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Development of a complementary PET/MR dual-modal imaging probe for targeting prostate-specific membrane antigen (PSMA)2017-01-11
Literature Nanomedicine, IF 4.889
Background & Purpose Prostate cancer is one of the most common types of cancer in the world. The prostate specific membrane antigen (PSMA) is a famous biomarker of prostate cancer, and the glutamate-urea-lysine (GUL) conjugate is a proven PSMA targeting moiety. Iron oxide (IO) nanoparticle is for MRI imaging and 68Ga-DOTA is for PET positron emission. 68Ga-DOTA, GUL, PEG are all encapsulated in 68Ga-DOTA-IO-GUL imaging probe, of which selective uptake by PSMA+ tumor is demonstrated. Specific binding of DOTA-IO-GUL to PSMA-positive cells was confirmed by an in vitro competitive binding study using PSMA-targeting agent MIP-1072.
Fig.1 In vivo micro MRI image results. (A) Before injection, control image; (B) after injection of DOTA-IO-GUL (0.1 mL, 0.2 mM) through the tail vein (1 h). Left tumor is PSMA positive (22Rv1) and right tumor is PSMA-negative (PC-3). Red circle demonstrates the selective uptake of DOTA-IO-GUL to the positive tumor (49.1 Fe ng/g).
Fig. 2 In vivo PET result. (A) PSMA-selective uptake result in micro PET imaging. (SUVmean = 0.668) 68Ga-DOTA-IO-GUL (10.2 MBq, 0.1 mL) tail vein injection after 1 h imaging. Left tumor is PSMA-positive (22Rv1) and right tumor is PSMA-negative (PC-3). (B) Blocking study result with co-injection of MIP-1072 (50 mg/kg).
Peptide therapeutics: current status and future directions2017-01-03
Literature：Drug Discovery Today, IF 5.625
Keywords：peptide therapeutics, SWOT, rational design, GLP-1, CPP
Background：Peptides are recognized for being highly selective and efficacious and, at the same time, relatively safe and well tolerated. Given that the low-hanging fruits in the form of obvious peptide targets have already been picked, it has now become necessary to explore new routes beyond traditional peptide design. Examples of such approaches are multifunctional and cell penetrating peptides, as well as peptide drug conjugates. Here, we discuss SWOT analysis of peptides as medicines, and emerging new opportunities in peptide drug design and development.
Figure 1 Analysis of SWOT of naturally occurring peptides in their use as therapeutics
Conclusions Currently：There are about 60 peptide drugs are proven by FDA, over 140 peptides are during clinical research and around 500 peptides are investigated pre-clinically. Peptide drugs have promising prospects due to their potent and specific, yet safe, mode of action.
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