Amino acid sequences of SRIF-based radiochemicals
Amino acids: first letter capitalized: L-amino acid; first letter in lowercase: D-amino acid.
| Ligand | Chelator/Prosthetic Group | AA1 | AA2 | AA3 | AA4 | AA5 | AA6 | AA7 | AA8 | AA9 | AA10 |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Peptide Agonists with Predominantly SST2 Affinity | |||||||||||
| Octreotide | — | phe | Cys | Phe | trp | Lys | Thr | Cys | Thr-ol | ||
| Tyr3-octreotide (TOC) | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr-ol | |||
| RC160 (Vapreotide) | phe | Cys | Tyr | trp | Lys | Val | Cys | Trp-NH2 | |||
| Lanreotide (BIM-23014) | 2-nal | Cys | Tyr | trp | Lys | Val | Cys | Thr-NH2 | |||
| Radiopeptide Agonists and Precursors with Predominantly SST2 Affinity | |||||||||||
| DTPA-octreotide | DTPA | phe | Cys | Phe | trp | Lys | Thr | Cys | Thr-ol | ||
| DOTA-lanreotide | DOTA | 2-nal | Cys | Tyr | trp | Lys | Val | Cys | Thr-NH2 | ||
| In-DTPA-OC | In-DTPA | phe | Cys | Phe | trp | Lys | Thr | Cys | Thr-ol | ||
| DOTA-TOC | DOTA | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr-ol | ||
| Y-DOTA-TOC | Y-DOTA | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr-ol | ||
| DOTA-OC | DOTA | phe | Cys | Phe | trp | Lys | Thr | Cys | Thr-ol | ||
| Y-DOTA-OC | Y-DOTA | phe | Cys | Phe | trp | Lys | Thr | Cys | Thr-ol | ||
| Ga-DOTA-TOC | Ga-DOTA | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr-ol | ||
| Ga-DOTA-OC | Ga-DOTA | phe | Cys | Phe | trp | Lys | Thr | Cys | Thr-ol | ||
| DTPA-TATE | DTPA | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr | ||
| In-DTPA-TATE | In-DTPA | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr | ||
| DOTA-TATE | DOTA | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr | ||
| Y-DOTA-TATE | Y-DOTA | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr | ||
| In-DOTA-TOC | In-DOTA | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr-ol | ||
| Ga-DOTA-TATE | Ga-DOTA | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr | ||
| Lu-DOTATATE | Lu-DOTA | phe | Cys | Tyr | trp | Lys | Thr | Cys | Thr | ||
| I-Gluc-TOC | Glucosyl | phe | Cys | 3-I-Tyr | trp | Lys | Thr | Cys | Thr-ol | ||
| I-Gluc-TATE | Glucosyl | phe | Cys | 3-I-Tyr | trp | Lys | Thr | Cys | Thr | ||
| I-Gluc-S-TATE | Glucosyl-S- | phe | Cys | 3-I-Tyr | trp | Lys | Thr | Cys | Thr | ||
| I-Gal-S-TATE | Galactosyl-S- | phe | Cys | 3-I-Tyr | trp | Lys | Thr | Cys | Thr | ||
| Gluc-Lys(FP)-TATE | Glucosyl-Lys(fluoropropionyl) | phe | Cys | 3-I-Tyr | trp | Lys | Thr | Cys | Thr | ||
| Agonists toward Pansomatostatin-Like Binding Profile | |||||||||||
