ライフサイエンスコーパス: GRPR

1 GRPR activation also induces Akt phosphorylation, a prox

2 GRPR affinity (half-maximal inhibitory concentration, ro

3 GRPR appears to mediate all effects of GRP, but only par

4 GRPR mutant mice showed comparable thermal, mechanical,

5 GRPR overexpression was found in 75.8% of the 1,432 tumo

6 GRPR specificity was confirmed by significantly reduced

7 GRPR-binding specificity was demonstrated by reduced tum

8 GRPR-binding specificity was studied by coinjection of a

9 GRPR-deficient mice showed decreased inhibition of princ

10 GRPR-expressing neurons have high intrinsic excitability

11 ct spinal cerebrospinal fluid injection of a GRPR antagonist significantly inhibited scratching behav

12 particle generator, (212)Pb, combined with a GRPR-targeting peptide, GRPR1, in a prostate cancer mode

13 tion, we first studied four loss-of-affinity GRPR chimeric receptors formed by exchanging the four ex

14 Interestingly, pancreatic uptake, albeit GRPR-specific, declined rapidly with time.

15 gated for tumor integrin alpha(v)beta(3) and GRPR imaging, respectively.

16 Dual integrin alpha(v)beta(3) and GRPR recognition showed significantly improved tumor-tar

17 omparable dual integrin alpha(v)beta(3)- and GRPR-binding affinities in vitro, both of which were sli

18 used for dual integrin alpha(v)beta(3)- and GRPR-targeted imaging.

19 , beta-catenin, oestrogen receptor-alpha and GRPR that promotes melanoma aggressiveness in women.

20 ry concentration, room temperature, 2 h) and GRPR-mediated internalization (37 degrees C, 60 min) wer

21 (177)Lu-NeoBOMB1) showed comparably high and GRPR-specific uptake in the PC-3 xenografts (e.g., 30.6

22 a disruption of crosstalk between 5-HT1A and GRPR may be a useful antipruritic strategy.

23 biophysical studies suggest that 5-HT1A and GRPR may function as receptor heteromeric complexes.

24 egrin or GRPR or that coexpress integrin and GRPR for imaging and therapeutic applications.

25 a promising PET tracer for dual integrin and GRPR positive tumor imaging.

26 fact that many tumors are both integrin and GRPR positive, we designed and synthesized a heterodimer

27 4 amino acids that differed between NMBR and GRPR in the uTM5 region were exchanged, but only the sub

28 In contrast, VIPR, SPR, and GRPR expression was detected in 31%, 27%, and 8% of panc

29 In contrast, VIPR, SPR, and GRPR expression was detected in fewer of the pancreatic

30 d, 17 of which yielded association with ASD (GRPR, AP1S2, DDX53, HDAC8, PCDH19, PTCHD1, PCDH11X, PTCH

31 ed using male immunocompromised mice bearing GRPR-positive PC-3 human prostate cancer xenografts.

32 Because GRPR is overexpressed in a high percentage of ER-positiv

33 The association between GRPR expression and distant metastasis-free interval was

34 We studied associations between GRPR expression and clinical, pathologic, and biologic p

35 d a significant positive correlation between GRPR and SSTR2 expression analyzed by in vitro autoradio

36 tory concentration of 50% values for binding GRPR of JMV4168, JMV5132, (nat)Ga-JMV4168, and (nat)Ga-J

37 ed a chimeric receptor approach to make both GRPR loss of affinity and NMBR gain of affinity chimeras

38 C cells that express elevated levels of both GRPR and EGFR, we found that GRP induced rapid phosphory

39 at morphine triggers internalization of both GRPR and MOR1D, whereas GRP specifically triggers GRPR i

40 esize that a peptide ligand recognizing both GRPR and integrin will be advantageous because of its du

41 nergic pathways, which are likely relayed by GRPR and NPRA in the spinal cord, respectively.

42 inding affinity with c(RGDyK) and comparable GRPR-binding affinity with BBN(7-14).

