Integrins as therapeutic targets: lessons and opportunities (Q37795552)

23 August 2017

title

Integrins as therapeutic targets: lessons and opportunities (English)

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23 August 2017

Marian Brennan

2

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Dermot Cox

object named as

Dermot Cox

series ordinal

1

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author name string

Niamh Moran

series ordinal

3

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23 August 2017

publication date

1 October 2010

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Nature Reviews Drug Discovery

23 August 2017

published in

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23 August 2017

volume

9

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23 August 2017

issue

10

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23 August 2017

page(s)

804-820

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Structure of integrin, a glycoprotein involved in the transmembrane linkage between fibronectin and actin

23 August 2017

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Implantation mechanisms: insights from the sheep.

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Integrins: the keys to unlocking angiogenesis

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Platelet membrane defects in Glanzmann's thrombasthenia. Evidence for decreased amounts of two major glycoproteins

31 March 2020

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Intravenous glycoprotein IIb/IIIa antagonists: their benefits, problems and future developments

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Development of eptifibatide

31 March 2020

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Platelet glycoprotein IIb/IIIa integrin blockade with eptifibatide in coronary stent intervention: the ESPRIT trial: a randomized controlled trial

31 March 2020

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Increased mortality with oral platelet glycoprotein IIb/IIIa antagonists: a meta-analysis of phase III multicenter randomized trials

31 March 2020

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Oral GPIIb/IIIa antagonists: what went wrong?

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Defects in the leukocyte adhesion cascade

31 March 2020

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Prevention of experimental autoimmune encephalomyelitis by antibodies against alpha 4 beta 1 integrin.

31 March 2020

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Natalizumab and progressive multifocal leukoencephalopathy: migrating towards safe adhesion molecule therapy in multiple sclerosis

31 March 2020

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Therapeutic anti-integrin (alpha4 and alphaL) monoclonal antibodies: two-edged swords?

31 March 2020

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Blocking adhesion molecules as therapy for multiple sclerosis: natalizumab

31 March 2020

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Effect of natalizumab on clinical and radiological disease activity in multiple sclerosis: a retrospective analysis of the Natalizumab Safety and Efficacy in Relapsing-Remitting Multiple Sclerosis (AFFIRM) study

31 March 2020

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A randomized, placebo-controlled trial of natalizumab for relapsing multiple sclerosis

31 March 2020

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Natalizumab plus interferon beta-1a for relapsing multiple sclerosis

31 March 2020

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Roles of integrin activation in eosinophil function and the eosinophilic inflammation of asthma

31 March 2020

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Progressive multifocal leukoencephalopathy and other disorders caused by JC virus: clinical features and pathogenesis

31 March 2020

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31 March 2020

Multiple sclerosis woes

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Reactivation of human herpesvirus-6 in natalizumab treated multiple sclerosis patients

31 March 2020

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Extended efalizumab therapy improves chronic plaque psoriasis: results from a randomized phase III trial.

31 March 2020

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CLinical experience acquired with the efalizumab (Raptiva) (CLEAR) trial in patients with moderate-to-severe plaque psoriasis: results from a phase III international randomized, placebo-controlled trial.

31 March 2020

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A novel targeted T-cell modulator, efalizumab, for plaque psoriasis

31 March 2020

1 reference

Efalizumab for patients with moderate to severe plaque psoriasis: a randomized controlled trial.

31 March 2020

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Impact of efalizumab on patient-reported outcomes in high-need psoriasis patients: results of the international, randomized, placebo-controlled Phase III Clinical Experience Acquired with Raptiva (CLEAR) trial [NCT00256139].

31 March 2020

1 reference

Efalizumab: results of a 3-year continuous dosing study for the long-term control of psoriasis

31 March 2020

1 reference

Progressive multifocal leukoencephalopathy in patients on immunomodulatory therapies

31 March 2020

1 reference

Integrins: roles in cancer development and as treatment targets

31 March 2020

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Integrins in angiogenesis and lymphangiogenesis

31 March 2020

1 reference

An open-label, multicenter, phase 2a study to assess the feasibility of imaging metastases in late-stage cancer patients with the alpha v beta 3-selective angiogenesis imaging agent 99mTc-NC100692.

