High Contrast PET Imaging of GRPR Expression in Prostate Cancer Using Cobalt-Labeled Bombesin Antagonist RM26

<div>(a) Inhibition of <sup>125</sup>I-Tyr<sup>4</sup>-BBN binding to PC-3 cells with <svg height="14.9001pt" id="M32" style="vertical-align:-3.833899pt" version="1.1" viewbox="-0.0498162 -11.0662 27.7169 14.9001" width="27.7169pt" xmlns="http://www.w3.org/2000/svg" xmlns:xlink="http://www.w3.org/1999/xlink"><g transform="matrix(.0091,0,0,-0.0091,0,-5.741)"><path d="M524 0V26C466 32 460 36 460 104V297C460 393 411 449 331 449C302 449 276 437 248 419C223 402 201 387 181 372V451C137 432 90 420 42 411V388C96 378 102 374 102 310V104C102 38 97 33 29 26V0H246V26C187 32 181 36 181 104V339C211 365 250 390 290 390C357 390 381 345 381 276V109C381 40 374 32 315 26V0H524Z" id="g190-111"></path><glyph.data ascent="989" descent="-360" horiz-adv-x="547" vert-adv-y="547" xpluscharwidth="4.977683590000001"></glyph.data></g><g transform="matrix(.0091,0,0,-0.0091,4.95,-5.741)"><path d="M433 39L423 65C413 59 399 54 387 54C370 54 352 69 352 114V299C352 352 342 392 307 422C285 440 255 449 225 449C168 437 102 399 75 379C56 365 44 353 44 339C44 315 69 296 87 296C101 296 111 303 116 319C124 349 133 371 145 385C156 397 171 404 190 404C241 404 275 364 275 291V274C253 256 180 229 120 209C65 190 39 159 39 110C39 47 88 -12 159 -12C189 -12 237 25 277 52C282 35 288 21 301 8C312 -3 333 -12 348 -12L433 39ZM275 84C256 65 221 48 195 48C164 48 124 73 124 124C124 161 146 180 185 198C206 208 254 229 275 240V84Z" id="g190-98"></path><glyph.data ascent="989" descent="-360" horiz-adv-x="439" vert-adv-y="439" xpluscharwidth="8.944886830000002"></glyph.data></g><g transform="matrix(.0091,0,0,-0.0091,8.772,-5.741)"><path d="M298 36L289 62C276 55 253 45 228 45C202 45 169 60 169 141V397H276C289 405 292 426 282 437H169V574L155 576L90 509V437H45L17 408L21 397H90V107C90 28 125 -12 188 -12C198 -12 213 -8 230 1L298 36Z" id="g190-117"></path><glyph.data ascent="989" descent="-360" horiz-adv-x="305" vert-adv-y="305" xpluscharwidth="11.54749085"></glyph.data></g><g transform="matrix(.013,0,0,-0.013,12.089,0)"><path d="M614 175C564 76 510 21 408 21C256 21 146 149 146 336C146 488 235 629 402 629C510 629 570 586 597 480L626 488C620 541 614 582 606 638C578 643 510 665 429 665C206 665 44 527 44 316C44 157 153 -15 402 -15C474 -15 558 5 586 11C604 45 629 119 643 165L614 175Z" id="g190-68"></path><glyph.data ascent="989" descent="-360" horiz-adv-x="665" vert-adv-y="665" xpluscharwidth="20.734"></glyph.data></g><g transform="matrix(.013,0,0,-0.013,20.93,0)"><path d="M257 449C165 449 37 374 37 209C37 98 119 -12 256 -12C355 -12 473 65 473 226C473 349 381 449 257 449ZM244 416C333 416 380 320 380 204C380 67 329 21 267 21C184 21 130 115 130 241C130 354 184 416 244 416Z" id="g190-112"></path><glyph.data ascent="989" descent="-360" horiz-adv-x="510" vert-adv-y="510" xpluscharwidth="27.56"></glyph.data></g></svg>-NOTA-PEG<sub>2</sub>-RM26 and <svg height="14.9001pt" id="M33" style="vertical-align:-3.833899pt" version="1.1" viewbox="-0.0498162 -11.0662 23.5674 