Structural basis for allostery in integrins and binding to fibrinogen-mimetic therapeutics

No abstract is available for this paper.

• Publication year

  2004

• Venue

  Nature

• Publication date

  2004-11-04

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1038/nature02976PMID 15378069PMCID PMC4372090
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Ribbons.

  2019cited by this paper
• The Relative Influence of Metal Ion Binding Sites in the I-like Domain and the Interface with the Hybrid Domain on Rolling and Firm Adhesion by Integrin α4β7*

  2004cited by this paper
• Locking the beta3 integrin I-like domain into high and low affinity conformations with disulfides.

  2004cited by this paper
• Integrin beta3 regions controlling binding of murine mAb 7E3: implications for the mechanism of integrin alphaIIbbeta3 activation.

  2004cited by this paper
• Activation of integrin beta-subunit I-like domains by one-turn C-terminal alpha-helix deletions.

  2004cited by this paper
• A Specific Interface between Integrin Transmembrane Helices and Affinity for Ligand

  2004cited by this paper
• Activation of integrin β-subunit I-like domains by one-turn C-terminal α-helix deletions

  2004cited by this paper
• Structure of an Integrin-Ligand Complex Deduced from Solution X-ray Scattering and Site-directed Mutagenesis*

  2003cited by this paper
• Stabilizing the open conformation of the integrin headpiece with a glycan wedge increases affinity for ligand

  2003cited by this paper
• Structures of the L I Domain and Its Complex with ICAM-1 Reveal a Shape-Shifting Pathway for Integrin Regulation

  2003cited by this paper
• Bidirectional Transmembrane Signaling by Cytoplasmic Domain Separation in Integrins

  2003cited by this paper
• Structure of integrin α5β1 in complex with fibronectin

  2003cited by this paper
• High Affinity Ligand Binding by Integrins Does Not Involve Head Separation*

  2003cited by this paper
• Bistable regulation of integrin adhesiveness by a bipolar metal ion cluster

  2003cited by this paper
• Conformational Changes in the Integrin βA Domain Provide a Mechanism for Signal Transduction via Hybrid Domain Movement*

  2003cited by this paper
• The ligand-binding face of the semaphorins revealed by the high-resolution crystal structure of SEMA4D

  2003cited by this paper
• HPA-1a phenotype-genotype discrepancy reveals a naturally occurring Arg93Gln substitution in the platelet beta 3 integrin that disrupts the HPA-1a epitope.

  2002cited by this paper
• Integrin activation involves a conformational change in the alpha 1 helix of the beta subunit A-domain.

  2002cited by this paper
• Integrin Activation Involves a Conformational Change in the α1 Helix of the β Subunit A-domain*

  2002cited by this paper
• A structural mechanism of integrin alpha(IIb)beta(3) "inside-out" activation as regulated by its cytoplasmic face.

  2002cited by this paper
• A Structural Mechanism of Integrin αIIbβ3 “Inside-Out” Activation as Regulated by Its Cytoplasmic Face

  2002cited by this paper
• Three-dimensional model of the human platelet integrin alpha IIbbeta 3 based on electron cryomicroscopy and x-ray crystallography.

  2002cited by this paper
• Three-dimensional model of the human platelet integrin αIIbβ3 based on electron cryomicroscopy and x-ray crystallography

  2002cited by this paper
• Predicted and experimental structures of integrins and beta-propellers.

  2002cited by this paper
• Global conformational rearrangements in integrin extracellular domains in outside-in and inside-out signaling.

  2002cited by this paper
• Integrin activation and structural rearrangement

  2002cited by this paper
• Alternative Splice Variants of α7β1Integrin Selectively Recognize Different Laminin Isoforms*

  2002cited by this paper
• Cysteine-rich module structure reveals a fulcrum for integrin rearrangement upon activation

  2002cited by this paper
• The structures of integrins and integrin-ligand complexes: implications for drug design and signal transduction.

  2002cited by this paper
• Crystal Structure of the Extracellular Segment of Integrin αVβ3 in Complex with an Arg-Gly-Asp Ligand

  2002cited by this paper
• Predicted and experimental structures of integrins and β-propellers

  2002cited by this paper
• Amino acid residues in the alpha IIb subunit that are critical for ligand binding to integrin alpha IIbbeta 3 are clustered in the beta-propeller model.

