6GWQ

Crystal Structure of Stabilized Active Plasminogen Activator Inhibitor-1 (PAI-1-stab) in Complex with an Inhibitory Nanobody (VHH-2g-42)

Summary for 6GWQ

• Entry DOI: 10.2210/pdb6gwq/pdb
• Descriptor: Plasminogen Activator Inhibitor-1, VHH-2g-42 (3 entities in total)
• Functional Keywords: plasminogen activator inhibitor-1, pai-1, pai-1-stab, serpin, protease inhibitor, serine protease inhibitor, nanobody, antibody fragment, protein complex, hydrolase
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 2
• Total formula weight: 55503.26

Authors

Sillen, M.,Weeks, S.D.,Strelkov, S.V.,Declerck, P.J. (deposition date: 2018-06-25, release date: 2020-01-01, Last modification date: 2024-01-17)

Primary citation

Sillen, M.,Weeks, S.D.,Zhou, X.,Komissarov, A.A.,Florova, G.,Idell, S.,Strelkov, S.V.,Declerck, P.J.
Molecular mechanism of two nanobodies that inhibit PAI-1 activity reveals a modulation at distinct stages of the PAI-1/plasminogen activator interaction.
J.Thromb.Haemost., 18:681-692, 2020

PubMed Abstract: Plasminogen activator inhibitor-1 (PAI-1), a key inhibitor of plasminogen activators (PAs) tissue-type PA (tPA) and urokinase-type PA (uPA) plays a crucial role in many (patho)physiological processes (e.g., cardiovascular disease, tissue fibrosis) as well as in many age-related pathologies. Therefore, much effort has been put into the development of small molecule or antibody-based PAI-1 inhibitors.

PubMed: 31858714
DOI: 10.1111/jth.14716

Experimental method

X-RAY DIFFRACTION (2.32 Å)