31 March 2020

1 reference

Phase I trial of the positron-emitting Arg-Gly-Asp (RGD) peptide radioligand 18F-AH111585 in breast cancer patients

31 March 2020

1 reference

Alpha-v integrins as therapeutic targets in oncology.

31 March 2020

1 reference

Integrin-associated Lyn kinase promotes cell survival by suppressing acid sphingomyelinase activity

31 March 2020

1 reference

alphaV integrin promotes in vitro and in vivo survival of cells in metastatic melanoma

31 March 2020

1 reference

Pharmacodynamic (phase 0) study using etaracizumab in advanced melanoma

31 March 2020

1 reference

A randomized phase 2 study of etaracizumab, a monoclonal antibody against integrin alpha(v)beta(3), + or - dacarbazine in patients with stage IV metastatic melanoma

31 March 2020

1 reference

Phase I and pharmacokinetic study of etaracizumab (Abegrin), a humanized monoclonal antibody against alphavbeta3 integrin receptor, in patients with advanced solid tumors.

31 March 2020

1 reference

Phase I/IIa study of cilengitide and temozolomide with concomitant radiotherapy followed by cilengitide and temozolomide maintenance therapy in patients with newly diagnosed glioblastoma

31 March 2020

1 reference

Randomized phase II study of cilengitide, an integrin-targeting arginine-glycine-aspartic acid peptide, in recurrent glioblastoma multiforme

31 March 2020

1 reference

Phase I clinical trial of cilengitide in children with refractory brain tumors: Pediatric Brain Tumor Consortium Study PBTC-012.

31 March 2020

1 reference

Integrins as target: first phase III trial launches, but questions remain

31 March 2020

1 reference

Evaluation of the safety, pharmacokinetics and treatment effects of an alpha(nu)beta(3) integrin inhibitor on bone turnover and disease activity in men with hormone-refractory prostate cancer and bone metastases

31 March 2020

1 reference

Regulation of integrin alpha vbeta 3-mediated endothelial cell migration and angiogenesis by integrin alpha5beta1 and protein kinase A.

31 March 2020

1 reference

Regulation of angiogenesis in vivo by ligation of integrin alpha5beta1 with the central cell-binding domain of fibronectin

31 March 2020

1 reference

Mechanism-based receptor-binding model to describe the pharmacokinetic and pharmacodynamic of an anti-α5β1 integrin monoclonal antibody (volociximab) in cancer patients

31 March 2020

1 reference

Volociximab, a chimeric monoclonal antibody that specifically binds alpha5beta1 integrin: a phase I, pharmacokinetic, and biological correlative study

31 March 2020

1 reference

Single and combined effects of alphavbeta3- and alpha5beta1-integrins on capillary tube formation in a human fibrinous matrix

31 March 2020

1 reference

Cell integrins: commonly used receptors for diverse viral pathogens

31 March 2020

1 reference

The interaction of bacterial pathogens with platelets

31 March 2020

1 reference

Roles for fibrinogen, immunoglobulin and complement in platelet activation promoted by Staphylococcus aureus clumping factor A.

31 March 2020

1 reference

Elucidating the role of Staphylococcus epidermidis serine-aspartate repeat protein G in platelet activation.

31 March 2020

1 reference

Fibronectin-binding proteins of Staphylococcus aureus mediate activation of human platelets via fibrinogen and fibronectin bridges to integrin GPIIb/IIIa and IgG binding to the FcgammaRIIa receptor

31 March 2020

1 reference

alpha(6) Integrin is the main receptor of human papillomavirus type 16 VLP.

31 March 2020

1 reference

Rotavirus-neutralizing antibodies inhibit virus binding to integrins alpha 2 beta 1 and alpha 4 beta 1.

