Inhibitors of prostate-specific membrane antigen in the diagnosis and therapy of metastatic prostate cancer - a review of patent literature
- Authors
- Ha, Hyunsoo; Kwon, Hongmok; Lim, Taehyeong; Jang, Jaebong; Park, Song-Kyu; Byun, Youngjoo
- Issue Date
- 3-6월-2021
- Publisher
- TAYLOR & FRANCIS LTD
- Keywords
- Prostate-specific membrane antigen (PSMA); metastatic prostate cancer; imaging probes; radionuclides; Lys-urea-Glu
- Citation
- EXPERT OPINION ON THERAPEUTIC PATENTS, v.31, no.6, pp.525 - 547
- Indexed
- SCIE
SCOPUS
- Journal Title
- EXPERT OPINION ON THERAPEUTIC PATENTS
- Volume
- 31
- Number
- 6
- Start Page
- 525
- End Page
- 547
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/127867
- DOI
- 10.1080/13543776.2021.1878145
- ISSN
- 1354-3776
- Abstract
- Introduction Prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II, is a potential target protein for imaging and treatment of patients with prostate cancer because of its overexpression during metastasis. Various PSMA-targeted imaging and therapeutic probes have been designed and synthesized based on the Lys-urea-Glu motif. Structural modifications have been made exclusively in the linker region, while maintaining the Lys-urea-Glu structure that interacts with S1 and S1MODIFIER LETTER PRIME pockets. Area Covered This review includes WIPO-listed patents (from January 2017 to June 2020) reporting PSMA-targeted probes based on the Lys-urea-Glu or Glu-urea-Glu structure. Expert opinion : PSMA-targeted imaging agents labeled with radionuclides such as fluorine-18, copper-64, gallium-68, and technetium-99m have been successfully translated into clinical phase for the early diagnosis of metastatic prostate cancer. Recently, PSMA-targeted therapeutic agents labeled with iodine-131, lutetium-177, astatine-211, and lead-212 have also been developed with notable progress. Most PSMA-targeted agents are based on the Lys-urea-Glu or Glu-urea-Glu structure, demonstrate strong PSMA-binding affinity in nanomolar range, and achieve diverse structural modifications in the non-pharmacophore pocket. By exploiting the S1 accessory pocket or the tunnel region of the PSMA active site, the in vivo efficacy and pharmacokinetic profiles of the PMSA-targeted agents can be effectively modulated.
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Collections - College of Pharmacy > Department of Pharmaceutical Science > 1. Journal Articles
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