  2001cited by this paper
• C-terminal opening mimics 'inside-out' activation of integrin α5β1

  2001cited by this paper
• Amino Acid Residues in the αIIb Subunit That Are Critical for Ligand Binding to Integrin αIIbβ3 Are Clustered in the β-Propeller Model*

  2001cited by this paper
• C-terminal opening mimics 'inside-out' activation of integrin alpha5beta1.

  2001cited by this paper
• Crystal Structure of the Extracellular Segment of Integrin αVβ3

  2001cited by this paper
• Cell surface receptors.

  2000cited by this paper
• Multiple discontinuous ligand-mimetic antibody binding sites define a ligand binding pocket in integrin alpha(IIb)beta(3).

  2000cited by this paper
• Multiple Discontinuous Ligand-mimetic Antibody Binding Sites Define a Ligand Binding Pocket in Integrin αIIbβ3 *

  2000cited by this paper
• Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.

  2000cited by this paper
• Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.

  1999cited by this paper
• Domains in plexins: links to integrins and transcription factors.

  1999cited by this paper
• Integrin affinity modulation.

  1998cited by this paper
• Platelet GPIIb/IIIa antagonists: the first anti-integrin receptor therapeutics.

  1997cited by this paper
• An extensively modified version of MolScript that includes greatly enhanced coloring capabilities.

  1997cited by this paper
• Ligand binding to integrin alphaIIbbeta3 is dependent on a MIDAS-like domain in the beta3 subunit.

  1996cited by this paper
• Ligand Binding to Integrin αIIbβ3 Is Dependent on a MIDAS-like Domain in the β3 Subunit*

  1996cited by this paper
• The Pla Alloantigen System Is a Sensitive Indicator of the Structural Integrity of the Amino-terminal Domain of the Human Integrin β3 Subunit

  1995cited by this paper
• Crystal structure of the A domain from the alpha subunit of integrin CR3 (CD11b/CD18).

  1995cited by this paper
• The P1A alloantigen system is a sensitive indicator of the structural integrity of the amino-terminal domain of the human integrin beta 3 subunit.

  1995cited by this paper
• Two conformations of the integrin A-domain (I-domain): a pathway for activation?

  1995cited by this paper
• Raster3D Version 2.0. A program for photorealistic molecular graphics.

  1994cited by this paper
• Functional properties of alternatively spliced forms of the Drosophila PS2 integrin alpha subunit.

  1993cited by this paper
• Design of potent and specific integrin antagonists. Peptide antagonists with high specificity for glycoprotein IIb-IIIa.

  1993cited by this paper
• Functional Properties of Alternatively Spliced Forms of the Drosophila PS2 Integrin α Subunit

  1993cited by this paper
• Ligands “activate” integrin αIIbβ3 (platelet GPIIb-IIIa)

  1991cited by this paper
• Ligands "activate" integrin alpha IIb beta 3 (platelet GPIIb-IIIa).

  1991cited by this paper
• Assignment of disulphide bonds in human platelet GPIIIa. A disulphide pattern for the beta-subunits of the integrin family.

  1991cited by this paper
• Mechanisms of cooperativity and allosteric regulation in proteins: By Max Perutz. Pp. 101. Cambridge University Press. 1990. Paperback £11.95, US $17.95

  1990cited by this paper
• The human platelet alloantigens, PlA1 and PlA2, are associated with a leucine33/proline33 amino acid polymorphism in membrane glycoprotein IIIa, and are distinguishable by DNA typing.

  1989cited by this paper
• Mechanisms of cooperativity and allosteric regulation in proteins

  1989cited by this paper
• A murine monoclonal antibody that completely blocks the binding of fibrinogen to platelets produces a thrombasthenic-like state in normal platelets and binds to glycoproteins IIb and/or IIIa.

  1983cited by this paper
• Perspectives Series: Cell Adhesion in Vascular Biology Platelet Gpiib/iiia Antagonists: the First Anti-integrin Receptor Therapeutics

  year unknowncited by this paper

• Allosteric Disulfide Bridges in Integrins: The Molecular Switches of Redox Regulation of Integrin-Mediated Cell Functions

  2025cites this paper
• Targeting asparagine and cysteine in SARS-CoV-2 variants and human pro-inflammatory mediators to alleviate COVID-19 severity; a cross-section and in-silico study

  2025influential citation
• Variations of the Depletion Zones around Inclusions Explain the Complexity of Brush-Induced Depletion Interactions.

