9HZ3

PCSK9 AZD0780 complex

This is a non-PDB format compatible entry.

Summary for 9HZ3

• Entry DOI: 10.2210/pdb9hz3/pdb
• Descriptor: Proprotein convertase subtilisin/kexin type 9, 1-[6-[[(1~{S},3~{S})-3-[[5-[bis(fluoranyl)methoxy]pyrimidin-2-yl]amino]cyclopentyl]amino]pyridin-3-yl]pyridin-2-one, ... (4 entities in total)
• Functional Keywords: pcsk9 azd0780, protein binding
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 2
• Total formula weight: 76574.38

Authors

Johansson, P. (deposition date: 2025-01-13, release date: 2026-05-27, Last modification date: 2026-07-01)

Primary citation

Vega, R.B.,O'Mahony, G.,Barbour, A.M.,Yu, H.,Knochel, J.,Brengdahl, J.,Hochdorfer, T.,Bergenholm, L.,Toppner Carlsson, E.,Ahnmark, A.,Underwood, C.R.,Rudvik, A.,Carter, D.,Laru, J.,Gutgsell, A.,Twaddle, L.,Garkaviy, P.,Bogstedt, A.,Hurt-Camejo, E.,Miliotis, T.,Ryaboshapkina, M.,Hober, A.,Hubbard, B.,Serrano-Wu, M.,Kaushik, V.,Geschwindner, S.,McCarthy, M.C.,Linden, D.,Rosenmeier, J.B.
Laroprovstat, the First Oral Small-Molecule PCSK9 Inhibitor for the Treatment of Hypercholesterolemia: Results From a Randomized, Single-Blind, Placebo-Controlled Phase 1 Trial in Treatment-Naive Patients.
Circulation, 153:1999-2010, 2026

PubMed Abstract: Inhibition of proprotein convertase subtilisin/kexin type 9 (PCSK9) is an effective therapy for reducing low-density lipoprotein (LDL) cholesterol (LDL-C) in adults with hyperlipidemia, including heterozygous familial hypercholesterolemia, thereby lowering cardiovascular risk. Current PCSK9 inhibitors are injectable therapies; no oral small-molecule PCSK9 inhibitor has yet been approved.

PubMed: 42137960
DOI: 10.1161/CIRCULATIONAHA.125.075973

Experimental method

X-RAY DIFFRACTION (1.432 Å)