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Gastrin-Releasing Peptide (GRP) Stimulates Osteoclastogenesis in Periodontitis.

Periodontitis is a chronic inflammatory disease with alveolar bone resorption and subsequent tooth loss as its ultimate outcomes. Gastrin-releasing peptide (GRP) is a neuropeptide with growth-stimulatory and tumorigenic properties, and neuropeptides have previously been suggested to play a role in the complex cascade of chemical activity associated with periodontal inflammation. In this study, GRP treatment enhanced the differentiation of bone marrow-derived macrophages (BMMs) into osteoclasts, and gastrin-releasing peptide receptor (GRPR) antagonists suppressed the pro-osteoclastogenic effect

Synergistic antipruritic effects of gamma aminobutyric acid A and B agonists in a mouse model of atopic dermatitis.

BACKGROUND: Despite recent insights into the pathophysiology of acute and chronic itch, chronic itch remains an often intractable condition. Among major contributors to chronic itch is dysfunction of spinal cord gamma aminobutyric acidergic (GABAergic) inhibitory controls. OBJECTIVES: We sought to test the hypothesis that selective GABA agonists as well as cell transplant-derived GABA are antipruritic against acute itch and in a transgenic mouse model of atopic dermatitis produced by overexpression of the TH2 cell-associated cytokine, IL-31 (IL-31Tg mice). METHODS: We injected wild-type and

Radiolabeled Peptides and Antibodies in Medicine.

Radiolabeled peptides are a relatively new, very specific radiotracer group, which is still expanding. This group is very diverse in terms of peptide size. It contains very small structures containing several amino acids and whole antibodies. Moreover, radiolabeled peptides are diverse in terms of the binding aim and therapeutic or diagnostic applications. The majority of this class of radiotracers is utilized in oncology, where the same structure can be used in therapy and diagnostic imaging by varying the radionuclide. In this study, we collected new reports of radiolabeled peptide applicati

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… K. ; Varshney R. ; Allard M. ; Fernandez P. ; Hindie E. ( 2014 ) Targeting Neuropeptide Receptors for Cancer Imaging and Therapy: Perspectives with Bombesin, Neurotensin, and Neuropeptide-Y Receptors . J. Nucl. … T. ( 2015 ) Insights into bombesin receptors and ligands: Highlighting recent advances . …

Activation of kappa-opioid receptors depresses electrically evoked excitatory postsynaptic potentials on 5-HT-sensitive neurones in the rat dorsal raphé nucleus in vitro.

Intracellular recordings from dorsal raphé neurones in slices from rat brains were used to study the actions of kappa-opioid receptor agonists on an excitatory postsynaptic potential (epsp) evoked by local electrical stimulation of afferent terminals. The epsp was observed on all 5-HT-sensitive neurones and was blocked by 1 microM TTX. The epsp was reduced in a dose-dependent manner by the specific kappa-opioid receptor agonist [5R-(5 alpha,7 alpha,8 beta)]-N-methyl-N-[7-(1-pyrrolidinyl)-1- oxaspiro[4.5]dec-8-yl]-4-benzofuranacetamide monohydrochloride (CI-977) (1-100 nM). The effects of CI-97

Smart Targeting To Improve Cancer Therapeutics.

Cancer is the second largest cause of death worldwide with the number of new cancer cases predicted to grow significantly in the next decades. Biotechnology and medicine can and should work hand-in-hand to improve cancer diagnosis and treatment efficacy. However, success has been frequently limited, in particular when treating late-stage solid tumors. There still is the need to develop smart and synergistic therapeutic approaches to achieve the synthesis of strong and effective drugs and delivery systems. Much interest has been paid to the development of smart drug delivery systems (drug-loade

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… Development of high affinity camptothecin-bombesin conjugates that have targeted cytotoxicity for bombesin receptor-containing tumor. J Biol Chem . 2004;279(22):23580−23589. doi: 10.1074/jbc.M401938200 151. Moody T, Sun L, Mantey S, et al. … In vitro and in vivo antitumor effects of cytotoxic camptothecin-bombesin conjugates are mediated by specific interaction with cellular bombesin. J Pharmacol Exp Ther . 2006;318(3):1265−1272. doi: 10.1124/jpet.106.104141 152. Guan H, McGuire MJ, Li S, et al. …

Learn from antibody-drug conjugates: consideration in the future construction of peptide-drug conjugates for cancer therapy.

