Allosteric targeting of receptor tyrosine kinases

Improved Glucose Metabolism In Vitro and In Vivo by an Allosteric Monoclonal Antibody That Increases Insulin Receptor Binding Affinity

(2014) John A. Corbin et al.   PLoS One

Molecular Mechanism of SSR128129E, an Extracellularly Acting, Small-Molecule, Allosteric Inhibitor of FGF Receptor Signaling

(2013) Corentin Herbert et al.   CANCER CELL

Inhibition of Tumor Angiogenesis and Growth by a Small-Molecule Multi-FGF Receptor Blocker with Allosteric Properties

(2013) Françoise Bono et al.   CANCER CELL

Impact of Quaternary Structure Dynamics on Allosteric Drug Discovery

(2013) Eileen K. Jaffe   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Tyrosine Kinase Inhibitors: Their On-Target Toxicities as Potential Indicators of Efficacy

(2013) Devron R. Shah et al.   DRUG SAFETY

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

Emerging paradigms in GPCR allostery: implications for drug discovery

(2013) Denise Wootten et al.   NATURE REVIEWS DRUG DISCOVERY

Structural and mechanistic insights into VEGF receptor 3 ligand binding and activation

(2013) V.-M. Leppanen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Allosteric Regulation of PKM2 Allows Cellular Adaptation to Different Physiological States

(2013) D. Y. Gui et al.   Science Signaling

The Growing Arsenal of ATP-Competitive and Allosteric Inhibitors of BCR-ABL

(2012) O. Hantschel et al.   CANCER RESEARCH

Inhibitors of the TAM subfamily of tyrosine kinases: Synthesis and biological evaluation

(2012) Rosa M. Suárez et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting Extracellular Domains D4 and D7 of Vascular Endothelial Growth Factor Receptor 2 Reveals Allosteric Receptor Regulatory Sites

(2012) C. A. C. Hyde et al.   MOLECULAR AND CELLULAR BIOLOGY

Serine is a natural ligand and allosteric activator of pyruvate kinase M2

(2012) Barbara Chaneton et al.   NATURE

Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors

(2012) M. McTigue et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Rational Engineering of Enzyme Allosteric Regulation through Sequence Evolution Analysis

(2012) Jae-Seong Yang et al.   PLoS Computational Biology

Allosteric Communication across the Native and Mutated KIT Receptor Tyrosine Kinase

(2012) Elodie Laine et al.   PLoS Computational Biology

Targeting the SH2-Kinase Interface in Bcr-Abl Inhibits Leukemogenesis

(2011) Florian Grebien et al.   CELL

Crystal Structure and Allosteric Activation of Protein Kinase C βII

(2011) Thomas A. Leonard et al.   CELL

Allosteric modulation by protein kinase Cε leads to modified responses of EGF receptor towards tyrosine kinase inhibitors

(2011) Simona Weisheit et al.   CELLULAR SIGNALLING

Regulation of the catalytic activity of the EGF receptor

(2011) Nicholas F Endres et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

(2011) Bruce J. Melancon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nuclear hormone receptors: Allosteric switches

(2011) Iain J. McEwan   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Catalytic Control in the EGF Receptor and Its Connection to General Kinase Regulatory Mechanisms

(2011) Natalia Jura et al.   MOLECULAR CELL

An allosteric Akt inhibitor effectively blocks Akt signaling and tumor growth with only transient effects on glucose and insulin levels in vivo

(2010) Craig Cherrin et al.   CANCER BIOLOGY & THERAPY

Effective Suppression of Vascular Network Formation by Combination of Antibodies Blocking VEGFR Ligand Binding and Receptor Dimerization

(2010) Denis Tvorogov et al.   CANCER CELL

Cell Signaling by Receptor Tyrosine Kinases

(2010) Mark A. Lemmon et al.   CELL

PKCε acts as negative allosteric modulator of EGF receptor signalling

(2010) Simona Weisheit et al.   CELLULAR SIGNALLING

Allosteric Peptide Activators of Pro-Hepatocyte Growth Factor Stimulate Met Signaling

(2010) Kyle E. Landgraf et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors

(2010) Jianming Zhang et al.   NATURE

Cyclotraxin-B, the First Highly Potent and Selective TrkB Inhibitor, Has Anxiolytic Properties in Mice

(2010) Maxime Cazorla et al.   PLoS One

Direct contacts between extracellular membrane-proximal domains are required for VEGF receptor activation and cell signaling

(2010) Y. Yang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Receptor tyrosine kinase transmembrane domains

(2010) Edwin Li et al.   Cell Adhesion & Migration

Structure–function analysis of VEGF receptor activation and the role of coreceptors in angiogenic signaling

(2009) Felix S. Grünewald et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

The Intracellular Juxtamembrane Domain of the Epidermal Growth Factor (EGF) Receptor Is Responsible for the Allosteric Regulation of EGF Binding

(2009) Jennifer L. Macdonald-Obermann et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Minireview: Not Picking Pockets: Nuclear Receptor Alternate-Site Modulators (NRAMs)

(2009) Terry W. Moore et al.   MOLECULAR ENDOCRINOLOGY

A Molecular View of Anti-ErbB Monoclonal Antibody Therapy

(2008) Daniel J. Leahy   CANCER CELL

A Peptoid “Antibody Surrogate” That Antagonizes VEGF Receptor 2 Activity

(2008) D. Gomika Udugamasooriya et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A quantitative analysis of kinase inhibitor selectivity

(2008) Mazen W Karaman et al.   NATURE BIOTECHNOLOGY

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

(2008) P. Jeffrey Conn et al.   NATURE REVIEWS DRUG DISCOVERY

Contacts between membrane proximal regions of the PDGF receptor ectodomain are required for receptor activation but not for receptor dimerization

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

Non-canonical fibroblast growth factor signalling in angiogenesis

(2007) M. Murakami et al.   CARDIOVASCULAR RESEARCH