posted on 2023-01-03, 21:29authored byYa-Qiong Yan, Jia-Qi Wang, Lingze Zhang, Pei-Pei Yang, Xin-Wei Ye, Cong Liu, Da-Yong Hou, Wen-Jia Lai, Jie Wang, Xiang-Zhong Zeng, Wanhai Xu, Lei Wang
The One-Bead One-Compound (OBOC) library screening is
an efficient
technique for identifying targeting peptides. However, due to the
relatively large bead size, it is challenging for the OBOC method
to be applied for in vivo screening. Herein, we report
an in vivo Localized Instillation Beads library (LIB)
screening method to discover targeting peptides with the OBOC technique.
Inspired by localized instillation, we constructed a cavity inside
of a transplanted tumor of a mouse. Then, the OBOC heptapeptide library
was injected and incubated inside the tumor cavity. After an efficient
elution process, the retained beads were gathered, from which three
MDA-MB-231 tumor-targeting heptapeptides were discovered. It was verified
that the best peptide had 1.9-fold higher tumor accumulation than
the commonly used targeting peptide RGD in vivo.
Finally, two targeting proteins were discovered as potential targets
of our targeting peptide to the MDA-MB-231 tumor. The in vivo LIB screening method expands the scope of OBOC peptide screening
applications to discover targeting peptides in vivo feasibly and reliably.