

(2010) L. Lin et al.   CANCER RESEARCH

Dasatinib: A potent SRC inhibitor in clinical development for the treatment of solid tumors

(2010) John Araujo et al.   CANCER TREATMENT REVIEWS

The Src, Syk, and Tec family kinases: Distinct types of molecular switches

(2010) J. Michael Bradshaw   CELLULAR SIGNALLING

Differential Functions of Growth Factor Receptor-Bound Protein 7 (GRB7) and Its Variant GRB7v in Ovarian Carcinogenesis

(2010) Y. Wang et al.   CLINICAL CANCER RESEARCH

Use of SPR to Study the Interaction of G7-18NATE Peptide with the Grb7-SH2 Domain

(2010) Menachem J. Gunzburg et al.   International Journal of Peptide Research and Therapeutics

EGF-induced Grb7 Recruits and Promotes Ras Activity Essential for the Tumorigenicity of Sk-Br3 Breast Cancer Cells

(2010) Pei-Yu Chu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Characterization of molecular recognition of STAT3 SH2 domain inhibitors through molecular simulation

(2010) In-Hee Park et al.   JOURNAL OF MOLECULAR RECOGNITION

An Oral Spleen Tyrosine Kinase (Syk) Inhibitor for Rheumatoid Arthritis

(2010) Michael E. Weinblatt et al.   NEW ENGLAND JOURNAL OF MEDICINE

Identification of Purine-Scaffold Small-Molecule Inhibitors of Stat3 Activation by QSAR Studies

(2010) Vijay M. Shahani et al.   ACS Medicinal Chemistry Letters

Structure-Based Design of Conformationally Constrained, Cell-Permeable STAT3 Inhibitors

(2010) Jianyong Chen et al.   ACS Medicinal Chemistry Letters

Growth factor receptor-bound protein-7 (Grb7) as a prognostic marker and therapeutic target in breast cancer

(2009) Y. Nadler et al.   ANNALS OF ONCOLOGY

Novel high-throughput screening system for identifying STAT3–SH2 antagonists

(2009) Yutaka Uehara et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Discovery of thioether-bridged cyclic pentapeptides binding to Grb2-SH2 domain with high affinity

(2009) Sheng Jiang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors

(2009) Cindy Gomez et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Natural product inhibitors of protein–protein interactions mediated by Src-family SH2 domains

(2009) Bianca Sperl et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibition of Syk with fostamatinib disodium has significant clinical activity in non-Hodgkin lymphoma and chronic lymphocytic leukemia

(2009) J. W. Friedberg et al.   BLOOD

Disruption of Transcriptionally Active Stat3 Dimers with Non-phosphorylated, Salicylic Acid-Based Small Molecules: Potent in vitro and Tumor Cell Activities

(2009) Steven Fletcher et al.   CHEMBIOCHEM

T-cell receptor proximal signaling via the Src-family kinases, Lck and Fyn, influences T-cell activation, differentiation, and tolerance

(2009) Robert J. Salmond et al.   IMMUNOLOGICAL REVIEWS

Autoinhibition and adapter function of Syk

(2009) Yogesh Kulathu et al.   IMMUNOLOGICAL REVIEWS

Osteoimmunology: Crosstalk Between the Immune and Bone Systems

(2009) Tomoki Nakashima et al.   JOURNAL OF CLINICAL IMMUNOLOGY

Structure−Affinity Relationships of Glutamine Mimics Incorporated into Phosphopeptides Targeted to the SH2 Domain of Signal Transducer and Activator of Transcription 3

(2009) Pijus K. Mandal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Conformationally Constrained Peptidomimetic Inhibitors of Signal Transducer and Activator of Transcription 3: Evaluation and Molecular Modeling

(2009) Pijus K. Mandal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Switching between low and high affinity for the Syk tandem SH2 domain by irradiation of azobenzene containing ITAM peptidomimetics

