Themed collection Medicinal Inorganic Chemistry

Guest editors introduce this web collection celebrating current achievements and future perspectives in medicinal inorganic chemistry, including: metal-based diagnostics and therapeutics, mechanistic studies of metallotherapeutics, the role of metal ions and metal ion homeostasis in disease, chelation therapy, metalloprotein inhibitors, and metal ion sensing.

Exploration of medicinal chemistry of the elements of the periodic table, and especially metals, offers the promise of new drugs and diagnostic agents with novel targets and new mechanisms of action.

This feature article highlights the field of metallic radionuclides in nuclear oncology for diagnosis with PET or SPECT and treatment with α, β⁻, or Auger electron therapy.

Recent results on a variety of transition metal complexes targeted to DNA are reviewed in order to illustrate many of the issues involved in new therapeutic design.

The N-terminus of hCTR1 was demonstrated to bind three Cu⁺ ions tightly (log K = 14.92) and reversibly via its Met-rich motifs.

The platinum-assisted cleavage of the C-terminal HIV NCp7 zinc finger is a novel strategy to inactivate this important biological target.

Simultaneous multi-element imaging using NanoSIMS provides information on the subcellular localisation of both metal and ligands inside tumour cells treated with ¹⁵N-labelled Pt drugs.

The reaction of S-bound {Fe(NO)₂}⁹ dinitrosyl iron complexes with dioxygen results in the formation of Roussin's red esters and thiolate oxidation.

Copper coordination to soluble oligomers of the English (AβH(6)R) mutant of the amyloid-β peptide is probed.

The biological investigation of novel titanium(IV) complexes shows very interesting properties concerning their binding to biomolecules, cellular accumulation and intracellular distribution depending on the ligand system.

[Pt(Dip)₂](PF₆)₂, prepared by the microwave irradiation method, achieves a selective stabilization towards parallel c-myc GQ via aromatic anchors on phenathroline ligands.

Zinc alters the aggregation pathway of human islet amyloid polypeptide (hIAPP), an amyloidogenic peptide linked to type II diabetes, to favor nonfibrillar oligomers over amyloid fibers.

Organometallic lapachol complexes, in particular a Ru derivative, induce apoptosis in human tumour cell lines by a mode of action involving oxidative stress.

Tropolone emerged from the screening of a chelator fragment library (CFL) as an inhibitor of the Zn²⁺-dependent virulence factor, Pseudomonas aeruginosa elastase (LasB).

Rhodamine-embedded maghemite nanoparticles provide a novel strategy for tracing and transporting platinum anticancer drugs in vitro and in vivo.

Conversion of 1 to 2 results in enhanced antioxidant and radical scavenging capacity thus encouraging applications for neurological disorders such as Alzheimer's disease.

A rapid and sensitive LC-MS approach for the quantification of non-radioactive metal contaminants present in metal radionuclide formulations was developed.

The cytotoxicity of a copper complex increases in response to UV light, which triggers cleavage of the complex and causes extensive cytoplasmic vacuolization that is indicative of nonapoptotic cell death.

A multifunctional breast cancer targeted conjugate was synthesized that combines features of an anti-estrogen and a DNA-directed platinating–intercalating hybrid agent.

Metal complexed derivatives of antimicrobial peptides demonstrate enhanced antimicrobial activity against a variety of pathogenic bacteria and mediate irreversible cleavage of nucleic acids, suggesting a likely mechanism of action.

A cyclometallated Pt complex able to interact specifically with the amyloid-β peptide, via the Glu11 and His13 side-chains, can preclude Zn induced aggregation of Aβ.