31 March 2020

1 reference

Rotaviruses interact with alpha4beta7 and alpha4beta1 integrins by binding the same integrin domains as natural ligands

31 March 2020

1 reference

Integrin-using rotaviruses bind alpha2beta1 integrin alpha2 I domain via VP4 DGE sequence and recognize alphaXbeta2 and alphaVbeta3 by using VP7 during cell entry

31 March 2020

1 reference

Alpha5beta1-integrin controls ebolavirus entry by regulating endosomal cathepsins

31 March 2020

1 reference

Human CD18 is the functional receptor for Aggregatibacter actinomycetemcomitans leukotoxin

31 March 2020

1 reference

Monomeric expression of bovine beta2-integrin subunits reveals their role in Mannheimia haemolytica leukotoxin-induced biological effects

31 March 2020

1 reference

RTX cytotoxins recognize beta2 integrin receptors through N-linked oligosaccharides

31 March 2020

1 reference

Integrin subunit CD18 Is the T-lymphocyte receptor for the Helicobacter pylori vacuolating cytotoxin

31 March 2020

1 reference

Helicobacter exploits integrin for type IV secretion and kinase activation

31 March 2020

1 reference

Involvement of alpha5beta1-integrin and TNF-alpha in Staphylococcus aureus alpha-toxin-induced death of epithelial cells

31 March 2020

1 reference

Heterodimeric integrin complexes containing beta1-integrin promote internalization and lethality of anthrax toxin

31 March 2020

1 reference

The extracellular matrix protein mindin serves as an integrin ligand and is critical for inflammatory cell recruitment

31 March 2020

1 reference

Structure of the F-spondin domain of mindin, an integrin ligand and pattern recognition molecule

31 March 2020

1 reference

Polymorphisms and haplotypes of integrinalpha1 (ITGA1) are associated with bone mineral density and fracture risk in postmenopausal Koreans

31 March 2020

1 reference

Integrin beta3 Leu33Pro polymorphism and risk of hip fracture: 25 years follow-up of 9233 adults from the general population

31 March 2020

1 reference

Effect of L-000845704, an alphaVbeta3 integrin antagonist, on markers of bone turnover and bone mineral density in postmenopausal osteoporotic women

31 March 2020

1 reference

The final steps of integrin activation: the end game

31 March 2020

1 reference

Computationally designed peptide inhibitors of protein-protein interactions in membranes

31 March 2020

1 reference

Global conformational rearrangements in integrin extracellular domains in outside-in and inside-out signaling

31 March 2020

1 reference

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

31 March 2020

1 reference

Crystal structure of the extracellular segment of integrin alpha Vbeta3

31 March 2020

1 reference

Solution properties of full-length integrin alpha(IIb)beta3 refined models suggest environment-dependent induction of alternative bent /extended resting states

31 March 2020

1 reference

Linking integrin conformation to function

31 March 2020

1 reference

Therapeutic antagonists and conformational regulation of integrin function

31 March 2020

1 reference

Integrin structure, allostery, and bidirectional signaling

31 March 2020

1 reference

Transmembrane domain helix packing stabilizes integrin alphaIIbbeta3 in the low affinity state

31 March 2020

1 reference

Mechanisms that regulate adaptor binding to beta-integrin cytoplasmic tails

31 March 2020

1 reference

Ligand switching in cell-permeable peptides: manipulation of the alpha-integrin signature motif

31 March 2020

1 reference

A structural mechanism of integrin alpha(IIb)beta(3) "inside-out" activation as regulated by its cytoplasmic face

31 March 2020

1 reference

Association of the membrane proximal regions of the alpha and beta subunit cytoplasmic domains constrains an integrin in the inactive state

31 March 2020

1 reference

Bidirectional transmembrane signaling by cytoplasmic domain separation in integrins

31 March 2020

1 reference

Integrin beta cytoplasmic domain interactions with phosphotyrosine-binding domains: a structural prototype for diversity in integrin signaling

31 March 2020

1 reference

The cytosolic protein talin induces an intermediate affinity integrin alphaLbeta2.