43 PEG(3)-Glu-RGD-BBN possesses the comparable GRPR and integrin alpha(v)beta(3) receptor-binding affin

44 domain (uTM5) of the NMBR by the comparable GRPR domains decreased the affinity 16-fold.

45 r subtypes of breast cancer were considered, GRPR was overexpressed in 86.2% of luminal A-like tumors

46 NeoBOMB1 is a novel DOTA-coupled GRPR antagonist with high affinity for GRPR and excellen

47 These analogs have demonstrated GRPR-specific small-animal PET of tumors but have variou

48 of (64)Cu-DOTA-[Lys(3)]BBN is able to detect GRPR-positive prostate cancer.

49 [Lys3]BBN and PET are suitable for detecting GRPR-positive prostate cancer in vivo.

50 PR are the critical residues for determining GRPR selectivity and suggest that both receptor-ligand c

51 atching, an effect largely reduced by either GRPR antagonists or PI3Kgamma inhibitor.

52 nd behavioral approaches to further evaluate GRPR downstream signaling pathways.

53 Due to its high boron loading and excellent GRPR selectivity, this conjugate can be considered as a

54 est a mechanism whereby aberrantly expressed GRPR might alter the outcome of patients with colorectal

55 ectively ablated lamina I neurons expressing GRPR in the spinal cord of mice.

56 upled GRPR antagonist with high affinity for GRPR and excellent in vivo stability.

57 GRP has high affinity for GRPR and lower affinity for NMBR.

58 an RGD for integrin binding and bombesin for GRPR binding.

59 ich patients can be potential candidates for GRPR-based imaging or targeted therapy, we screened inva

60 ults demonstrate that selectivity of GRP for GRPR over NMBR is primarily determined by two amino acid

61 poses a NGO nanoclusters-based nanoprobe for GRPR targeted near-infrared fluorescence imaging for OSC

62 tory concentration of 50% values (in nM) for GRPR binding of JMV5132, JMV4168, (nat)Ga-JMV5132, (nat)

63 for the GRPR and >3,000-fold selectivity for GRPR over the closely related neuromedin B receptor (NMB

64 l to improve radiopharmaceutical therapy for GRPR-expressing malignancies.

65 ng showed that NPFF cells also differed from GRPR cells in having a higher frequency of miniature EPS

66 were vertical cells, but these differed from GRPR neurons (which are also vertical cells) in having a

67 able three amino acids in NMBR by those from GRPR caused a gain in affinity for each antagonist.

68 by novel sounds and aversive shocks, and GRP-GRPR signaling enhances auditory fear memories.

69 t the descending 5-HT system facilitates GRP-GRPR signaling via 5-HT1A to augment itch-specific outpu

70 These data demonstrate that GRP-GRPR signaling is necessary and sufficient for transmitt

71 s article we demonstrate that abrogating GRP/GRPR signaling specifically down-regulates HP1(Hsbeta) e

72 ined the mechanism of EGFR activation by GRP/GRPR in HNSCC proliferation.

73 In contrast, GRP/GRPR can be aberrantly expressed in colon cancer where t

74 These experiments establish GRP/GRPR signaling as a potent modulator of mesolimbic circu

75 tide/gastrin-releasing peptide receptor (GRP/GRPR) autocrine growth pathway is activated early in HNS

76 Activation of SCN GRP/GRPR neurons evoked scratching behavior.

77 It triggered GRPR internalization in HEK-GRPR cells and Ca(2+) release in PC-3 cells (EC(50) = 1.

78 Furthermore, high GRPR and SSTR2 mRNA levels were observed more frequently

79 when breast tumors overexpressed GRPR, high GRPR expression was also found in metastatic lymph nodes

80 All compounds revealed similarly high GRPR affinity (half-maximal inhibitory concentration, 1.

81 Primary tumors with high GRPR expression were associated with lower risk of dista

82 attractive biological features--e.g. higher GRPR-selectivity--vs their frog-homologues.