Cancer is one of the leading causes of death worldwide due to high heterogeneity. Although chemotherapy remains the mainstay of cancer therapy, non-selective toxicity and drug resistance of mono-chemotherapy incur broad criticisms. Subsequently, various combination strategies have been developed to improve clinical efficacy, also known as cocktail therapy. However, conventional "cocktail administration" is just passable, due to the potential toxicities to normal tissues and unsatisfactory synergistic effects, especially for the combined drugs with different pharmacokinetic properties. The drug

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… (7–14) Bombesin receptors Gly-Phe-Leu-Gly TH19P01 Sortilin receptor Redox sensitive Ddisulfide bond Bicycle MMP-14 Table 3 PDCs under phase III or phase II development Name Phase Target antigen Payload Refs GRN1005 3 LRP-1 Paclitaxel [ 161 ] AEZS-108 3 LHRH receptor DOX [ 162 ] EP-100 2 LHRH receptor … (7–14) | Bombesin receptors Gly-Phe-Leu-Gly | | TH19P01 | Sortilin receptor Redox sensitive | Ddisulfide bond | | Bicycle | MMP-14 Table 3 PDCs under phase III or phase II development Name | Phase | Target antigen | Payload | Refs GRN1005 | 3 | LRP-1 | Paclitaxel | [ 161 ] AEZS-108 | 3 | LHRH receptor …

Molecular Approaches To Target GPCRs in Cancer Therapy

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… Radiolabeled and, more recently, nanoparticle-linked peptides (SST, bombesin, cholecystokinin [ 102 ], etc. ) have been used for in vivo imaging of inflammatory conditions and metastasis. … Development of high affinity camptothecin-bombesin conjugates that have targeted cytotoxicity for bombesin receptor-containing tumor cells J. Biol. Chem. 2004 279 23580 23589 15016826 10.1074/jbc.M401938200 99. Leuschner C. Hansel W. …

Histone Deacetylase Inhibitors in Pediatric Brain Cancers: Biological Activities and Therapeutic Potential.

Brain cancers are the leading cause of cancer-related deaths in children. Biological changes in these tumors likely include epigenetic deregulation during embryonal development of the nervous system. Histone acetylation is one of the most widely investigated epigenetic processes, and histone deacetylase inhibitors (HDACis) are increasingly important candidate treatments in many cancer types. Here, we review advances in our understanding of how HDACis display antitumor effects in experimental models of specific pediatric brain tumor types, i.e., medulloblastoma (MB), ependymoma (EPN), pediatric

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… However, bombesin receptor antagonists failed to potentiate the effects of HDACi inhibition ( Jaeger et al., 2016 ). Other studies have investigated combinations of HDACis with protein kinase signaling inhibitors. … Viability of D283 medulloblastoma cells treated with a histone deacetylase inhibitor combined with bombesin receptor antagonists. Childs Nerv. Syst. 32 61–64. 10.1007/s00381-015-2963-4 Jain S. U., Do T. J., Lund P. J., Rashoff A. Q., Diehl K. L., Cieslik M., et al. (2019). …

Anticancer peptides as novel immunomodulatory therapeutic candidates for cancer treatment.

Cancer remains a concern after years of research in this field. Conventional therapies such as chemotherapy, radiation, and surgery are available for cancer treatment, but they are characterized by various side effects. There are several immunological challenges that make it difficult for the immune system and conventional therapies to treat cancer. Some of these challenges include heterogeneity, resistance to medicines, and cancer relapse. Even advanced treatments like immune checkpoint inhibitors (ICIs), which revolutionized cancer treatment, have associated toxicity and resistance further n

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… A study by Liu et al. [ 124 ] (2011) showed the increased cytotoxicity of magainin upon conjugation with another peptide bombesin and suggested its applicability in targeted drug delivery. … Enhancement of cytotoxicity of antimicrobial peptide magainin II in tumor cells by bombesin-targeted delivery. Acta Pharmacol Sin. 2011;32:79–88. doi: 10.1038/aps.2010.162. 125. Anghel R, Jitaru D, Bădescu L, Bădescu M, Ciocoiu M. …

Antimitotic drugs in the treatment of cancer.

Cancer is a complex disease since it is adaptive in such a way that it can promote proliferation and invasion by means of an overactive cell cycle and in turn cellular division which is targeted by antimitotic drugs that are highly validated chemotherapy agents. However, antimitotic drug cytotoxicity to non-tumorigenic cells and multiple cancer resistance developed in response to drugs such as taxanes and vinca alkaloids are obstacles faced in both the clinical and basic research field to date. In this review, the classes of antimitotic compounds, their mechanisms of action and cancer cell res

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… Cancer cells may also produce their own growth factor ligands such as Bombesin-like peptides (secreted by human small cell lung cancer) or signal to non-tumorigenic surrounding tissue to supply cancer cells with growth factors (Fig. 1 ) [ 6 ]. … Bombesin-like peptides can function as autocrine growth factors in human small-cell lung cancer. Nature. 1985;316:823–825. doi: 10.1038/316823a0. 7. Kim MY, Oskarsson T, Acharyya S, Nguyen DX, Zhang XHF, Norton L, Massagué J. Tumor self-seeding by circulating cancer cells. …

Developing Actively Targeted Nanoparticles to Fight Cancer: Focus on Italian Research.