31 March 2020

1 reference

Talin 1 and paxillin facilitate distinct steps in rapid VLA-4-mediated adhesion strengthening to vascular cell adhesion molecule 1

31 March 2020

1 reference

An essential role for talin during alpha(M)beta(2)-mediated phagocytosis

31 March 2020

1 reference

A role for talin in presynaptic function

31 March 2020

1 reference

Disruption of the talin gene arrests mouse development at the gastrulation stage

31 March 2020

1 reference

The antithrombotic potential of selective blockade of talin-dependent integrin alpha IIb beta 3 (platelet GPIIb-IIIa) activation

31 March 2020

1 reference

Structural basis of integrin activation by talin

31 March 2020

1 reference

The tail of integrins, talin, and kindlins

31 March 2020

1 reference

Kindlin-1 and -2 directly bind the C-terminal region of beta integrin cytoplasmic tails and exert integrin-specific activation effects

31 March 2020

1 reference

Integrin-linked kinase associated with integrin activation

31 March 2020

1 reference

Integrin cytoplasmic domains mediate inside-out signal transduction

31 March 2020

1 reference

A deletion in the ?? subunit locks platelet integrin ??IIb??3 into a high affinity state

31 March 2020

1 reference

Integrin affinity modulation

31 March 2020

1 reference

Regulation of Integrin αIIbβ3Activation by Distinct Regions of Its Cytoplasmic Tails†

31 March 2020

1 reference

A novel functional role for the highly conserved alpha-subunit KVGFFKR motif distinct from integrin alphaIIbbeta3 activation processes

31 March 2020

1 reference

Analysis of Fyn function in hemostasis and alphaIIbbeta3-integrin signaling

31 March 2020

1 reference

Solution structures of the cytoplasmic tail complex from platelet integrin alpha IIb- and beta 3-subunits

31 March 2020

1 reference

Differential binding of ICln in platelets to integrin-derived activating and inhibitory peptides

31 March 2020

1 reference

Binding of paxillin to alpha4 integrins modifies integrin-dependent biological responses

31 March 2020

1 reference

Paxillin selectively associates with constitutive and chemoattractant-induced high-affinity alpha4beta1 integrins: implications for integrin signaling.

31 March 2020

1 reference

Efalizumab binding to the LFA-1 L I domain blocks ICAM-1 binding via steric hindrance

31 March 2020

1 reference

The role of the divalent cation in the structure of the I domain from the CD11a/CD18 integrin

31 March 2020

1 reference

Structures of the alpha L I domain and its complex with ICAM-1 reveal a shape-shifting pathway for integrin regulation

31 March 2020

1 reference

Generation of an LFA-1 antagonist by the transfer of the ICAM-1 immunoregulatory epitope to a small molecule

31 March 2020

1 reference

Competition between intercellular adhesion molecule-1 and a small-molecule antagonist for a common binding site on the alphal subunit of lymphocyte function-associated antigen-1.

31 March 2020

1 reference

Rolling adhesion through an extended conformation of integrin alphaLbeta2 and relation to alpha I and beta I-like domain interaction

31 March 2020

1 reference

Small molecule integrin antagonists that bind to the beta2 subunit I-like domain and activate signals in one direction and block them in the other

31 March 2020

1 reference

Small molecule inhibitors induce conformational changes in the I domain and the I-like domain of lymphocyte function-associated antigen-1. Molecular insights into integrin inhibition

31 March 2020

1 reference

Intersubunit signal transmission in integrins by a receptor-like interaction with a pull spring.

31 March 2020

1 reference

Structure of an allosteric inhibitor of LFA-1 bound to the I-domain studied by crystallography, NMR, and calorimetry

31 March 2020

1 reference

Design of LFA-1 antagonists based on a 2,3-dihydro-1H-pyrrolizin-5(7aH)-one scaffold

31 March 2020

1 reference

Structural basis for LFA-1 inhibition upon lovastatin binding to the CD11a I-domain

31 March 2020

1 reference

Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-

31 March 2020

1 reference

1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1

31 March 2020

1 reference

Improved lymphocyte function-associated antigen-1 (LFA-1) inhibition by statin derivatives: molecular basis determined by x-ray analysis and monitoring of LFA-1 conformational changes in vitro and ex vivo

31 March 2020

1 reference

Monoclonal antibodies that block the activity of leukocyte function-associated antigen 1 recognize three discrete epitopes in the inserted domain of CD11a