83 Analog affinities for the human GRPR determined against [(125)I-Tyr(4)]BBN were at the n

84 u-RM2, (177)Lu-AMTG showed slightly improved GRPR affinity, a similar low internalization rate, sligh

85 The substitutions of Thr(297) in GRPR by Pro from the comparable position in NMBR, Phe(30

86 ement of Thr(297), Phe(302), and Ser(305) in GRPR by the three comparable NMBR amino acids caused a 5

87 All effects of GRP were abrogated in GRPR-null mice.

88 comparable high and specific accumulation in GRPR-positive PC-3 tumors.

89 Significant accumulation of the activity in GRPR-positive pancreas was also observed (10.4 +/- 0.15

90 , in ex vivo naive mouse spinal cords and in GRPR transiently expressing HEK293 cells.

91 ion dosimetry, and efficacy were assessed in GRPR-positive prostate tumor-bearing mice after intraven

92 ng experiments against [(125)I-Tyr(4)]BBN in GRPR-positive PC-3 cell membranes.

93 inical evaluation of [(99m)Tc]Demomedin C in GRPR-expressing models are reported.

94 against [(125)I-Tyr(4)]BBN were conducted in GRPR-positive PC-3 cell membranes.

95 In radioligands specifically internalized in GRPR-expressing PC-3 cells.

96 Cs efficiently and specifically localized in GRPR-positive PC-3 xenografts in mice (4.4 percentage in

97 EC3 amino acids that differed in the NMBR in GRPR showed that two separate NMBR substitutions in the

98 tide chain, and compare their performance in GRPR-positive in vitro and in vivo models.

99 11)In-, and (177)Lu-NeoBOMB1 radioligands in GRPR-expressing cells and mouse models.

100 ching behaviour was significantly reduced in GRPR mutant mice in response to pruritogenic stimuli, wh

101 and its intracellular delivery was tested in GRPR expressing PC3 cells stably transfected with a luci

102 odels, in favor of future theranostic use in GRPR-positive cancer patients.

103 motif on key biologic parameters, including GRPR affinity, internalization efficiency, and in vivo s

104 antagonists at 20- and 30-A distance induce GRPR dimerization.

105 fine relieves itch by selectively inhibiting GRPR spinoparabrachial neurons.

106 s HP1(Hsbeta) expression and that inhibiting GRPR signaling, or ablating HP1(Hsbeta) expression, incr

107 This makes GRPR a multicancer target for theranostics, that is, mol

108 In addition, blocking MOR1D-GRPR association attenuates MIS but not MIA.

109 We show that NAc MSh GRPR-positive cells represent subpopulations of D2 recep

110 Binding affinity for both human and murine GRPR was determined using a cell-based competition assay

111 Next, GRPR, SSTR2, and CXCR4 mRNA levels were measured by quan

112 raphy on human cancer samples (IC(50) in nM: GRPR, 1.4 +/- 0.2; NMBR, 106 +/- 18; and BB(3)R, >1000).

113 presses integrin on tumor vasculature but no GRPR in tumor tissue, which had no uptake of (64)Cu-NOTA

114 e report on the direct comparison of 3 novel GRPR-targeted radiolabeled tracers: Al(18)F-JMV5132, (68

115 ide of SB3 by Sta(13)-Leu(14)-NH2, the novel GRPR antagonist NeoBOMB1 was generated and labeled with

116 ecommend a clinical evaluation of this novel GRPR-targeted ligand to investigate its potential for ra

117 cid with an aromatic ring in position 185 of GRPR and the size of the backbone substitution in positi

118 the backbone substitution in position 198 of GRPR were important for GRP selectivity.

119 n of NPY and abolished by spinal ablation of GRPR+ neurons with intrathecal injection of bombesin-sap

120 g via the unidirectional cross-activation of GRPR signaling by MOR1D heterodimerization.

121 us or cooling agents inhibit the activity of GRPR neurons via GABAergic signaling.

122 Upstream, but not downstream, aspects of GRPR signaling have been investigated extensively.

123 02), and Ser(305) of the fourth EC domain of GRPR are the critical residues for determining GRPR sele

124 nging the four extracellular (EC) domains of GRPR with the corresponding NMBR EC domains.

125 substitution of the third EC domain (EC3) of GRPR markedly decreased GRP affinity.

