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Research library — page 31

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RPEP-01801 · 2011

CCK-8 Activates mTOR Signaling in Hypothalamic Appetite Neurons

Sulfated CCK-8 activated phospho-mTOR immunoreactive neurons in the paraventricular nucleus, linking the satiety hormone to mTOR nutrient-sensing pathways in appetite-controlling brain regions.

Lembke, Vanessa; Goebel, Miriam; Frommelt, Lisa; Inhoff, Tobias; Lommel, Reinhardt; Stengel, Andreas; Taché, Yvette; Grötzinger, Carsten; Bannert, Norbert; Wiedenmann, Bertram; Klapp, Burghard F; Kobelt, Peter ·

RPEP-01803 · 2011

New Screening Assay for Finding Ghrelin Receptor Drug Candidates

A homogeneous time-resolved fluorescence assay was developed for high-throughput screening of GHS-R1a ligands, enabling rapid identification of novel ghrelin receptor drug candidates for obesity and GH deficiency.

Leyris, Jean-Philippe; Roux, Thomas; Trinquet, Eric; Verdié, Pascal; Fehrentz, Jean-Alain; Oueslati, Nadia; Douzon, Stéphanie; Bourrier, Emmanuel; Lamarque, Laurent; Gagne, Didier; Galleyrand, Jean-Claude; M'kadmi, Céline; Martinez, Jean; Mary, Sophie; Banères, Jean-Louis; Marie, Jacky ·

RPEP-01804 · 2011

Soluble Thymosin Alpha-1 Concatemer With Enhanced Immunostimulatory Activity

A novel soluble thymosin alpha-1 concatemer showed stronger immunostimulatory activity than monomeric TA1, enhancing T-cell activation and cytokine production — improved manufacturing for enhanced immune therapy.

Li, Weina; Song, Liqiang; Wu, Shouzhen; Xue, Xiaochang; Zhang, Lu; He, Liqing; Han, Wei; Wang, Qing; Ling, Rui; Zhang, Wei; Yan, Zhen; Zhang, Yingqi ·

RPEP-01805 · 2011

BDNF and TrkB Increase in Pain-Sensing Nerves During Inflammation

BDNF and its TrkB receptor were upregulated in dorsal root ganglia during inflammatory pain in vivo and in vitro, establishing the BDNF-TrkB axis as a contributor to inflammatory pain sensitization.

Lin, Ya-Tin; Ro, Long-Sun; Wang, Hung-Li; Chen, Jin-Chung ·

RPEP-01814 · 2011

Rearranging the Small Intestine Changes How CCK Controls Appetite: Surgical Implications

Ileal interposition (moving a piece of lower intestine up) attenuated CCK-8 and CCK-33 satiety responses, showing that intestinal anatomical rearrangement changes gut peptide appetite signaling — bariatric surgery insight.

Metcalf, Shannon A; Washington, Martha C; Brown, Thelma A L; Williams, Carol S; Strader, April D; Sayegh, Ayman I ·

RPEP-01816 · 2011

Neuropeptides in the Human Thymus: Normal Function and Disease Changes

The human thymus contains diverse neuropeptides (VIP, substance P, NPY, CGRP, somatostatin) that regulate thymic function, with changes in neuropeptide profiles occurring in thymic pathology and autoimmune disease.

Mignini, F; Sabbatini, M; D'Andrea, V; Cavallotti, C ·

RPEP-01819 · 2011

Ghrelin in Reproductive Function: Beyond Appetite to Fertility Regulation

Ghrelin's reproductive roles include direct gonadal effects, hypothalamic GnRH modulation, and metabolic-fertility coupling — linking nutritional status to reproductive capacity through the ghrelin system.

Muccioli, Giampiero; Lorenzi, Teresa; Lorenzi, Maria; Ghè, Corrado; Arnoletti, Elisa; Raso, Giuseppina Mattace; Castellucci, Mario; Gualillo, Oreste; Meli, Rosaria ·

RPEP-01820 · 2011

Active Peptides From Milk: Complete Review of Production Methods and Health Functions

Comprehensive review of bioactive milk peptides covering production methods (enzymatic, fermentation, recombinant), functional activities (antimicrobial, antihypertensive, opioid, immunomodulatory, mineral-binding), and commercial applications.