31 March 2020

1 reference

The I domain of integrin leukocyte function-associated antigen-1 is involved in a conformational change leading to high affinity binding to ligand intercellular adhesion molecule 1 (ICAM-1)

31 March 2020

1 reference

Crystal structure of isoflurane bound to integrin LFA-1 supports a unified mechanism of volatile anesthetic action in the immune and central nervous systems

31 March 2020

1 reference

The volatile anesthetic isoflurane perturbs conformational activation of integrin LFA-1 by binding to the allosteric regulatory cavity

31 March 2020

1 reference

Blocking LFA-1 activation with lovastatin prevents graft-versus-host disease in mouse bone marrow transplantation.

31 March 2020

1 reference

Therapeutic integrin inhibition: allosteric and activation-specific inhibition strategies may surpass the initial ligand-mimetic strategies

31 March 2020

1 reference

AL-57, a ligand-mimetic antibody to integrin LFA-1, reveals chemokine-induced affinity up-regulation in lymphocytes.

31 March 2020

1 reference

Integrin beta3 regions controlling binding of murine mAb 7E3: implications for the mechanism of integrin alphaIIbbeta3 activation

31 March 2020

1 reference

Crystal structure of the extracellular segment of integrin alpha Vbeta3 in complex with an Arg-Gly-Asp ligand

31 March 2020

1 reference

Blocking alpha4-integrins - A small molecule approach to treatment of multiple sclerosis

31 March 2020

1 reference

Synthesis and SAR of pyridazinone-substituted phenylalanine amide alpha4 integrin antagonists

31 March 2020

1 reference

Treatment of ulcerative colitis with a humanized antibody to the alpha4beta7 integrin

31 March 2020

1 reference

Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin

31 March 2020

1 reference

Intrinsic activating properties of GP IIb/IIIa blockers

31 March 2020

2 references

31 March 2020

12 December 2020

Application of high-throughput screening to identify a novel alphaIIb-specific small- molecule inhibitor of alphaIIbbeta3-mediated platelet interaction with fibrinogen.

1 reference

UR-3216: a new generation oral platelet GPIIb/IIIa antagonist

31 March 2020

1 reference

Antithrombotic effects of targeting alphaIIbbeta3 signaling in platelets

31 March 2020

1 reference

Novel integrin-specific targets for anti-platelet therapies

31 March 2020

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Integrin-associated proteins as potential therapeutic targets

31 March 2020

1 reference

Computational design of peptides that target transmembrane helices

31 March 2020

1 reference

New approaches to blockade of alpha4-integrins, proven therapeutic targets in chronic inflammation

31 March 2020

1 reference

A small molecule that inhibits the interaction of paxillin and alpha 4 integrin inhibits accumulation of mononuclear leukocytes at a site of inflammation

31 March 2020

1 reference

Synthetic D-amino acid peptide inhibits tumor cell motility on laminin-5.

31 March 2020

1 reference

Phase 1 trial of the antiangiogenic peptide ATN-161 (Ac-PHSCN-NH(2)), a beta integrin antagonist, in patients with solid tumours

31 March 2020

1 reference

The platelet integrin alpha IIbbeta 3 has an endogenous thiol isomerase activity.

31 March 2020

1 reference

Integrin-linked kinase--essential roles in physiology and cancer biology.

31 March 2020

1 reference

Integrin-linked kinase: a potential therapeutic target for the treatment of glioma.

31 March 2020

1 reference

QLT0267, a small molecule inhibitor targeting integrin-linked kinase (ILK), and docetaxel can combine to produce synergistic interactions linked to enhanced cytotoxicity, reductions in P-AKT levels, altered F-actin architecture and improved treatmen

31 March 2020

1 reference

Effects of the integrin-linked kinase inhibitor QLT0267 on squamous cell carcinoma of the head and neck

31 March 2020

1 reference

Combined inhibition of integrin linked kinase and FMS-like tyrosine kinase 3 is cytotoxic to acute myeloid leukemia progenitor cells.