126 PLCbeta3 and IP3R3, downstream effectors of GRPR, specifically block MIS but not MIA.

127 correlate messenger RNA (mRNA) expression of GRPR, SSTR2, and CXCR4 with clinicopathologic and biolog

128 ) transients, and action potential firing of GRPR(+) neurons.

129 inhibits itch by suppressing the function of GRPR neurons.

130 -radiolabeled GRP analogs for PET imaging of GRPR expression in prostate cancer xenografted mice.

131 Hence, the prognostic impact of GRPR was lost when examined within specific molecular su

132 ochemistry for the presence and intensity of GRPR expression.

133 0.90], P=0.001), whereas high mRNA levels of GRPR were associated with a prolonged progression-free s

134 esin-saporin treatment reduced the number of GRPR+ neurons by 97% in the lumber spinal cord and 91% i

135 e aimed to offer a comprehensive overview of GRPR-targeted theranostics to inform researchers, clinic

136 elop 18F-labeled bombesin analogs for PET of GRPR expression in prostate cancer xenograft models.

137 d that these peptides can be used for PET of GRPR-expressing prostate cancer.

138 lockade diminished serine phosphorylation of GRPR with ozone or OVA.

139 tide conjugate enters cells via a process of GRPR mediated endocytosis followed by trafficking to dee

140 These data strengthen the role of GRPR neurons as a key circuit for itch transmission and

141 We review the role of GRPR-targeted molecular imaging for all stages of prosta

142 Here, we explore the current state of GRPR-targeted theranostics from bench to bedside, highli

143 ate its potential for radioligand therapy of GRPR-expressing malignancies.

144 RP sequences in the detection and therapy of GRPR-expressing tumors in humans.

145 pharmacokinetics for imaging and therapy of GRPR-expressing tumors.

146 pharmacokinetics for imaging and therapy of GRPR-expressing tumors.

147 gnificant impact on staging and treatment of GRPR-expressing tumors.

148 als for potential diagnosis and treatment of GRPR-positive tumors.

149 are needed to gain a better understanding of GRPR and PSMA expression patterns in these patients.

150 ch and chemical itch information converge on GRPR neurons and thus map an exquisite spinal circuitry

151 ow that glutamatergic excitatory inputs onto GRPR(+) neurons are facilitated in mouse models of chron

152 he facilitation of glutamatergic inputs onto GRPR(+) neurons under chronic itch-like conditions, prov

153 itory spontaneous synaptic transmission onto GRPR neurons.

154 ause pharmacological blockade of the CGRP or GRPR pathway, or genetic ablation of Grpr, led to a dras

155 gastrin-releasing peptide receptor (GRPR) or GRPR neurons in the SCN abolished contagious scratching

156 or targeting tumors that express integrin or GRPR or that coexpress integrin and GRPR for imaging and

157 r high selectivity of PD168368 for NMBR over GRPR.

158 mportantly, when breast tumors overexpressed GRPR, high GRPR expression was also found in metastatic

159 ated receptor for gastrin-releasing peptide (GRPR), we used a chimeric receptor approach and a site-d

160 ated with estrogen receptor (ER) positivity (GRPR was high in 83.2% of ER-positive and 12% of ER-nega

161 naptic terminals connected onto postsynaptic GRPR(+) neurons.

162 ancer, using recently developed radiolabeled GRPR ligands.

163 neurons, whereas expression of its receptor GRPR is restricted to lamina I of the dorsal spinal cord

164 e mediated by the heptahelical GRP receptor (GRPR) and NMB receptor (NMBR).

165 with spinal neurons expressing GRP receptor (GRPR) functioning as a key part of a convergent circuit

166 -Cas9-mediated knockout of the GRP receptor (GRPR) in auditory cortex indicate that VIP cells are str

167 Moreover, we found that GRP receptor (GRPR) is expressed in GABAergic interneurons of the late

168 Here we report that the GRP receptor (GRPR) is expressed in nucleus accumbens medial shell (NA

169 littermates, bombesin-treated GRP receptor (GRPR)-null mice had increased interstitial fibrosis but

170 cells, and neutrophils express GRP receptor (GRPR).