Muro Urista, C; Álvarez Fernández, R; Riera Rodriguez, F; Arana Cuenca, A; Téllez Jurado, A ·

RPEP-01822 · 2011

CRF Peptide Family in Appetite and Anxiety: The Stress-Eating Connection

CRF family peptides (CRF, urocortins) regulate both food intake and anxiety through distinct CRF1/CRF2 receptor pathways, linking stress responses to eating behavior — the molecular basis of stress eating.

Nakayama, Naoko; Suzuki, Hajime; Li, Jiang-Bo; Atsuchi, Kaori; Tsai, Minglun; Amitani, Haruka; Asakawa, Akihiro; Inui, Akio ·

RPEP-01823 · 2011

Endokinin C/D Peptides in Pain and Inflammation Processing

Endokinin C/D-derived peptides modulated nociceptive and inflammatory responses in rats through tachykinin receptor activation, expanding the known tachykinin peptide family's role in pain and inflammation.

Naono-Nakayama, Rumi; Sunakawa, Natsuki; Ikeda, Tetsuya; Matsushima, Osamu; Nishimori, Toshikazu ·

RPEP-01824 · 2011

Melanocortin Agonist Reduces Alcohol Consumption in Rats: MC Receptors in Addiction

A melanocortin (MC) receptor agonist reduced voluntary ethanol consumption in rats, establishing melanocortin receptor activation as a potential therapeutic approach for reducing alcohol intake in addiction.

Navarro, Montserrat; Lerma-Cabrera, Jose M; Carvajal, Francisca; Lowery, Emily G; Cubero, Inmaculada; Thiele, Todd E ·

RPEP-01829 · 2011

Peptide Absorption Through the Gut Transporter hPEPT1: Drug Delivery Through the Intestine

Dipeptide affinity and translocation relationships via the intestinal peptide transporter hPEPT1 were characterized, guiding design of peptide-based oral drugs that exploit this gut absorption pathway.

Omkvist, Diana Højmark; Trangbæk, Dennis Jespersen; Mildon, Jemma; Paine, James S; Brodin, Birger; Begtrup, Mikael; Nielsen, Carsten Uhd ·

RPEP-01832 · 2011

GHRH Antagonists Inhibit Ovarian Cancer Growth: Blocking the Growth Hormone Axis Fights Cancer

Growth hormone-releasing hormone antagonists inhibited human ovarian cancer growth through multiple mechanisms — direct antiproliferative, reduced IGF-1 signaling, and apoptosis induction — adding ovarian cancer to GHRH antagonist targets.

Papadia, A; Schally, A V; Halmos, G; Varga, J L; Seitz, S; Buchholz, S; Rick, F; Zarandi, M; Bellyei, S; Treszl, A; Szalontay, L; Lucci, J A ·

RPEP-01835 · 2011

Automated Radiolabeling of Peptides for Cancer Imaging and Therapy

A fully automated disposable cassette system for radiolabeling peptides (PET, SPECT, therapeutic isotopes) standardized the production of radiopharmaceutical peptides — enabling clinical-grade peptide radiotracer manufacturing.

Petrik, Milos; Knetsch, Peter A; Knopp, Roger; Imperato, Giovanni; Ocak, Meltem; von Guggenberg, Elisabeth; Haubner, Roland; Silbernagl, Roland; Decristoforo, Clemens ·

RPEP-01836 · 2011

BPC-157 Treats Sphincter Failure-Induced Esophagitis AND Pancreatitis in Rats and Humans

BPC-157 improved sphincter dysfunction-related esophagitis and pancreatitis in both rat models AND human acute pancreatitis patients with low sphincter pressures — translational evidence spanning animal to human.

Petrovic, I; Dobric, I; Drmic, D; Sever, M; Klicek, R; Radic, B; Brcic, L; Kolenc, D; Zlatar, M; Kunjko, K; Jurcic, D; Martinac, M; Rasic, Z; Boban Blagaic, A; Romic, Z; Seiwerth, S; Sikiric, P ·

RPEP-01839 · 2011

In Prader-Willi Syndrome, High Ghrelin Better Explains Overeating Than High PYY/GLP-1

Adults with Prader-Willi syndrome had elevated ghrelin more consistently than altered PYY/GLP-1, with high ghrelin better explaining the hyperphagia (extreme eating) than satiety peptide changes.

