dota peptide DOTATATE is a DOTA-conjugated peptide - DOTAligand conjugate a peptide to the DOTA chelator Unveiling the Power of DOTA Peptide: A Revolution in Medical Imaging and Treatment

Dotachelator full Name The field of medical diagnostics and therapeutics has been significantly advanced by the development of sophisticated molecular tools. Among these, DOTA peptide conjugates stand out for their remarkable versatility and efficacy, particularly in medical applications as contrast agents and in targeted cancer treatmentslabeled, DOTA-conjugated tetrapeptides having high affinity .... DOTA, an acronym for 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid, is a powerful chelating agent known for its ability to form highly stable complexes with various metal ions.A radiolabeled divalent histamine-succinyl-glycine (HSG) hapten-peptidelinked with the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10- ... When this DOTA ligand is conjugated to a peptide, it creates a powerful platform for delivering radionuclides or imaging agents precisely to specific biological targets.

The synthesis of DOTA-peptide conjugates is a complex but well-established process. Researchers have developed various methods, including solution-phase and solid-phase synthesis techniques, to efficiently attach DOTA to peptides.TFA is commonly used as a chemical reagent to remove residual protecting groups during purification ofpeptidesand also as a mobile-phase modifier in a ... For instance, the synthesis and chelation chemistry of DOTA-peptide conjugates have been extensively studied, focusing on creating bifunctional derivatives of DOTA that facilitate seamless conjugation. Techniques like copper-free click chemistry have also emerged, offering efficient bioconjugation to azide-modified peptides. The ability to conjugate a peptide to the DOTA chelator with high precision is crucial for the development of effective diagnostic and therapeutic agents.DOTAcontains four acetic acid carboxylate groups and four nitrogens in it 12-atom cyclic structure. C- or N-functionalized derivatives of this basic structure ...

One of the most prominent applications of DOTA peptide is in positron emission tomography (PET) imaging. DOTATATE is a DOTA-conjugated peptide that has gained significant traction in this area. DOTATATE acetate (GMP), for example, serves as a precursor for radiolabeled DOTA-[Tyr3]octreotate. This compound can be labeled with radionuclides, such as Gallium-68, to create DOTA-peptides for PET imaging that can be labeled with 68 Ga. This allows for highly sensitive visualization of tumors expressing somatostatin receptors, which are common in neuroendocrine tumors (NETs). Studies have shown that [68 Ga]Ga-DOTA-peptide PET/CT is a valuable tool for diagnosing and staging NETs. The ability to achieve high specific activities (e.g., 1 GBq per nmol) within a short timeframe (around 20 minutes) makes these DOTA-peptides clinically applicable.Synthesis, Radiolabeling, and Biodistribution Study of a ...

Beyond imaging, DOTA peptide plays a critical role in peptide receptor radionuclide therapy (PRRT). DOTA-TATE therapy is a form of PRRT that targets somatostatin receptors (SSR). By attaching a therapeutic radionuclide to a DOTA-conjugated peptide like DOTA-TATE, the radioactive payload is delivered directly to cancer cells expressing the target receptors, minimizing damage to healthy tissues. Lutetium-177 labeled 177Lu-DOTATATE is a prime example of this therapeutic approach for gastroenteropancreatic neuroendocrine tumors.Conjugation of DOTA-like chelating agents to peptides and ... PRRT, in general, has been demonstrated to be a well-tolerated and safe treatment with generally mild and self-limiting acute side effects.

The versatility of DOTA peptide extends to other imaging modalities and therapeutic targets.Synthesis and Assessment of Peptide Gd-DOTA ... For instance, Gd-DOTA conjugates are being explored as promising targeted small molecular macrocyclic contrast agents for Magnetic Resonance (MR) molecular imaging of prostate cancer. These conjugates are designed to specifically target EDB-FN (Endocrine-Disruptant-Binding Factor-1). Furthermore, DOTA-cyclo(RGDfK) acetate, a DOTA-conjugated peptide, is used as a precursor for radiometal-labeled DOTA-RGD, targeting integrins involved in angiogenesis. The development of final labeled DTPA- and DOTA-conjugated peptides with excellent stability, specific activity, and radiochemical purity is continuously being optimized.DOTAis an organic compound and commonly used as a complexing agent, which has been widely used as contrast agent for cancer treatments.

The structural characteristics of DOTA contribute significantly to its effectivenessSmall molecules & peptides.DOTA-cyclo(RGDfK) acetate. Precursor for radiometal-labelled DOTA-RGD. DOTA-RGD Sequence: cyclo[-Arg-Gly-Asp-D-Phe. DOTA is an octadentate ligand featuring four carboxylate and four amino groups within its 12-atom cyclic structure, enabling it to form thermodynamically stable complexesRadiolabeling of DOTA-like conjugated peptides with .... Its structure and chemical name are fundamental to its chelating capabilities. Research continues to explore the DOTA chemical properties, from its pKa values to its functionalization with various derivatives, to enhance its utility in bioconjugation and radiolabeling. The ongoing research into DOTA-TATE acetate and other DOTA-related peptides underscores the dynamic and evolving nature of this important class of molecules in advancing healthcare.作者：S Huclier-Markai·2014·被引用次数：84—TheDOTAmacrocyclic ligand forms stable complexes with many cations and has been shown to be the most suitable chelating moiety for scandium. Initially, the ...