Human carbonic anhydrase IX is a membrane enzyme that is significantly expressed in some types of cancer cells, while copper radioisotopes offer wide range of diagnostic, therapeutic and theranostic properties. The work was focused on a new approach to the labelling of antibody IgG M75 for epitope human carbonic anhydrase IX with copper radioisotopes Cu and Cu and its in vivo testing in mice with inoculated colorectal cancer. Monoclonal antibody IgG M75 for epitope human carbonic anhydrase IX was successfully conjugated with copper-specific chelator "phosphinate" and labelled with Cu and Cu The obtained molecule has considerable potential as a radioimmuno pharmaceutical suitable for imaging of tumours expressing carbonic anhydrase IX by positron emission tomography (PET).

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.apradiso.2018.10.021DOI Listing

Publication Analysis

Top Keywords

carbonic anhydrase
20
human carbonic
16
antibody igg
12
igg m75
12
m75 epitope
12
epitope human
12
copper radioisotopes
8
carbonic
5
anhydrase
5
radiolabeling antibody
4

Similar Publications

Some novel sulphonyl thiourea derivatives (7a-m) containing 4,6-diarylpyrimidine rings were designed and synthesized using a one-pot procedure. These compounds exhibited remarkable dual inhibitory activity against human carbonic anhydrase CA I, CA II, CA IX, and XII isoenzymes and some cancer cell lines. Among them, some thioureas had significantly more potent inhibitory activities in the order of 7l > 7c > 7f (against the CA I isoform), 7f > 7b > 7c (against the CA II isoform), 7c > 7g > 7a > 7b (against the CA IX isoform), and 7d > 7c > 7g > 7f (against the CA XII isoform).

View Article and Find Full Text PDF

Background Heart failure (HF) is commonly managed by addressing water and sodium (Na) balance, with arterial circulation playing a major role in influencing renal Na and water excretion. Recently, chloride (Cl) has been recognized as an important factor in HF, associated with volume regulation and its modulation of renin-angiotensin-aldosterone system (RAAS) activity through macula densa signaling, which impacts Na retention and neurohormonal activation. Acetazolamide, a carbonic anhydrase inhibitor, can enhance decongestion in HF by increasing urinary Na and Cl excretion when added to loop diuretics, a mechanism supported by prior studies demonstrating improved urine output and decongestion.

View Article and Find Full Text PDF

Carbonic anhydrases (CAs) IX and XII are crucial for the survival and metastasis of solid tumors under hypoxic conditions. We designed compounds -, integrating triazole and benzenesulfonamide scaffolds known for inhibiting tumor-associated CAs IX/XII. Initial synthesis included compounds -, followed by diversification with small hydrophobic groups (-) and hydrophilic heterocyclic secondary amines (-).

View Article and Find Full Text PDF

Hydrogen sulfide (H2S) plays crucial inflammatory modulating roles, representing a promising candidate for anti-inflammatory therapies. However, current H2S delivery approaches lack sufficient specificity against inflammatory response. Herein, regarding the overexpressed aminopeptidase N (APN) at the inflammation sites, an APN-activated self-immolative carbonyl sulfide (COS)/H2S donor (AlaCOS) was developed for inflammatory response-specific H2S delivery.

View Article and Find Full Text PDF

Serendipitous high-resolution structure of Escherichia coli carbonic anhydrase 2.

Acta Crystallogr F Struct Biol Commun

February 2025

Department of Biological Chemistry, University of Michigan, Ann Arbor, MI 48109, USA.

X-ray crystallography remains the dominant method of determining the three-dimensional structure of proteins. Nevertheless, this resource-intensive process may be hindered by the unintended crystallization of contaminant proteins from the expression source. Here, the serendipitous discovery of two novel crystal forms and one new, high-resolution structure of carbonic anhydrase 2 (CA2) from Escherichia coli that arose during a crystallization campaign for an unrelated target is reported.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!