171 ), but that none coexpress the GRP receptor (GRPR).

172 of gastrin-releasing peptide (GRP) receptor (GRPR) in both androgen-dependent (AD) and androgen-indep

173 in-releasing peptide (GRP) and its receptor (GRPR) are important components of itch transmission.

174 rin-releasing peptide (GRP) or its receptor (GRPR).

175 ssion of gastrin-releasing peptide receptor (GRPR) and integrin alpha(v)beta(3) as well as unfavorabl

176 e potent gastrin-releasing peptide receptor (GRPR) antagonist (68)Ga-SB3 ((68)Ga-DOTA-p-aminomethylan

177 and the gastrin-releasing peptide receptor (GRPR) are coexpressed within a subpopulation of excitato

178 for the gastrin releasing peptide receptor (GRPR) as determined against [(125)I-Tyr(4)]BBN was high

179 n of the gastrin-releasing peptide receptor (GRPR) gene and that on chromosome 8 occurred approximate

180 n of the gastrin-releasing peptide receptor (GRPR) has been reported on various cancer types, for exa

181 ting the gastrin-releasing peptide receptor (GRPR) have shown promising results.

182 MOR) and gastrin-releasing peptide receptor (GRPR) in spinal GRPR-expressing neurons has been implica

183 zes with gastrin-releasing peptide receptor (GRPR) in the spinal cord, relaying itch information.

184 role of gastrin-releasing peptide receptor (GRPR) in various diseases, including cancer, has been ex

185 ssion of gastrin-releasing peptide receptor (GRPR) in various tumor types suggests that GRPR is an at

186 ubset of gastrin-releasing peptide receptor (GRPR) interneurons and are thus positioned at the center

187 The gastrin-releasing peptide receptor (GRPR) is a well-known target in cancer diagnosis and can

188 Gastrin releasing peptide receptor (GRPR) is an attractive target for OSCC imaging and thera

189 ted that gastrin-releasing peptide receptor (GRPR) is an itch-specific gene in the spinal cord, a lon

190 The gastrin-releasing peptide receptor (GRPR) is found to be overexpressed in a variety of human

191 Gastrin-releasing peptide receptor (GRPR) is overexpressed in human prostate cancer and is b

192 The gastrin-releasing peptide receptor (GRPR) is overexpressed in human prostate cancer.

193 The gastrin-releasing peptide receptor (GRPR) is overexpressed in many solid malignancies, parti

194 The gastrin-releasing peptide receptor (GRPR) is overexpressed in various cancers, including pro

195 /CT with gastrin-releasing peptide receptor (GRPR) ligand [(68)Ga]Ga-AMTG has recently been shown to

196 a novel gastrin-releasing peptide receptor (GRPR) ligand with improved metabolic stability, which mi

197 sts that gastrin-releasing peptide receptor (GRPR) might be a valuable target in breast cancer.

198 ation of gastrin-releasing peptide receptor (GRPR) neurons, which are essential for transmitting chem

199 ation of gastrin-releasing peptide receptor (GRPR) or GRPR neurons in the SCN abolished contagious sc

200 that the gastrin-releasing peptide receptor (GRPR) plays an important part in mediating itch sensatio

201 pressing gastrin releasing peptide receptor (GRPR) primarily comprise excitatory interneurons that re

202 CGRP and gastrin-releasing peptide receptor (GRPR) transmission because pharmacological blockade of t

203 for the gastrin-releasing peptide receptor (GRPR) with a fixed distance between their recognition mo

204 eceptor (gastrin-releasing peptide receptor (GRPR)).

205 Gastrin-releasing peptide receptor (GRPR), a member of the G protein-coupled receptor superf

206 peptide, gastrin-releasing peptide receptor (GRPR), is an exception, because numerous classes of pept

207 eceptor, gastrin-releasing peptide receptor (GRPR), is expressed by various cell types, and it is ove

208 n of the gastrin-releasing peptide receptor (GRPR), somatostatin receptor 2 (SSTR2), and chemokine C-

209 y to the gastrin-releasing peptide receptor (GRPR), which is overexpressed on a variety of solid tumo

210 city for gastrin-releasing peptide receptor (GRPR)-/prostate-specific membrane antigen (PSMA)-express

211 erapy of gastrin releasing peptide receptor (GRPR)-expressing tumors.