31 March 2020

1 reference

Drug-induced immune thrombocytopenia

31 March 2020

1 reference

The incidence and significance of anti-natalizumab antibodies: results from AFFIRM and SENTINEL.

31 March 2020

1 reference

Agonizing integrin antagonists?

31 March 2020

1 reference

Stimulation of tumor growth and angiogenesis by low concentrations of RGD-mimetic integrin inhibitors.

31 March 2020

1 reference

Evidence of platelet activation during treatment with a GPIIb/IIIa antagonist in patients presenting with acute coronary syndromes

31 March 2020

1 reference

Alpha4-integrin antagonism--an effective approach for the treatment of inflammatory diseases?

31 March 2020

1 reference

Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)n

31 March 2020

1 reference

A structural basis for integrin activation by the cytoplasmic tail of the alpha IIb-subunit

31 March 2020

1 reference

Talin controls integrin activation

31 March 2020

1 reference

Identification of a novel calcium-binding protein that interacts with the integrin alphaIIb cytoplasmic domain

31 March 2020

1 reference

Ancient ubiquitous protein 1 binds to the conserved membrane-proximal sequence of the cytoplasmic tail of the integrin alpha subunits that plays a crucial role in the inside-out signaling of alpha IIbbeta 3

31 March 2020

1 reference

Protein phosphatase 1 associates with the integrin alphaIIb subunit and regulates signaling

31 March 2020

1 reference

Protein phosphatase 2A negatively regulates integrin alpha(IIb)beta(3) signaling

31 March 2020

1 reference

Identification and characterization of triosephosphate isomerase that specifically interacts with the integrin alphaIIb cytoplasmic domain

31 March 2020

1 reference

Compartmentalization regulates the interaction between the platelet integrin alpha IIb beta 3 and ICln

31 March 2020

1 reference

RN181, a novel ubiquitin E3 ligase that interacts with the KVGFFKR motif of platelet integrin alpha(IIb)beta3.

31 March 2020

1 reference

Structure of an integrin with an αI domain, complement receptor type 4

31 March 2020

1 reference

VMD: visual molecular dynamics

31 March 2020

1 reference

Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp

31 March 2020

1 reference

Orbofiban: an orally active GPIIb/IIIa platelet receptor antagonist

31 March 2020

1 reference

Xemilofiban/orbofiban: insight into drug development.

31 March 2020

1 reference

Orally active fibrinogen receptor antagonists. 2. Amidoximes as prodrugs of amidines

31 March 2020

1 reference

Design and synthesis of a new class of selective integrin alpha5beta1 antagonists

31 March 2020

1 reference

A deletion in the alpha subunit locks platelet integrin alpha IIb beta 3 into a high affinity state

31 March 2020

1 reference

12 December 2020

Randomised placebo-controlled trial of effect of eptifibatide on complications of percutaneous coronary intervention: IMPACT-II. Integrilin to Minimise Platelet Aggregation and Coronary Thrombosis-II

1 reference

12 December 2020

Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion

1 reference

12 December 2020

1 reference

12 December 2020

Inhibition of platelet glycoprotein IIb/IIIa with eptifibatide in patients with acute coronary syndromes

1 reference

12 December 2020

Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty

1 reference

12 December 2020

Structural basis of integrin transmembrane activation

1 reference

12 December 2020

Effects of platelet glycoprotein IIb/IIIa blockade with tirofiban on adverse cardiac events in patients with unstable angina or acute myocardial infarction undergoing coronary angioplasty. The RESTORE Investigators. Randomized Efficacy Study of Tiro

1 reference

12 December 2020

Inhibition of the platelet glycoprotein IIb/IIIa receptor with tirofiban in unstable angina and non-Q-wave myocardial infarction

1 reference

12 December 2020

Association between ligand-induced conformational changes of integrin IIbbeta3 and IIbbeta3-mediated intracellular Ca2+ signaling

1 reference

12 December 2020

Sulfonamide derivative, E7820, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium

1 reference

12 December 2020

Identifiers

DOI

10.1038/NRD3266

1 reference

Dimensions Publication ID

23 August 2017

1008531438

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