14.9001" width="23.5674pt" xmlns="http://www.w3.org/2000/svg" xmlns:xlink="http://www.w3.org/1999/xlink"><g transform="matrix(.0091,0,0,-0.0091,0,-5.741)"><path d="M524 0V26C466 32 460 36 460 104V297C460 393 411 449 331 449C302 449 276 437 248 419C223 402 201 387 181 372V451C137 432 90 420 42 411V388C96 378 102 374 102 310V104C102 38 97 33 29 26V0H246V26C187 32 181 36 181 104V339C211 365 250 390 290 390C357 390 381 345 381 276V109C381 40 374 32 315 26V0H524Z" id="g190-111"></path><glyph.data ascent="989" descent="-360" horiz-adv-x="547" vert-adv-y="547" xpluscharwidth="4.977683590000001"></glyph.data></g><g transform="matrix(.0091,0,0,-0.0091,4.95,-5.741)"><path d="M433 39L423 65C413 59 399 54 387 54C370 54 352 69 352 114V299C352 352 342 392 307 422C285 440 255 449 225 449C168 437 102 399 75 379C56 365 44 353 44 339C44 315 69 296 87 296C101 296 111 303 116 319C124 349 133 371 145 385C156 397 171 404 190 404C241 404 275 364 275 291V274C253 256 180 229 120 209C65 190 39 159 39 110C39 47 88 -12 159 -12C189 -12 237 25 277 52C282 35 288 21 301 8C312 -3 333 -12 348 -12L433 39ZM275 84C256 65 221 48 195 48C164 48 124 73 124 124C124 161 146 180 185 198C206 208 254 229 275 240V84Z" id="g190-98"></path><glyph.data ascent="989" descent="-360" horiz-adv-x="439" vert-adv-y="439" xpluscharwidth="8.944886830000002"></glyph.data></g><g transform="matrix(.0091,0,0,-0.0091,8.772,-5.741)"><path d="M298 36L289 62C276 55 253 45 228 45C202 45 169 60 169 141V397H276C289 405 292 426 282 437H169V574L155 576L90 509V437H45L17 408L21 397H90V107C90 28 125 -12 188 -12C198 -12 213 -8 230 1L298 36Z" id="g190-117"></path><glyph.data ascent="989" descent="-360" horiz-adv-x="305" vert-adv-y="305" xpluscharwidth="11.54749085"></glyph.data></g><g transform="matrix(.013,0,0,-0.013,12.089,0)"><path d="M303 0V28C221 34 213 39 213 125V525C213 610 221 616 303 622V650H38V622C120 616 128 610 128 525V125C128 40 120 34 38 28V0H303Z" id="g121-71"></path><glyph.data ascent="989" descent="-360" horiz-adv-x="341" vert-adv-y="341" xpluscharwidth="16.522"></glyph.data></g><g transform="matrix(.013,0,0,-0.013,16.314,0)"><path d="M524 0V26C466 32 460 36 460 104V297C460 393 411 449 331 449C302 449 276 437 248 419C223 402 201 387 181 372V451C137 432 90 420 42 411V388C96 378 102 374 102 310V104C102 38 97 33 29 26V0H246V26C187 32 181 36 181 104V339C211 365 250 390 290 390C357 390 381 345 381 276V109C381 40 374 32 315 26V0H524Z" id="g121-108"></path><glyph.data ascent="989" descent="-360" horiz-adv-x="547" vert-adv-y="547" xpluscharwidth="23.425"></glyph.data></g></svg>-NOTA-PEG<sub>2</sub>-RM26. Data are presented as mean values of three dishes ± SD. (b) LigandTracer sensorgram and fitted binding curve of <sup>57</sup>Co-NOTA-PEG<sub>2</sub>-RM26 interaction with GRPR-expressing PC-3 cells at room temperature. Uptake curves were recorded at 0.33 and 6 nM. The data were fitted to a one-to-one interaction model.</div>

Contrast Media & Molecular Imaging

fig3

Figure 3

Figure 3: High Contrast PET Imaging of GRPR Expression in Prostate Cancer Using Cobalt-Labeled Bombesin Antagonist RM26 