Active targeting is a valuable and promising approach with which to enhance the therapeutic efficacy of nanodelivery systems, and the development of tumor-targeted nanoparticles has therefore attracted much research attention. In this field, the research carried out in Italian Pharmaceutical Technology academic groups has been focused on the development of actively targeted nanosystems using a multidisciplinary approach. To highlight these efforts, this review reports a thorough description of the last 10 years of Italian research results on the development of actively targeted nanoparticles t

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… Liposomes that can target bombesin (BN)-receptor-overexpressing tissues have been prepared for theranostic purposes. …

Actinium-225 targeted alpha particle therapy for prostate cancer.

Targeted alpha particle therapy (TAT) has emerged as a promising strategy for the treatment of prostate cancer (PCa). Actinium-225 (225Ac), a potent alpha-emitting radionuclide, may be incorporated into targeting vectors, causing robust and in some cases sustained antitumor responses. The development of radiolabeling techniques involving EDTA, DOTA, DOTPA, and Macropa chelators has laid the groundwork for advancements in this field. At the forefront of clinical trials with 225Ac in PCa are PSMA-targeted TAT agents, notably [225Ac]Ac-PSMA-617, [225Ac]Ac-PSMA-I&T and [225Ac]Ac-J591. Ongoing inve

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… In addition to this, peptide formulation labeled with the 211 At has been tested to achieve TAT by targeting bombesin receptor 147 . … The bombesin targeting [ 211 At]At-AB-3 molecules failed to accumulate in the tumor to achieve sufficient concentration, possibly due to stability and dehalogenation issues. …

From Innate Immunity to Cancer Therapy: Antimicrobial Peptides as Emerging Anticancer Agents.

The potential for the use of antimicrobial peptides (AMPs) as anticancer agents has garnered much interest because of their selective cytotoxicity to tumor cells and ability to evade multidrug resistance mechanisms. AMPs are shorter cationic amphiphilic molecules, part of our innate immune system, with direct membrane-disruptive activity and immunomodulatory effects. Anticancer peptides (ACPs) can be derived from natural biophysical sources or synthetically engineered, taking advantage of the unique biophysical properties of cancer cell membranes to exert their anti-tumor activities rapidly an

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… PEGylated bombesin analogs, which exhibited considerably better in vitro and in vivo stability, and moreover enhanced tumor absorption [ 59 ]. PEG-conjugated GIRLRG peptide, which was displayed to have better metabolic stability and specificity to GRP78-overexpressing tumor cells [ 62 ]. 4.3. … clinically examined peptides: Tigapotide, SF1126, ATN-161, Teverelix, IRL-1620, Nelipepimut-S, Iseganan, G17DT, Canfosfamide, PM02734, CTCE-0214, Darinaparsin, and Labradimil; as well as eleven supplementary peptide prospects in study, specifically Ozarelix, Soblidotin, LTX-315, Balixafortide, VEGFR2–169, Bombesin …

Astatine-211 based radionuclide therapy: Current clinical trial landscape.

Astatine-211 (211At) has physical properties that make it one of the top candidates for use as a radiation source for alpha particle-based radionuclide therapy, also referred to as targeted alpha therapy (TAT). Here, we summarize the main results of the completed clinical trials, further describe ongoing trials, and discuss future prospects.

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… 67 , 68 ) | | 2Rs15d (Nanobody) | ( 69 ) | | 5F7 (single-domain antibody) | ( 70 ) Various | HER2/CEA | C6.5 & T84.66 (diabodies) | ( 71 ) Prostate | PSMA | (2S)-2-(3-(1-carboxy-5-(4- 211 At-astato-benzamido) pentyl)ureido) pentanedioic acid | ( 72 ) | PSCA | A11 (Minibody) | ( 73 ) | GRPR | Bombesin … Preliminary Evaluation of Astatine-211-Labeled Bombesin Derivatives for Targeted Alpha Therapy . Chem Pharm Bull (Tokyo). ( 2020 ) 68 : 538 – 45 . 10.1248/cpb.c20-00077 32475858 75. Carlin S Mairs RJ Welsh P Zalutsky MR . …

Radionuclide-labelled nanoparticles for cancer combination therapy: a review.