  2025cites this paper
• Mn2+ accelerates ligand-binding site activation of αIIbβ3 integrin: Insight from all-atom simulation

  2025influential citation
• Current status and future direction of mechanotransduction mechanisms: Perspectives from cell membrane to nucleus.

  2025cites this paper
• Protective Effect of Biobran/MGN-3, an Arabinoxylan from Rice Bran, Against the Cytotoxic Effects of Polyethylene Nanoplastics in Normal Mouse Hepatocytes: An In Vitro and In Silico Study

  2025cites this paper
• Physical and Mechanobiological Basis of Biological Functions of Platelets

  2025cites this paper
• An αIIbβ3 ligand-mimetic murine monoclonal antibody that produces platelet activation by engaging the FcγIIa receptor

  2025cites this paper
• Inhibition of Metalloproteinases-2, -9, and -14 Suppresses Papillary Thyroid Carcinoma Cell Migration and Invasion

  2025cites this paper
• A Novel KGD-Based αIIbβ3 Antagonist Prevents Arterial Thrombosis While Preserving Hemostasis and Avoiding Thrombocytopenia

  2025cites this paper
• Integrin Alpha8 Beta1 (81): An In-Depth Review of an Overlooked RGD-Binding Receptor

  2025cites this paper
• A Review of Talin- and Integrin-Dependent Molecular Mechanisms in Cancer Invasion and Metastasis

  2025cites this paper
• Langerin+ Dendritic Cells in Cutaneous Fibrosis: The TGF-β1 Signaling Axis

  2025cites this paper
• Multifaceted, unique role of CD11c in leukocyte biology

  2025cites this paper
• Molecular interactions between fibrinogen and 6-methoxydihydrosanguinarine and their modulation of anticancer activity in melanoma A375 cells.

  2025cites this paper
• Investigating the Distribution of Intimin and Invasin in Aeromonas hydrophila and Their Role in Host Tissue Attachment

  2025cites this paper
• The integrin odyssey – a journey full of fundamental discoveries

  2025cites this paper
• The emerging role of human transmembrane RGD-based counter-receptors of integrins in health and disease

  2025cites this paper
• Cancer Immunotherapy via Disruption of Integrin αvβ3 and CD47 Costabilization on Cancer Cell Surface

  2025cites this paper
• Reversible Platelet Aggregation Induced by Low-Temperature Storage in Heparinized Whole Blood Samples

  2025cites this paper
• Integrins in Cardiovascular Health and Disease: Molecular Mechanisms and Therapeutic Opportunities

  2025cites this paper
• Switching Roles—Exploring Concentration-Dependent Agonistic versus Antagonistic Behavior of Integrin Ligands

  2025cites this paper
• Platelet Physiology

  2024cites this paper
• Synthetic integrin antibodies discovered by yeast display reveal αV subunit pairing preferences with β subunits

  2024cites this paper
• Application of Funnel Metadynamics to the Platelet Integrin αIIbβ3 in Complex with an RGD Peptide

  2024cites this paper
• Distinct platelet interactions with soluble and immobilized von Willebrand factor modulate platelet adhesion and aggregation with differential impact on hemostasis and thrombosis

  2024cites this paper
• Current and Future Roles of Glycoprotein IIb–IIIa Inhibitors in Primary Angioplasty for ST-Segment Elevation Myocardial Infarction

  2024cites this paper
• Integrin signalling in joint development, homeostasis and osteoarthritis

  2024cites this paper
• Conformational response of αIIbβ3 and αVβ3 integrins to force.

  2024cites this paper
• Molecular dynamics simulations involving different β-propeller mutations reported in Swiss and French patients correlate with their disease phenotypes

  2024cites this paper
• An αIIbβ3 monoclonal antibody traps a semiextended conformation and allosterically inhibits large ligand binding

  2024cites this paper
• Extracellular matrix-derived materials for tissue engineering and regenerative medicine: A journey from isolation to characterization and application

  2024cites this paper
• Full-length αIIbβ3 cryo-EM structure reveals intact integrin initiate-activation intrinsic architecture.

