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Title:
POLYPEPTIDE TARGETING INTEGRIN α6 AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/267097
Kind Code:
A1
Abstract:
A polypeptide targeting integrin α6 and the use thereof. The polypeptide has a sequence motif of RWYD, and is stronger in affinity, wherein the equilibrium dissociation constant KD reaches the level of nM, and the affinity is greatly improved. The polypeptide has a strong affinity to integrin α6, a strong specificity and no biological toxicity, is relatively stable in vivo and reasonable in distribution, and can be used as a targeting carrier. In addition, the polypeptide targeting integrin α6 can be used as a molecular probe in the molecular imaging of various tumors with highly-expressed integrin α6. Further provided is a dimer of the polypeptide, which has a more significant targeting effect and no biological toxicity. The polypeptide targeting integrin α6 can be used in the molecular imaging of various tumors with highly-expressed integrin α6, and has an important application value in the molecular imaging of tumors.

Inventors:
ZENG MUSHENG (CN)
FENG GUOKAI (CN)
YE JIACONG (CN)
Application Number:
PCT/CN2021/104639
Publication Date:
December 29, 2022
Filing Date:
July 06, 2021
Export Citation:
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Assignee:
UNIV SUN YAT SEN (CN)
SUN YAT SEN UNIV CANCER CENTER SYSUCC (CN)
International Classes:
A61K47/62; C07K5/11; A61K49/00; A61K49/14; A61K51/08; A61P35/00; C07K19/00
Foreign References:
CN107987127A2018-05-04
CN104250287A2014-12-31
CN110420337A2019-11-08
US20180141974A12018-05-24
Other References:
LUO QI, YANG GUANGJIE, GAO HANNAN, WANG YANPU, LUO CHUANGWEI, MA XIAOTU, GAO YU, LI XIAODA, ZHAO HUIYUN, JIA BING, SHI JIYUN, WANG: "An Integrin Alpha 6-Targeted Radiotracer with Improved Receptor Binding Affinity and Tumor Uptake", BIOCONJUGATE CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 31, no. 5, 20 May 2020 (2020-05-20), US , pages 1510 - 1521, XP093017253, ISSN: 1043-1802, DOI: 10.1021/acs.bioconjchem.0c00170
MEI YAN, LI YING‐HE, YANG XIAO‐CHUN, ZHOU CHAO, LI ZHI‐JIAN, ZHENG XIAO‐BIN, YE JIA‐CONG, LI CHENG, ZHANG XUAN‐HONG, YUAN JIAN‐MIN: "An optimized integrin α6‐targeted peptide for positron emission tomography/magnetic resonance imaging of pancreatic cancer and its precancerous lesion", CLINICAL AND TRANSLATIONAL MEDICINE, INTERNATIONAL SOCIETY FOR TRANSLATIONAL MEDICINE, SE, vol. 10, no. 4, 1 August 2020 (2020-08-01), SE , XP093017254, ISSN: 2001-1326, DOI: 10.1002/ctm2.157
Attorney, Agent or Firm:
JIAQUAN IP LAW (CN)
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