| Ga-DOTA-NOC | Ga-DOTA | phe | Cys | 1-Nal | trp | Lys | Thr | Cys | Thr-ol | ||
| In-DOTA-NOC | In-DOTA | phe | Cys | 1-Nal | trp | Lys | Thr | Cys | Thr-ol | ||
| In-DOTA-BOC | In-DOTA | phe | Cys | BzThi | trp | Lys | Thr | Cys | Thr-ol | ||
| NOC-ATE | phe | Cys | 1-Nal | trp | Lys | Thr | Cys | Thr | |||
| BOC-ATE | phe | Cys | BzThi | trp | Lys | Thr | Cys | Thr-ol | |||
| In-DOTA-NOC-ATE | In-DOTA | phe | Cys | 1-Nal | trp | Lys | Thr | Cys | Thr | ||
| Lu-DOTA-NOC-ATE | Lu-DOTA | phe | Cys | 1-Nal | trp | Lys | Thr | Cys | Thr | ||
| In-DOTA-BOC-ATE | In-DOTA | phe | Cys | BzThi | trp | Lys | Thr | Cys | Thr-ol | ||
| Lu-DOTA-BOC-ATE | Lu-DOTA | phe | Cys | BzThi | trp | Lys | Thr | Cys | Thr-ol | ||
| KE108 | Y-DOTA | Tyr | dab | Arg | Phe | Phe | trp | Lys | Thr | Phe | |
| KE121 | dab | Arg | Phe | Phe | trp | Lys | Thr | Phe | |||
| Y-DOTA-K121 (Y-KE88) | Y-DOTA | dab | Arg | Phe | Phe | trp | Lys | Thr | Phe | ||
| Ga-DOTA-K121 (Ga-KE88) | Y-DOTA | dab | Arg | Phe | Phe | trp | Lys | Thr | Phe | ||
| Y-DOTAGA-KE121 (Y-KE87) | Y-DOTA | dab | Arg | Phe | Phe | trp | Lys | Thr | Phe | ||
| Antagonists | |||||||||||
| In-DOTA-BASS | In-DOTA | pNO2−Phe | cys | Tyr | trp | Lys | Thr | Cys | tyr-NH2 | ||
| In-DOTA-JR11 | In-DOTA | Cpa | cys | Aph(Hor) | Aph(Cbm) | Lys | Thr | Cys | tyr-NH2 | ||
| Ga-DOTA-JR11 (Ga-OPS201) | Ga-DOTA | Cpa | cys | Aph(Hor) | Aph(Cbm) | Lys | Thr | Cys | tyr-NH2 | ||
| Ga-NODAGA-JR11 (Ga-OPS202) | Ga-NODAGA | Cpa | cys | Aph(Hor) | Aph(Cbm) | Lys | Thr | Cys | tyr-NH2 | ||
| Lu-DOTA-JR11 (Lu-OPS201) | Lu-DOTA | Cpa | cys | Aph(Hor) | Aph(Cbm) | Lys | Thr | Cys | tyr-NH2 | ||
| sst3-ODN-8 | NH2CO | cys | Phe | Tyr | DAgl8(Me,2-naphthoyl) | Lys | Thr | Phe | Cys | ||
| DOTA-sst3-ODN-8 | DOTA | NH2CO | cys | Phe | Tyr | DAgl8(Me,2-naphthoyl) | Lys | Thr | Phe | Cys | |
| DOTA-TOC | DOTA | d-Phe | Cys | Phe | d-Trp | Lys | Thr | Cys | Thr(ol) | ||
AgI, α-Aminoglycyl; Aph(Cbm), 4-aminocarbamoylphenylalanine; Aph(Hor), 4-amino-L-hydroorotylphenylalanine; BOC, [BzThi3]-octreotide; BOC-ATE, [BzThi3]-octreotate; BzThi, 3-benzothienylalanine; Cpa, 4-Cl-phenylalanine; Dab, α,γ-diaminobutyryl; DOTA, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid; DOTAGA, 1-(1-carboxy-3-carboxy-propyl)-4,7,10(carboxymethyl)-1,4,7,10-tetraazacyclo-dodecane; DTPA, diethylenetriaminepentaacetic acid; Gal-S, galactosyl-mercaptopropionyl; Gluc, glucosyl; Gluc-S, glucosyl-mercaptopropionyl; Gluc-Lys(FP), Nα-glucosyl-Nε-(2-fluoropropionyl)Lys; 1-Nal, 1-naphthylalanine; NOC, [1-Nal3]-octreotide; TATE, [Tyr3,Thr8]-octreotide; TOC, [Tyr3]-octreotide.