JP-2025516319-A5 -

Dates

Publication Date

20260511

Application Date

20230503

Description

According to a first aspect of the present invention, C[HyP][HyP]DAYLGC[tBuGly]SYCEPW (Sequence ID 1, referred to herein as BCY23180); C[Cis-HyP][HyP]DAYLGC[tBuGly]SYCEPW (Sequence ID 3, referred to herein as BCY23182); CP[Cis-HyP]DAYLGC[tBuGly]SYCEPW (Sequence ID 5, referred to herein as BCY23184); CP[HyP]DA[DOPA]LGC[tBuGly]SYCEPW (Sequence ID 6, referred to herein as BCY23185); CP[HyP]DA[pCaPhe]LGC[tBuGly]SYCEPW (Sequence ID 7, referred to herein as BCY23186); CP[HyP]DA[pCoPhe]LGC[tBuGly]SYCEPW (Sequence ID 8, referred to herein as BCY23187); CP[HyP]DA[hTyr]LGC[tBuGly]SYCEPW (Sequence ID 9, referred to herein as BCY23188); CP[HyP]DAYLGC[tBuGly]S[DOPA]CEPW (Sequence ID 21, referred to herein as BCY23200); CP[HyP]DAYLGC[tBuGly]S[pCaPhe]CEPW (Sequence ID 22, referred to herein as BCY23201); CP[HyP]DAYLGC[tBuGly]S[pCoPhe]CEPW (Sequence ID 23, referred to herein as BCY23202); CP[HyP]DAYLGC[tBuGly]S[hTyr]CEPW (Sequence ID 24, referred to herein as BCY23203); CP[HyP]DAYLGC[tBuGly]SYCE[HyP]W (Sequence ID 25, referred to herein as BCY23204); CP[HyP]DAYLGC[tBuGly]SYCE[Oxa]W (Sequence ID 26, referred to herein as BCY23205); CP[HyP]DAYLGC[tBuGly]SYCE[Cis-HyP]W (Sequence ID 27, referred to herein as BCY23206); CP[HyP]DAYLGC[tBuGly]SYCEPY (Sequence ID 28, referred to herein as BCY23207); CP[HyP]DAYLGC[tBuGly]SYCEP[DOPA] (Sequence ID 29, referred to herein as BCY23208); CP[HyP]DAYLGC[tBuGly]SYCEP[pCaPhe] (Sequence ID 30, referred to herein as BCY23209); CP[HyP]DAYLGC[tBuGly]SYCEP[pCoPhe] (Sequence ID 31, referred to herein as BCY23210); CP[HyP]DAYLGC[tBuGly]SYCEP[hTyr] (Sequence ID 32, referred to herein as BCY23211); CP[HyP]EAYLGC[tBuGly]SYCEPW (Sequence ID 33, referred to herein as BCY23216); CP[HyP][Gla]AYLGC[tBuGly]SYCEPW (Sequence ID 34, referred to herein as BCY23217); CP[HyP]DAY S GC[tBuGly]SYCEPW (Sequence ID 35, referred to herein as BCY23218); CP[HyP]DAYTGC[tBuGly]SYCEPW (Sequence ID 36, referred to herein as BCY23219); CP[HyP]DAYDGC[tBuGly]SYCEPW (Sequence ID 37, referred to herein as BCY23220); CP[HyP]DAYEGC[tBuGly]SYCEPW (Sequence ID 38, referred to herein as BCY23221); CP[HyP]DAYNGC[tBuGly]SYCEPW (Sequence ID 39, referred to herein as BCY23222); CP[HyP]DAYQGC[tBuGly]SYCEPW (Sequence ID 40, referred to herein as BCY23223); CP[HyP]DAYLGC[tBuGly][HSer]YCEPW (Sequence ID 41, referred to herein as BCY23224); CP[HyP]DAYLGC[tBuGly]SYCDPW (Sequence ID 47, referred to herein as BCY23230); CP[HyP]DAYLGC[tBuGly]SYC[Gla]PW (Sequence ID 48, referred to herein as BCY23231); and CP[HyP]DAYLGC[3HyV]SYCEPW (Sequence ID 50, referred to herein as BCY23515), [Here, Cis-HyP represents cis-L-4-hydroxyproline, DOPA represents 3,4-dihydroxyphenylalanine, Gla represents L-γ-carboxyglutamic acid, HyP represents hydroxyproline, HSer represents homoserine, hTyr represents homotyrosine, 3HyV represents 3-hydroxy-L-valine, Oxa represents oxazolidine-4-carboxylic acid, pCaPhe represents L-4-carbamoylphenylalanine, pCoPhe represents 4-carboxy-L-phenylalanine, and tBuGly represents t-butylglycine.] A peptide ligand specific to transferrin receptor 1 (TfR1) is provided, comprising an amino acid sequence selected from the above. Detailed description of the invention Peptide ligands According to a first aspect of the present invention, C[HyP][HyP]DAYLGC[tBuGly]SYCEPW (Sequence ID 1, referred to herein as BCY23180); C[Cis-HyP][HyP]DAYLGC[tBuGly]SYCEPW (Sequence ID 3, referred to herein as BCY23182); CP[Cis-HyP]DAYLGC[tBuGly]SYCEPW (Sequence ID 5, referred to herein as BCY23184); CP[HyP]DA[DOPA]LGC[tBuGly]SYCEPW (Sequence ID 6, referred to herein as BCY23185); CP[HyP]DA[pCaPhe]LGC[tBuGly]SYCEPW (Sequence ID 7, referred to herein as BCY23186); CP[HyP]DA[pCoPhe]LGC[tBuGly]SYCEPW (Sequence ID 8, referred to herein as BCY23187); CP[HyP]DA[hTyr]LGC[tBuGly]SYCEPW (Sequence ID 9, referred to herein as BCY23188); CP[HyP]DAYLGC[tBuGly]S[DOPA]CEPW (Sequence ID 21, referred to herein as BCY23200); CP[HyP]DAYLGC[tBuGly]S[pCaPhe]CEPW (Sequence ID 22, referred to herein as BCY23201); CP[HyP]DAYLGC[tBuGly]S[pCoPhe]CEPW (Sequence ID 23, referred to herein as BCY23202); CP[HyP]DAYLGC[tBuGly]S[hTyr]CEPW (Sequence ID 24, referred to herein as BCY23203); CP[HyP]DAYLGC[tBuGly]SYCE[HyP]W (Sequence ID 25, referred to herein as BCY23204); CP[HyP]DAYLGC[tBuGly]SYCE[Oxa]W (Sequence ID 26, referred to herein as BCY23205); CP[HyP]DAYLGC[tBuGly]SYCE[Cis-HyP]W (Sequence ID 27, referred to herein as BCY23206); CP[HyP]DAYLGC[tBuGly]SYCEPY (Sequence ID 28, referred to herein as BCY23207); CP[HyP]DAYLGC[tBuGly]SYCEP[DOPA] (Sequence ID 29, referred to herein as BCY23208); CP[HyP]DAYLGC[tBuGly]SYCEP[pCaPhe] (Sequence ID 30, referred to herein as BCY23209); CP[HyP]DAYLGC[tBuGly]SYCEP[pCoPhe] (Sequence ID 31, referred to herein as BCY23210); CP[HyP]DAYLGC[tBuGly]SYCEP[hTyr] (Sequence ID 32, referred to herein as BCY23211); CP[HyP]EAYLGC[tBuGly]SYCEPW (Sequence ID 33, referred to herein as BCY23216); CP[HyP][Gla]AYLGC[tBuGly]SYCEPW (Sequence ID 34, referred to herein as BCY23217);