DOTAsynthesis The intricate world of medical science is continuously seeking innovative solutions for diagnosis and treatment. At the forefront of these advancements lies the remarkable dota peptide, a powerful tool that has significantly impacted fields like medical imaging and cancer therapy. This article delves into the multifaceted applications and scientific underpinnings of dota peptide, exploring its role as a complexing agent, its integration into DOTA-peptide conjugates, and its crucial function in developing promising targeted small molecular macrocyclic contrast agents.
At its core, DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) is a macrocyclic chelator, a molecule adept at tightly binding to metal ions作者:F Ebrahimi·2024—In this study, the VEGFR1/2-targetingpeptideVGB3 was conjugated with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), using 6-aminohexanoic .... This property makes it an invaluable component in radiopharmaceuticals.作者:JR Lever·2019·被引用次数:7—Peptideswere prepared by solid-phase techniques, using orthogonal strategies to achieve branching toDOTA, and then characterized by HPLC, mass spectroscopy ... When DOTA is conjugated to a peptide, it forms DOTA-peptide conjugates. These conjugates are designed to target specific biological molecules or cells within the body. The peptide moiety acts as a guide, directing the DOTA-metal complex to a particular site, while the DOTA chelator ensures the stable and secure attachment of a radioisotope作者:WAP Breeman·2005·被引用次数:396—DOTA-peptides for PET imaging can be labelled with 68 Gaup to specific activities of 1 GBq per nmol within 20 min, enabling the clinical application of ....
This strategic combination has revolutionized diagnostic imaging, particularly Positron Emission Tomography (PET) and Single-Photon Emission Computed Tomography (SPECT). DOTA-peptides for PET imaging can be labelled with 68 Ga (Gallium-68), a positron-emitting radionuclide. The resulting Gallium ga 68 dotatate (also known as 68Ga-DOTA-peptide) allows for highly sensitive visualization of tumors expressing specific receptors, such as somatostatin receptors.作者:WAP Breeman·2005·被引用次数:396—DOTA-peptides for PET imaging can be labelled with 68 Gaup to specific activities of 1 GBq per nmol within 20 min, enabling the clinical application of ... This enables earlier and more accurate diagnosis of neuroendocrine tumors (NETs) and other malignancies. The description of DOTATATE is a DOTA-conjugated peptide highlights this specific and widely used example. Furthermore, DOTATATE acetate is a DOTA-conjugated peptide, serving as a precursor for such imaging agents.
Beyond diagnostics, dota peptide plays a pivotal role in targeted radionuclide therapyDefinition of lutetium Lu 177-DOTA-di-HSG peptide IMP-288. By conjugating DOTA to peptides that bind to cancerous cells, therapeutic radioisotopes can be delivered directly to the tumor site, minimizing damage to healthy tissuesDOTAis an organic compound and commonly used as a complexing agent, which has been widely used as contrast agent for cancer treatments.. 177Lu-DOTATATE (Lutetium-177 dotatate) is a prime example of this therapeutic approachSmall molecules & peptides - Products. This therapy, often referred to as DOTA-TATE therapy, is a form of peptide receptor radionuclide therapy (PRRT) specifically targeting somatostatin receptors.Small molecules & peptides - Products The DOTA-TATE acetate (GMP), a precursor for radiolabeled DOTA-[Tyr3]octreotate, is essential for the production of these therapeutic agents. The ability to conjugate a peptide to the DOTA chelator and then label it with a radionuclide is a cornerstone of this treatment modality.
The synthesis of these complex molecules requires sophisticated chemical techniques. Researchers employ various methods, including solid-phase synthesis, to create stable DOTA-peptide conjugates. The review on "The Synthesis and Chelation Chemistry of DOTA-Peptide" by LM De León-Rodríguez details the solution and solid-phase synthesis of these conjugates, emphasizing their coordination and chelation properties. Similarly, other studies focus on optimizing these processes, such as the "Ultrasonic-Assisted Solid-Phase Peptide Synthesis of DOTA-TATE," which aims to improve yields and reduce coupling timeslabeled, DOTA-conjugated tetrapeptides having high affinity .... The development of efficient methods for producing final labeled DTPA- and DOTA-conjugated peptides is crucial for their clinical translationPeptide receptor radionuclide therapy with [177Lu]Lu- ....
The versatility of DOTA as a chelator extends to its ability to complex with a wide array of metal ions, including therapeutic radionuclides like Lutetium-177 and diagnostic isotopes like Gallium-68作者:SM Okarvi·2019·被引用次数:16—DOTA(Fig. 1) is an octadentate ligand with four carboxylate and four amino groups, which holds the ability to form thermodynamically stable and .... This ability to form thermodynamically stable complexes is a key feature of DOTA, which possesses four carboxylate and four amino groups in its 12-atom cyclic structure. The DOTA structure is fundamental to its chelating capacity. The exploration of DOTA-TATE and its applications further underscores the significance of this chelator in targeted therapies.
The ongoing research into DOTA-peptide chemistry is continuously expanding its potentialSynthesis and Assessment of Peptide Gd-DOTA .... For instance, studies are investigating DOTA-cyclo(RGDfK) acetate, a DOTA-conjugated peptide designed to target integrin receptors, which are often overexpressed in tumorsPeptide receptor radionuclide therapy with [177Lu]Lu- .... This represents another avenue for developing promising targeted small molecular macrocyclic contrast agents for both diagnostic and therapeutic purposes. The field also encompasses the synthesis and assessment of peptide Gd-DOTA conjugates for Magnetic Resonance (MR) molecular imaging, showcasing the broad applicability of DOTA-based strategies.
In conclusion, the dota peptide stands as a testament to scientific ingenuity, bridging the gap between fundamental chemistry and life-saving medical applications. Its role as a complexing agent, its integration into sophisticated DOTA-peptide conjugates, and its critical function in enabling advanced diagnostic imaging and targeted radionuclide therapies highlight its indispensable contribution to modern medicine. The continued exploration and refinement of DOTA-based technologies promise even more groundbreaking advancements in the fight against disease.
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