  2024cites this paper
• Integrins as a bridge between bacteria and cells: key targets for therapeutic wound healing

  2024cites this paper
• Structural insights into the molecular recognition of integrin αVβ3 by RGD-containing ligands: The role of the specificity-determining loop (SDL)

  2024cites this paper
• Structural aspects of CEACAM1 interactions

  2024cites this paper
• Synthetic integrin antibodies discovered by yeast display reveal αV subunit pairing preferences with β subunits

  2024cites this paper
• Subtelomeric plasticity contributes to gene family expansion in the human parasitic flatworm Schistosoma mansoni

  2024cites this paper
• The Integrin Receptors: From Discovery to Structure to Medicines

  2024cites this paper
• Contributions of the individual domains of αIIbβ3 integrin to its extension: Insights from multiscale modeling

  2024influential citation
• Molecular mechanisms of catch bonds and their implications for platelet hemostasis

  2023influential citation
• The Force-Dependent Mechanism of an Integrin α4β7–MAdCAM-1 Interaction

  2023cites this paper
• Integrin signaling in cancer: bidirectional mechanisms and therapeutic opportunities

  2023cites this paper
• Targeting the αVβ3/NgR2 pathway in neuroendocrine prostate cancer

  2023cites this paper
• Irisin acts through its integrin receptor in a two-step process involving extracellular Hsp90α.

  2023cites this paper
• Steered molecular dynamics simulation of force triggering the integrin α_IIbβ_3 extension via its ligand

  2023cites this paper
• Family-wide analysis of integrin structures predicted by AlphaFold2

  2023influential citation
• A single F153Sβ3 mutation causes constitutive integrin αIIbβ3 activation in a variant form of Glanzmann thrombasthenia

  2023cites this paper
• Molecular basis for the recognition of 24-(S)-hydroxycholesterol by integrin αvβ3

  2023cites this paper
• Comparative study of interaction energies between αIIbβ3 integrin and the peptidic, peptidomimetic and non-peptidic ligands by quantum mechanics FMO-PIEDA calculations

  2023cites this paper
• Family-wide analysis of integrin structures predicted by AlphaFold2

  2023cites this paper
• A molecular arm: the molecular bending–unbending mechanism of integrin

  2023cites this paper
• Cryo-EM structures of full-length integrin αIIbβ3 in native lipids

  2023cites this paper
• Lineage-Specific Induced Pluripotent Stem Cell–Derived Smooth Muscle Cell Modeling Predicts Integrin Alpha-V Antagonism Reduces Aortic Root Aneurysm Formation in Marfan Syndrome Mice

  2023cites this paper
• Use of Ecto-Tagged Integrins to Monitor Integrin Exocytosis and Endocytosis.

  2023cites this paper
• Glanzmann Thrombasthenia in Pakistani Patients: Identification of 7 Novel Pathogenic Variants in the Fibrinogen Receptor αIIbβ3

  2023cites this paper
• Molecular Modeling Insights into the Structure and Behavior of Integrins: A Review

  2023cites this paper
• INTEGRINS: A BEDSIDE TO BENCH TO BEDSIDE STORY.

  2023cites this paper
• Structural analysis of peptide binding to integrins for cancer detection and treatment

  2023cites this paper
• Full-length αIIbβ3 CryoEM structure reveals intact integrin initiate-activation intrinsic architecture

  2023cites this paper
• The challenges and opportunities of αvβ3-based therapeutics in cancer: from bench to clinical trials.

  2023cites this paper
• Molecular basis of conformational changes and mechanics of integrins

  2023cites this paper
• Targeting integrin pathways: mechanisms and advances in therapy

  2023cites this paper
• Integrin-Dependent Transient Density Increase in Detergent-Resistant Membrane Rafts in Platelets Activated by Thrombin

  2023cites this paper
• Critical Analysis of Thrombocytopenia Associated With Glycoprotein IIb/IIIa Inhibitors and Potential Role of Zalunfiban, a Novel Small Molecule Glycoprotein Inhibitor, in Understanding the Mechanism(s)

  2023cites this paper
• Development of the Integrated Computer Simulation Model of the Intracellular, Transmembrane, and Extracellular Domain of Platelet Integrin α IIb β 3 (Platelet Membrane Glycoprotein: GPIIb–IIIa)

  2023cites this paper
• Molecular basis of clot retraction and its role in wound healing.