(2009) Joeri Kuil et al.   JOURNAL OF PEPTIDE SCIENCE

Thermodynamic and Structural Effects of Conformational Constraints in Protein−Ligand Interactions. Entropic Paradoxy Associated with Ligand Preorganization

(2009) John E. DeLorbe et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

ITAM-derived phosphopeptide-containing dendrimers as multivalent ligands for Syk tandem SH2 domain

(2009) Joeri Kuil et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Synthesis of Phosphatase-Stable, Cell-Permeable Peptidomimetic Prodrugs That Target the SH2 Domain of Stat3

(2009) Pijus K. Mandal et al.   ORGANIC LETTERS

Chemical Probes that Competitively and Selectively Inhibit Stat3 Activation

(2009) Xuejun Xu et al.   PLoS One

CARD9 versus CARMA1 in innate and adaptive immunity

(2009) Hiromitsu Hara et al.   TRENDS IN IMMUNOLOGY

Inhibition of Protein Kinase c-Src as a Therapeutic Approach for Cancer and Bone Metastases

(2008) Nadia Rucci et al.   Anti-Cancer Agents in Medicinal Chemistry

Treatment of rheumatoid arthritis with a syk kinase inhibitor: A twelve-week, randomized, placebo-controlled trial

(2008) Michael E. Weinblatt et al.   ARTHRITIS AND RHEUMATISM

Discovery of the catechol structural moiety as a Stat3 SH2 domain inhibitor by virtual screening

(2008) Wenshan Hao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Multiple ITAM-coupled NK-cell receptors engage the Bcl10/Malt1 complex via Carma1 for NF- B and MAPK activation to selectively control cytokine production

(2008) O. Gross et al.   BLOOD

Mouse models of non-Hodgkin lymphoma reveal Syk as an important therapeutic target

(2008) R. M. Young et al.   BLOOD

Cryptotanshinone Inhibits Constitutive Signal Transducer and Activator of Transcription 3 Function through Blocking the Dimerization in DU145 Prostate Cancer Cells

(2008) D.-S. Shin et al.   CANCER RESEARCH

Discovery of Chromone-Based Inhibitors of the Transcription Factor STAT5

(2008) Judith Müller et al.   CHEMBIOCHEM

Targeting Protein-Protein Interactions: Suppression of Stat3 Dimerization with Rationally Designed Small-Molecule, Nonpeptidic SH2 Domain Binders

(2008) Patrick T. Gunning et al.   CHEMBIOCHEM

Peptidomimetics, a synthetic tool of drug discovery

(2008) Josef Vagner et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Signal transducer and activator of transcription 5A/B in prostate and breast cancers

(2008) S.-H. Tan et al.   ENDOCRINE-RELATED CANCER

Targeting STAT3 in cancer: how successful are we?

(2008) Peibin Yue et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Solution structure of the Grb2 SH2 domain complexed with a high-affinity inhibitor

(2008) Kenji Ogura et al.   JOURNAL OF BIOMOLECULAR NMR

Synthesis and Utilization of Chiral α-Methylated α-Amino Acids with a Carboxyalkyl Side Chain in the Design of Novel Grb2-SH2 Peptide Inhibitors Free of Phosphotyrosine

(2008) Ya-Qiu Long et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selectivity and Mechanism of Action of a Growth Factor Receptor-Bound Protein 2 Src Homology 2 Domain Binding Antagonist

(2008) Alessio Giubellino et al.   JOURNAL OF MEDICINAL CHEMISTRY

A photoswitchable ITAM peptidomimetic: Synthesis and real time surface plasmon resonance (SPR) analysis of the effects of cis–trans isomerization on binding

(2007) Joeri Kuil et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis, and studies of small molecule STAT3 inhibitors

(2007) Deepak Bhasin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Ameliorating effects of compounds derived from Salvia miltiorrhiza root extract on microcirculatory disturbance and target organ injury by ischemia and reperfusion

(2007) Jing-Yan Han et al.   PHARMACOLOGY & THERAPEUTICS