Analogs for CLR/RAMP receptor ligands are provided that have agonist, superagonist, antagonist, super-antagonist, or multiple receptor modulating activity. The analogs can be selective for one or more CLR/RAMP receptors, or can be pan-specific for multiple G protein-coupled receptors.

The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer and increasing cellular internalization of said peptide compounds. The peptide compounds are selected from the following group consisting of; GVRAKAGVRNMFKSESY as set forth in SEQ ID NO: 9; GVRAKAGVRN(Nle)FKSESY as set forth in SEQ ID NO: 10; and YKSLRRKAPRWDAPLRDPALRQLL as set forth in SEQ ID NO: 11; and wherein at least one protecting group and/or at least one labelling agent is connected to said peptide compound.

The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer and increasing cellular internalization of said peptide compounds. The peptide compounds are selected from the following group consisting of; GVRAKAGVRNMFKSESY as set forth in SEQ ID NO: 9; GVRAKAGVRN(Nle)FKSESY as set forth in SEQ ID NO: 10; and YKSLRRKAPRWDAPLRDPALRQLL as set forth in SEQ ID NO: 11; and wherein at least one protecting group and/or at least one labelling agent is connected to said peptide compound.

Analogs for CLR/RAMP receptor ligands are provided that have agonist, superagonist, antagonist, super-antagonist, or multiple receptor modulatng activity. The analogs can be selective for one or more CLR/RAMP receptors, or can be pan-specific for multiple G protein-coupled receptors.

Targeted pharmaceuticals, particularly targeted radiopharmaceuticals, are provided which possess extended tumor retention time.

The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating inflammation. For example, the compounds can comprise compounds; IKLSGGVQAKAGVINMDKSESM, formula (V) as set forth in SEQ ID NO: 5, GVRAKAGVRN(Nle)FKSESY, formula (X) as set forth in SEQ ID NO: 10 and YKSLRRK.APRWDAPLRDPALRQLL, formula (XI) as set forth in SEQ ID NO: 11 wherein at least one protecting group and/or at least one labelling agent is connected to said peptide compound at an N- and/or C-terminal end, for use in inhibiting or decreasing TNF-alpha-induced COX-2 expression in cells expression sortilin.

A thio-selective radioactive labeling agent has the following general formula:
*R-L-VS, wherein said *R is a radioisotope, L is a linking group, and VS is a vinylsulfone functional group.

The present application relates to methods and uses of conjugates comprising antitumor agents (e.g., chemotherapeutic agents) conjugated to peptide compounds targeting Sortilin-expressing cancer stem cells (CSCs), in embodiments for the treatment of poor prognosis cancers refractory to standard antitumor therapies associated the presence of Sortilin-expressing CSCs, and for preventing or treating cancer relapse or recurrence.

The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer. For example, the compounds can comprise compounds of formula

TABLE-US-00001 (SEQIDNO:1) X.sub.1X.sub.2X.sub.3X.sub.4X.sub.5GVX.sub.6AKAGVX.sub.7NX.sub.8FKSESY (I) (SEQIDNO:2) (X.sub.9).sub.nGVX.sub.10AKAGVX.sub.11NX.sub.12FKSESY (II) (SEQIDNO:3) YKX.sub.13LRRX.sub.14APRWDX.sub.15PLRDPALRX.sub.16X.sub.17L (III) (SEQIDNO:4) YKX.sub.18LRR(X.sub.19).sub.nPLRDPALRX.sub.20X.sub.21L (IV) (SEQIDNO:5) IKLSGGVQAKAGVINMDKSESM (V) (SEQIDNO:6) IKLSGGVQAKAGVINMFKSESY (VI) (SEQIDNO:7) IKLSGGVQAKAGVINMFKSESYK (VII) (SEQIDNO:8) GVQAKAGVINMFKSESY (VIII) (SEQIDNO:9) GVRAKAGVRNMFKSESY (IX) (SEQIDNO:10) GVRAKAGVRN(Nle)FKSESY (X) (SEQIDNO:11) YKSLRRKAPRWDAPLRDPALRQLL (XI) (SEQIDNO:12) YKSLRRKAPRWDAYLRDPALRQLL (XII) (SEQIDNO:13) YKSLRRKAPRWDAYLRDPALRPLL (XIII) wherein X.sub.1 to X.sub.21 and n can have various different values and wherein at least one protecting group and/or at least one labelling agent is optionally connected to said peptide compound at an N- and/or C-terminal end.

Analogs for CLR/RAMP receptor ligands are provided that have agonist, superagonist, antagonist, super-antagonist, or multiple receptor modulatng activity. The analogs can be selective for one or more CLR/RAMP receptors, or can be pan-specific for multiple G protein-coupled receptors.