The GPIIb/IIIa (integrin αIIbβ3) odyssey: a technology-driven saga of a receptor with twists, turns, and even a bend

BS Coller, SJ Shattil - Blood, The Journal of the American …, 2008 - ashpublications.org
Starting 90 years ago with a clinical description by Glanzmann of a bleeding disorder
associated with a defect in platelet function, technologic advances helped investigators …

Single‐chain antibodies for the conformation‐specific blockade of activated platelet integrin αIIbβ3 designed by subtractive selection from naïve human phage …

M Schwarz, P Röttgen, Y Takada, FL Gall… - The FASEB …, 2004 - Wiley Online Library
Binding of fibrinogen to platelet integrin αIIbβ3 mediates platelet aggregation, and thus
inhibition of αIIbβ3 represents a powerful therapeutic strategy in cardiovascular medicine …

Autoreactive T cells to platelet GPIIb-IIIa in immune thrombocytopenic purpura. Role in production of anti-platelet autoantibody.

M Kuwana, J Kaburaki, Y Ikeda - The Journal of clinical …, 1998 - Am Soc Clin Investig
T cell proliferative responses to platelet membrane GPIIb-IIIa were examined in 14 patients
with chronic immune thrombocytopenic purpura (ITP), 7 systemic lupus erythematosus (SLE) …

Specific interaction of the recombinant disintegrin-like domain of MDC-15 (metargidin, ADAM-15) with integrin αvβ3

XP Zhang, T Kamata, K Yokoyama… - Journal of Biological …, 1998 - ASBMB
MDC-15 (ADAM-15, metargidin), a membrane-anchored metalloprotease/disintegrin/
cysteine-rich protein, is expressed on the surface of a wide range of cells and has an RGD …

A specific α5β1-integrin conformation promotes directional integrin translocation and fibronectin matrix formation

K Clark, R Pankov, MA Travis, JA Askari… - Journal of cell …, 2005 - journals.biologists.com
Integrin adhesion receptors are structurally dynamic proteins that adopt a number of
functionally relevant conformations. We have produced a conformation-dependent anti-α5 …

Closed headpiece of integrin αIIbβ3 and its complex with an αIIbβ3-specific antagonist that does not induce opening

J Zhu, J Zhu, A Negri, D Provasi… - Blood, The Journal …, 2010 - ashpublications.org
The platelet integrin αIIbβ3 is essential for hemostasis and thrombosis through its binding of
adhesive plasma proteins. We have determined crystal structures of the αIIbβ3 headpiece in …

Disrupting integrin transmembrane domain heterodimerization increases ligand binding affinity, not valency or clustering

BH Luo, CV Carman, J Takagi… - Proceedings of the …, 2005 - National Acad Sciences
Residues important in the interaction between the 23-residue transmembrane (TM) domains
of the integrin αIIb-and β3-subunits were identified by mutating each non-Leu residue to …

Requirement of α and β subunit transmembrane helix separation for integrin outside-in signaling

J Zhu, CV Carman, M Kim, M Shimaoka… - Blood, The Journal …, 2007 - ashpublications.org
Adhesion to extracellular ligands through integrins regulates cell shape, migration, growth,
and survival. How integrins transmit signals in the outside-to-in direction remains unknown …

Identification of amino acid sequences in fibrinogen γ-chain and tenascin C C-terminal domains critical for binding to integrin αVβ3

K Yokoyama, HP Erickson, Y Ikeda, Y Takada - Journal of Biological …, 2000 - ASBMB
Integrin α v β 3 recognizes fibrinogen γ and α E chain C-terminal domains (γC and α EC) but
does not require the γC dodecapeptide sequence HHLGGAKQAGDV 400–411 for binding to …

Structure-guided design of pure orthosteric inhibitors of αIIbβ3 that prevent thrombosis but preserve hemostasis

BD Adair, JL Alonso, J van Agthoven, V Hayes… - Nature …, 2020 - nature.com
A prevailing dogma is that inhibition of vascular thrombosis by antagonizing platelet integrin
αIIbβ3 cannot be achieved without compromising hemostasis, thus causing serious bleeding …