Selective CXCR4 binding peptide conjugate and methods for making and using the same
申请人:Mainline Biosciences LLC
公开号:US11123437B2
公开(公告)日:2021-09-21
The present invention provides a selective CXCR4 binding peptide conjugate (“PC”), and a method for using and producing the same. In particular, the selective CXCR4 binding peptide conjugate of the invention comprises a peptide portion that selectively binds to CXCR4 and a medically useful compound, such as an imaging agent, a diagnostic agent, or a therapeutically or pharmaceutically active compound. In one particular embodiment, the selective CXCR4 binding peptide conjugate (“PC”) is of the formula:
or a pharmaceutically acceptable salt thereof, wherein a, b, AA1, AA2, Ar1, X1, and AA3 are those defined herein. The peptide conjugate of the invention can be used in a variety of medical applications including, but not limited to, a targeted drug delivery or imaging a patient or diagnosing a patient for a disease or a clinical condition associated with overexpression and/or upregulation of CXCR4, such as cancers, HIV infection, and immune disorders. Compositions, kits and methods are also disclosed herein for such uses.
本发明提供了一种选择性 CXCR4 结合肽共轭物("PC"),以及使用和生产 PC 的方法。特别是,本发明的选择性 CXCR4 结合肽共轭物包括选择性结合 CXCR4 的肽部分和医学上有用的化合物,如成像剂、诊断剂或治疗或制药活性化合物。在一个特定的实施方案中,选择性 CXCR4 结合肽共轭物("PC")的结构式如下:
或其药学上可接受的盐,其中 a、b、AA1、AA2、Ar1、X1 和 AA3 为本文所定义者。本发明的多肽共轭物可用于多种医疗应用,包括但不限于靶向给药或为患者成像或诊断与 CXCR4 过表达和/或上调相关的疾病或临床症状,如癌症、HIV 感染和免疫紊乱。本文还公开了用于此类用途的组合物、试剂盒和方法。