Radionuclide therapy (RT) is widely used to advanced local cancers. However, its therapeutic efficacy is limited to the radiation resistance of cancer cells. Combination therapy aims to circumvent tumor resistance, and the combination of RT with photothermal therapy (PTT), photodynamic therapy (PDT), chemotherapy (CMT), and immunotherapy has shown promising treatment outcomes. Nanotechnology holds promise in advancing combination therapy by integrating multiple therapies on a nanostructure platform. This is due to the increased surface area, passive/active targeting capabilities, high payload

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… Conjugate of Protoporphyrin IX (PPIX) and the bombesin (BBN) was synthesized as targeted agent with 64 Cu labeling. [ 64 Cu]PPIX-PEG6-BBN exhibited high uptake in PC-3 cells. … Cherenkov radiation 5,10,15,20-Tetrakis(4-hydroxyphenyl) porphyrin 5,10,15,20-Tetrakis(5-(4-aminophenyl) porphyrin Deferoxamine-porphyrin-PEG nanocomplex Porphyrin-PEG Magnetic nanoparticles Porphyrin molecules Tetrasulfonated alkylated metalloporphyrin Tetra-phenyl porphyrin Protoporphyrin IX Bombesin …

Nanoparticles for Targeted Drug Delivery to Cancer Stem Cells: A Review of Recent Advances.

Cancer stem cells (CSCs) are a subpopulation of cells that can initiate, self-renew, and sustain tumor growth. CSCs are responsible for tumor metastasis, recurrence, and drug resistance in cancer therapy. CSCs reside within a niche maintained by multiple unique factors in the microenvironment. These factors include hypoxia, excessive levels of angiogenesis, a change of mitochondrial activity from aerobic aspiration to aerobic glycolysis, an upregulated expression of CSC biomarkers and stem cell signaling, and an elevated synthesis of the cytochromes P450 family of enzymes responsible for drug

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… Au NPs have also been functionalized with folic acid, transferrin, and bombesin peptides for targeted drug delivery to ovarian, prostate, and breast cancers, respectively [ 83 , 84 , 85 ]. … Bombesin functionalized gold nanoparticles show in vitro and in vivo cancer receptor specificity Proc. Natl. Acad. Sci. USA 2010 107 8760 8765 10.1073/pnas.1002143107 20410458 PMC2889350 85. Li J.-L. Wang L. Liu X.-Y. Zhang Z.-P. Guo H.-C. Liu W.-M. Tang S.-H. …

Early detection of sporadic pancreatic cancer: summative review.

Pancreatic cancer (PC) is estimated to become the second leading cause of cancer death in the United States by 2020. Early detection is the key to improving survival in PC. Addressing this urgent need, the Kenner Family Research Fund conducted the inaugural Early Detection of Sporadic Pancreatic Cancer Summit Conference in 2014 in conjunction with the 45th Anniversary Meeting of the American Pancreatic Association and Japan Pancreas Society. This seminal convening of international representatives from science, practice, and clinical research was designed to facilitate challenging interdiscipli

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… Bombesin Receptors and MUC4 MRI Approach An unusual but nevertheless interesting approach has been imagined by Montet et al 137 using MRI modality. The investigators evaluated the feasibility to diagnose PC-targeting Bombesin receptors expressed in normal pancreatic tissue but not in PC. …

Current landscape and future directions of targeted-alpha-therapy for glioblastoma treatment.

Glioblastoma (GB) is the most aggressive malignancy of the central nervous system. Despite two decades of intensive research since the establishment of the standard of care, emerging strategies have yet to produce consistent satisfactory outcomes. Because of its specific localisation and intricate characteristics, GB is a uniquely regulated solid tumour with a strong resistance to therapy. Advances in targeted radionuclide therapy (TRT), particularly with the introduction of a-emitting radionuclides, have unveiled potential avenues for the management of GB. Recent preclinical and clinical stud

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… Ongoing clinical trials targeting GRPR with 212 Pb-labelled bombesin analogues ( NCT05283330 , recruiting) could potentially be adapted for GB treatment as well. Small molecules. …

The underexplored links between cancer and the internal body climate: Implications for cancer prevention and treatment.

In order to effectively manage and cure cancer we should move beyond the general view of cancer as a random process of genetic alterations leading to uncontrolled cell proliferation or simply a predictable evolutionary process involving selection for traits that increase cell fitness. In our view, cancer is a systemic disease that involves multiple interactions not only among cells within tumors or between tumors and surrounding tissues but also with the entire organism and its internal "milieu". We define the internal body climate as an emergent property resulting from spatial and temporal in

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… In some case for example, bombesin (BBS)-like neuropeptides secreted by SCC can act as autocrine growth factors ( 74 ). … Cross talk between the bombesin neuropeptide receptor and sonic hedgehog pathways in small cell lung carcinoma. Oncogene (2015) 34:1679–87. doi: 10.1038/onc.2014.104 75. Dossus L, Kouloura E, Biessy C, Viallon V, Siskos AP, Dimou N, et al. …

Program-Abstracts

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… Lewis , London, ON, Canada Intravital Imaging of Human Prostate Cancer Using Bombesin-Targeted Viral Nanoparticles 11:54 Christopher Gerner , Vienna, Austria Novel Multiple Myeloma Biomarker Candidates Identified in the Secretome of Bone Marrow Fibroblasts and Endothelial Cells 12:06 Thomas Mohr …