  2022cites this paper
• De novo functional groups designed to enhance neuronal integrin α5β1 binding using deep reinforcement learning

  2022cites this paper
• Dynamics of integrin α5β1, fibronectin, and their complex reveal sites of interaction and conformational change

  2022cites this paper
• A Biomolecular Toolbox for Precision Nanomotors

  2022cites this paper
• Platelet cancer cell interplay as a new therapeutic target.

  2022cites this paper
• Histomorphometry of Ossification in Functionalised Ceramics with Tripeptide Arg-Gly-Asp (RGD): An In Vivo Study

  2022cites this paper
• Description and Clinical Management of Patients With Glanzmann's Thrombasthenia in a University Hospital, a Referral Center Specialized in Hemostasis, in Bogotá, Colombia

  2022cites this paper
• Cryo-electron Microscopic Analysis of Single-Pass Transmembrane Receptors.

  2022cites this paper
• Junctional epithelium and hemidesmosomes: Tape and rivets for solving the “percutaneous device dilemma” in dental and other permanent implants

  2022cites this paper
• The extracellular Ero1α/PDI electron transport system regulates platelet function by increasing glutathione reduction potential

  2022cites this paper
• Regulation of integrin α5β1 conformational states and intrinsic affinities by metal ions and the ADMIDAS

  2022cites this paper
• Integrin Regulated Autoimmune Disorders: Understanding the Role of Mechanical Force in Autoimmunity

  2022cites this paper
• Structural insights into the function-modulating effects of nanobody binding to the integrin receptor αMβ2

  2022cites this paper
• The structural basis of β2 integrin intra-cellular multi-protein complexes

  2022cites this paper
• αIIbβ3 integrin intermediates: from molecular dynamics to adhesion assembly.

  2022cites this paper
• Structure-Based Discovery of a Novel Class of Small-Molecule Pure Antagonists of Integrin αVβ3

  2022cites this paper
• Full-length αIIbβ3 CryoEM structure reveals intact integrin initiate-activation intrinsic architecture

  2022cites this paper
• Integrin Conformational Dynamics and Mechanotransduction

  2022influential citation
• Novel approaches to antiplatelet therapy.

  2022cites this paper
• It's the water! The open and shut case of drug-induced integrin activation.

  2022cites this paper
• A general chemical principle for creating closure-stabilizing integrin inhibitors.

  2022cites this paper
• Integrin β1 and the Repair after Nervous System Injury

  2022cites this paper
• Ectopic Tumor VCAM-1 Expression in Cancer Metastasis and Therapy Resistance

  2022cites this paper
• RGD-Binding Integrins Revisited: How Recently Discovered Functions and Novel Synthetic Ligands (Re-)Shape an Ever-Evolving Field

  2021cites this paper
• Platelets, Constant and Cooperative Companions of Sessile and Disseminating Tumor Cells, Crucially Contribute to the Tumor Microenvironment

  2021cites this paper
• Complement Receptors and Their Role in Leukocyte Recruitment and Phagocytosis

  2021cites this paper
• Electron microscopy shows that binding of monoclonal antibody PT25-2 primes integrin αIIbβ3 for ligand binding.

  2021cites this paper
• Mechanisms of thrombosis and research progress on targeted antithrombotic drugs.

  2021cites this paper
• Overcoming challenges in developing small molecule inhibitors for GPVI and CLEC-2

  2021cites this paper
• Measurement of Integrin Activation and Conformational Changes on the Cell Surface by Soluble Ligand and Antibody Binding Assays.

  2021cites this paper
• The Lectin-Like Domain of Thrombomodulin Inhibits β1 Integrin-Dependent Binding of Human Breast Cancer-Derived Cell Lines to Fibronectin

  2021cites this paper
• Structural insights into integrin α5β1 opening by fibronectin ligand

  2021cites this paper
• Structural determinants of the integrin transmembrane domain required for bidirectional signal transmission across the cell membrane

  2021cites this paper
• TCN1 Deficiency Inhibits the Malignancy of Colorectal Cancer Cells by Regulating the ITGB4 Pathway

  2021cites this paper