212 ting the gastrin-releasing peptide receptor (GRPR).

213 PR), and gastrin-releasing peptide receptor (GRPR).

214 ress the gastrin-releasing peptide receptor (GRPR).

215 ress the gastrin-releasing peptide receptor (GRPR).

216 expressing gastrin release protein receptor (GRPR), and show that targeting specificity is increased

217 Coactivation of 5-HT1A and GRP receptors (GRPR) greatly potentiates subthreshold, GRP-induced Ca(2

218 Gastrin releasing peptide receptors (GRPR) have been shown to be overexpressed in prostate ca

219 presses gastrin-releasing peptide receptors (GRPR) is critical for pruriceptive transmission.

220 MA) and gastrin-releasing peptide receptors (GRPRs) are both overexpressed in PC.

221 Gastrin-releasing peptide receptors (GRPRs) are potential molecular imaging targets in a vari

222 Gastrin-releasing peptide receptors (GRPRs) expressed on human tumors can serve as molecular

223 targets gastrin-releasing peptide receptors (GRPRs), which are overexpressed in prostate cancer (PC).

224 RC-3095 is a selective GRPR antagonist, recently found to have antiinflammatory

225 -releasing peptide receptor (GRPR) in spinal GRPR-expressing neurons has been implicated.

226 First, we studied GRPR and SSTR2 expression in 13 clinical breast cancer s

227 rons that express GRP and that likely target GRPR-expressing interneurons.

228 (99m)Tc]Demomedin C, can successfully target GRPR-expressing human tumors in vivo while displaying at

229 (177)Lu, and evaluated its ability to target GRPR in a preclinical model of human prostate cancer.

230 y of human GRP-based radiopeptides to target GRPR-positive lesions in vivo and has revealed the impac

231 Inhibiting this pathway by targeting GRPR or oestrogen receptor-alpha reduces metastasis in m

232 promising radiopharmaceutical for targeting GRPR-expressing tumors.

233 together, our data suggested that targeting GRPR and NPRA may provide effective treatments for aller

234 These data demonstrate that GRPR is required for mediating the itch sensation rather

235 a progressive ratio test, demonstrating that GRPR regulates motivated behaviors.

236 We hypothesize that GRPR signals in part through the PI3Kgamma/Akt pathway.

237 Our results thus indicate that GRPR may represent the first molecule that is dedicated

238 We propose that GRPR is an alternative chemotactic receptor that may pla

239 In a dry skin model of itch, we show that GRPR blockade or PI3Kgamma inhibition reversed the scrat

240 Our data also suggest that GRPR+ neurons are different from the spinothalamic tract

241 electrophysiological studies suggested that GRPR neurons receive glutamatergic input from NMBR neuro

242 r, these findings are highly suggestive that GRPR is expressed by the central terminals of DRG nocice

243 (GRPR) in various tumor types suggests that GRPR is an attractive target for cancer imaging and ther

244 Together, the present study suggests that GRPR+ neurons constitute a long-sought labeled line for

245 The GRPR antagonist JMV594 (H-D-Phe-Gln-Trp-Ala-Val-Gly-His-

246 The GRPR antagonist radioligands (67)Ga-, (111)In-, and (177

247 The GRPR gene was shown to escape X-inactivation.

248 of the 11 amino acid differences between the GRPR and NMBR in this domain were exchanged.

249 Each had high affinity for the GRPR and >3,000-fold selectivity for GRPR over the close

250 showed high affinity and selectivity for the GRPR during receptor autoradiography on human cancer sam

251 mbranes showed high binding affinity for the GRPR or the PSMA.

