Deciphering albumin-directed drug delivery by imaging

Hu, Hui-Yu; Quintana, Jeremy M.; Weissleder, Ralph; Parangi, Sareh; Miller, Miles A.

doi:10.1016/j.addr.2022.114237

Cited by 37 publications

(29 citation statements)

References 237 publications

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“…47,48,52,55,60 Attaching an albumin binding group, (p-iodophenylbutanoyl or Evans Blue) to prolong blood circulation time is a common approach that has been exploited in the drug design of diagnostics and therapeutics. 61,62 A longer tumor retention is particularly desirable for targeted radiotherapy, through which delivering of a higher internal radiation dose to the tumor is maximized. Compared to [ 177 Lu]Lu-4, [ 177 Lu]Lu-7 contains a pegylated p-iodophenylbutanoyl group, and as expected, showed extended blood circulation time and increased tumor uptake and retention in the mice tumor model (Figure 7).…”

Section: ■ Results and Discussionmentioning

confidence: 99%

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

Zha¹,

Choi²,

et al. 2022

J. Med. Chem.

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Prostate-specific membrane antigen (PSMA) is a promising target for the diagnosis and radionuclide therapy of prostate cancer. This study reports conversion of a previously reported 68Ga-imaging agent, [68Ga]Ga-P16-093, to a Lu-177 radionuclide therapeutic agent. Substitution of the HBED-CC metal chelating group with DOTA(GA)2 led to P17-087 (4) and P17-088 (7). Both agents showed excellent PSMA binding affinity (IC50 = 10–30 nM) comparable to that of recently FDA-approved [177Lu]Lu-PSMA-617 (Pluvicto). Biodistribution studies in PSMA expressing tumor bearing mice showed that [177Lu]Lu-4 exhibited very high tumor uptake and a fast blood clearance similar to those of [177Lu]Lu-PSMA-617. Conversely, [177Lu]Lu-7, containing an albumin binder, extended its blood half-life and exhibited significantly higher uptake and longer tumor residence time than [177Lu]Lu-4 and [177Lu]Lu-PSMA-617. The switch from chelator HBED-CC to DOTA(GA)2 and the switch from the imaging isotope gallium-68 to the therapeutic isotope lutetium-177 have successfully transformed a PSMA-targeting agent from diagnosis to promising radionuclide therapeutic agents.

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Section: ■ Results and Discussionmentioning

confidence: 99%

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

Zha¹,

Choi²,

et al. 2022

J. Med. Chem.

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“…The developed tracers (i.e., [ 111 In]In-DTPA-B9-ABD low and [ 111 In]In-DTPAB9-ABD high ) had increased tumor uptake compared to [ 111 In]In-DTPA-B9, but the increase in tumor retention was partially CAIX-independent (DOI: ). Albumin hitchhiking is an effective strategy to prolong the circulation of small molecules and proteins and enhance tumor retention, , but the net value needs to be carefully addressed in developing radiopharmaceuticals.…”

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confidence: 66%

“…On the basis of the previous success in inventing nanobody-derived tracer [ 68 Ga]Ga-NOTA-Nb1053, 8 ). Albumin hitchhiking is an effective strategy to prolong the circulation of small molecules and proteins and enhance tumor retention, 10,11 but the net value needs to be carefully addressed in developing radiopharmaceuticals.…”

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confidence: 99%

Antibody-Based Imaging and Therapy for Precision Medicine

et al. 2022

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“…HSA serves as the depot and carrier protein by reversible interaction of exogenous and endogenous compounds. The transportation of various drugs, metabolites, and fatty acids is carried out by HSA present in blood plasma. − Any change in the levels of HSA in body fluids is a direct warning for physiological malfunctioning of visceral organs, especially the liver and kidneys . The level of HSA in blood plasma is usually used to screen liver and kidney function and diseases such as coronary heart diseases, multiple myeloma, diabetes mellitus, , kidney diseases, − neurometabolic disorders, , and liver cirrhosis. − The abnormalities in liver such as cirrhosis or hepatitis can cause hypoproteinemiaa condition with a reduced level of HSA in plasma.…”

Section: Introductionmentioning

confidence: 99%

Differentiation of HSA and BSA and Instantaneous Detection of HSO₃^– Using Confined Space of Serum Albumins and Live Cell Imaging of Exogenous/Endogenous HSO₃^–

et al. 2023

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The limitations of prevailing probes for the detection of human serum albumin (HSA) and HSO3 – make it challenging to apprehend the cooperative effect of both HSA and HSO3 – in biological systems. Herein, we present a multi-responsive fluorescent probe MGTP, which distinguishes HSA from bovine serum albumin (BSA) through an ∼104-fold fluorescence enhancement at an emission maximum of 595 nm with HSA and only an ∼10-fold increase at an emission maximum of 615 nm with a shoulder at 680 nm with BSA. The absorbance spectrum of MGTP also discriminates HSA and BSA with the respective absorption maxima at 543 nm and at 580 nm. MGTP in the confined space of HSA or BSA undergoes instantaneous conjugate addition of HSO3 – and results in a ratiometric change in fluorescence intensity with diminishing of red fluorescence (600 nm) and emergence of green fluorescence (515 nm). MGTP in the absence of SAs does not react with HSO3 – in phosphate-buffered saline buffer and reacts sluggishly in the dimethyl sulfoxide–water 1:1 mixture. The limit of detection values for the detection of HSA and HSO3 – are 4 and 6.88 nM, respectively. The drug binding studies reveal that MGTP preferably confines itself at the bilirubin site of HSA. In MCF-7 cancer cells, MGTP is localized into mitochondria and reveals both exogenous and endogenous visualization of HSO3 – through a change in fluorescence from the red to green channel.

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Deciphering albumin-directed drug delivery by imaging

Cited by 37 publications

References 237 publications

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

Antibody-Based Imaging and Therapy for Precision Medicine

Differentiation of HSA and BSA and Instantaneous Detection of HSO₃^– Using Confined Space of Serum Albumins and Live Cell Imaging of Exogenous/Endogenous HSO₃^–

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Deciphering albumin-directed drug delivery by imaging

Cited by 37 publications

References 237 publications

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

Antibody-Based Imaging and Therapy for Precision Medicine

Differentiation of HSA and BSA and Instantaneous Detection of HSO3– Using Confined Space of Serum Albumins and Live Cell Imaging of Exogenous/Endogenous HSO3–

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Product

Resources

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Differentiation of HSA and BSA and Instantaneous Detection of HSO₃^– Using Confined Space of Serum Albumins and Live Cell Imaging of Exogenous/Endogenous HSO₃^–