7EEK

Structure of Human serum albumin-Au compound complex

Summary for 7EEK

• Entry DOI: 10.2210/pdb7eek/pdb
• Descriptor: Serum albumin, PALMITOLEIC ACID, 11-methyl-2-oxa-4-thia-6,7-diaza-3$l^{3}-auratricyclo[7.4.0.0^{3,7}]trideca-1(13),5,9,11-tetraen-5-amine (3 entities in total)
• Functional Keywords: delivery, complex, transport protein
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 2
• Total formula weight: 136549.30

Authors

Yang, F.,Zhang, J.Z. (deposition date: 2021-03-18, release date: 2022-03-23, Last modification date: 2025-08-20)

Primary citation

Zhang, J.,Jiang, M.,Li, S.,Zhang, Z.,Sun, H.,Yang, F.,Liang, H.
Developing a Novel Anticancer Gold(III) Agent to Integrate Chemotherapy and Immunotherapy.
J.Med.Chem., 64:6777-6791, 2021

PubMed Abstract: To effectively treat gastric cancer, we innovatively attempted to develop a metal agent to integrate immunotherapy and chemotherapy by dual targeting the cellular components in the tumor microenvironment (TME) based on the specific residue of human serum albumin (HSA) nanoparticles (NPs). We synthesized a series of Au(III) α-N-heterocyclic thiosemicarbazone compounds and obtained a Au agent () with remarkable cytotoxicity to gastric cancer cells; moreover, we successfully constructed a novel complex NP delivery system. Importantly, the results showed that / NPs effectively inhibited gastric tumor growth and NPs enhanced the therapeutic efficiency, bioavailability, and targeting ability compared with those of alone. Furthermore, the / results revealed that / NPs could integrate chemotherapy and immunotherapy by synergistically attacking two different cellular components in TME at the same time, namely, polarizing the tumor-associated macrophages and inducing apoptosis of gastric cancer cells.

PubMed: 34000198
DOI: 10.1021/acs.jmedchem.1c00050

Experimental method

X-RAY DIFFRACTION (2.5 Å)