252 ecular basis for their high affinity for the GRPR, two classes of peptide antagonists, a statine anal

253 led to the N terminus and separated from the GRPR-targeting sequence by a cationic 4-amino-(1-carboxy

254 that two separate NMBR substitutions in the GRPR, Ile for Phe(185) or Ile for Ala(198), markedly dec

255 mpt to demonstrate a gain of affinity in the GRPR, the substitution of Tyr(219) for Phe caused an inc

256 N(7-14)NH(2) specifically accumulated in the GRPR-expressing PC-3 tumors and should be evaluated clin

257 tuting the fourth EC domain of NMBR into the GRPR resulted in a 300-fold gain in affinity for JMV594

258 ed by substituting the uTM5 of NMBR into the GRPR, a 9-fold increase in affinity occurred.

259 A dosage effect of the GRPR and a position effect of the SDC2 gene may, however

260 the fourth extracellular (EC) domain of the GRPR by the comparable NMBR domain markedly decreased th

261 between the aromatic ring of Phe(185) of the GRPR with GRP is the most important for GRP selectivity.

262 ned using in vitro and in vivo models of the GRPR-positive, PC-3 human prostate cancer cell line.

263 o evaluate the diagnostic performance of the GRPR-targeting radiopharmaceutical (68)Ga-RM2 in patient

264 In this study, the GRPR-targeting potential of (18)F-labeled NOTA-8-Aoc-BBN

265 ygalactosyl-carborane building blocks to the GRPR-selective ligand [d-Phe(6), beta-Ala(11), Ala(13),

266 n vivo interaction of radiopeptides with the GRPR.

267 Sta-BBN showed a similar binding affinity to GRPR on HSC-3 cells.

268 G-bombesin(7-14) bound with high affinity to GRPR with an inhibitory concentration of 50% of 3.5 and

269 G-bombesin(7-14) bound with high affinity to GRPR-expressing cells and that these peptides can be use

270 BBS binding to GRPR stimulated Gli through its downstream Galphaq and G

271 Ga-, (nat)In-, and (nat)Lu-NeoBOMB1 bound to GRPR with high affinity (half maximal inhibitory concent

272 SARNCs bound to GRPR with high affinity (range of 50% inhibitory concent

273 vents the facilitation of synaptic inputs to GRPR(+) neurons, and repetitive scratching behavior.

274 s with selectivity and with high affinity to GRPRs.

275 Recently, a (68)Ga-labeled antagonist to GRPRs, NeoBOMB1, was developed for PET.

276 mor-bearing xenograft mice, the CC-trapping, GRPR-targeted agonistic and antagonistic constructs led

277 e techniques confirmed that the CC-trapping, GRPR-targeted constructs were able to increase cellular

278 It triggered GRPR internalization in HEK-GRPR cells and Ca(2+) releas

279 and MOR1D, whereas GRP specifically triggers GRPR internalization and morphine-independent scratching

280 in a high percentage of ER-positive tumors, GRPR targeting offers wide perspectives for imaging and

281 for radioligand therapy, the most often used GRPR ligand, DOTA-Pip(5)-d-Phe(6)-Gln(7)-Trp(8)-Ala(9)-V

282 ermined in a competition-binding assay using GRPR-overexpressing PC-3 tumors.

283 data indicate that imaging and therapy using GRPR or SSTR2 radioligands might especially be beneficia

284 er, and other tumors and provide a quo vadis GRPR.

285 hting the preclinical development of various GRPR-targeting compounds and clinical applications.

286 find that itch is conveyed to the brain via GRPR-expressing spinal output neurons that target the la

287 f peptide +/- 40 nmol of Tyr(4)-BBN: in vivo GRPR blockade) in severe combined immune deficient mice

288 peptide +/- 40 nmol Tyr(4)-BBN: for in vivo GRPR blockade) in severe combined immunodeficiency mice

289 n PC-3 cells (37 degrees C, 60 min), whereas GRPR affinity (half-maximal inhibitory concentration) wa

290 input and form monosynaptic connections with GRPR neurons.

291 nano-graphene oxide (NGO) nanoparticles with GRPR-specific peptides AF750-6Ahx-Sta-BBN via hydrogen b