Purtell, Louise; Sze, Lisa; Loughnan, Georgina; Smith, Ellie; Herzog, Herbert; Sainsbury, Amanda; Steinbeck, Katharine; Campbell, Lesley V; Viardot, Alexander ·

RPEP-01841 · 2011

GHRH Antagonists Shrink Enlarged Prostates in Rats: A New Approach to BPH Treatment

GHRH antagonists reduced prostate size in experimental benign prostatic hyperplasia, with effects comparable to finasteride — offering a novel GH-axis-based approach to treating enlarged prostate without affecting testosterone.

Rick, Ferenc G; Schally, Andrew V; Block, Norman L; Nadji, Mehrdad; Szepeshazi, Karoly; Zarandi, Marta; Vidaurre, Irving; Perez, Roberto; Halmos, Gabor; Szalontay, Luca ·

RPEP-01845 · 2011

Peptides That Starve Tumors by Blocking New Blood Vessel Growth: A Comprehensive Review

Multiple anti-angiogenic peptides (50 amino acids or shorter) derived from endogenous proteins like thrombospondin, collagens, chemokines, and growth factors have shown promise in preclinical cancer models and some have reached clinical trials. These peptides work by blocking the formation of new blood vessels that tumors need to grow. Various protein modification strategies — including D-amino acid substitution and non-natural amino acid incorporation — have been used to improve their stability and potency. Computational tools and bioinformatics approaches are accelerating the discovery and optimization of new anti-angiogenic peptide candidates.

Rosca, Elena V; Koskimaki, Jacob E; Rivera, Corban G; Pandey, Niranjan B; Tamiz, Amir P; Popel, Aleksander S · Review

RPEP-01848 · 2011

A Neglected Brain Region and Its Neuropeptide Relaxin-3 May Hold Keys to Understanding Anxiety, Insomnia, and Memory

The nucleus incertus is a GABAergic brainstem nucleus with broad forebrain projections that: expresses CRF receptors and is activated by psychological stressors, modulates hippocampal theta rhythm (linked to spatial navigation and memory), contains a significant population of relaxin-3-expressing neurons, and projects to key nuclei involved in stress responses and behavioral activation. Chimeric peptides that selectively activate or inhibit the relaxin-3 receptor RXFP3 are now available for research, enabling targeted studies of relaxin-3/RXFP3 networks and their roles in arousal, stress, and cognition.

Ryan, Philip J; Ma, Sherie; Olucha-Bordonau, Francisco E; Gundlach, Andrew L ·

RPEP-01852 · 2011

Beyond Pain Relief: The Many Roles of Opioid Peptides in Depression, Gut Disease, Immunity, and More

The review catalogs the multifunctional roles of endogenous opioid peptides across multiple organ systems: - Central nervous system: Opioid peptides are implicated in depression (endorphin deficiency), anxiety (anxiolytic effects via mu and delta receptors), epilepsy (seizure modulation), and stress response - Gastrointestinal system: Roles in diarrhea, postoperative ileus, gastric ulceration, and irritable bowel syndrome through peripheral opioid receptors on mucosal cells - Immune system: Modulation of inflammatory responses in osteoarthritis and rheumatoid arthritis through opioid receptors on immune cells - Cardiovascular system: Critical role in ischemic pre- and post-conditioning, including pharmacological and remote preconditioning cardioprotection - Behavioral: Involvement in alcoholism and obesity/binge eating through reward circuit modulation The four major opioid peptides (from three independent gene families) exhibit different affinities for mu, delta, and kappa receptors, explaining their diverse and sometimes opposing effects across organ systems.

Sauriyal, Dharmraj Singh; Jaggi, Amteshwar Singh; Singh, Nirmal ·

RPEP-01853 · 2011

Peptide-Guided Missiles: Using Hormone Analogs to Deliver Chemo Directly to Tumors

Peptide hormones can be chemically attached to cancer-killing drugs (cytotoxic agents) to create targeted chemotherapy that homes in on tumors expressing specific peptide receptors. The review covers three families of peptide-drug conjugates: LH-RH analogs (AN-152, AN-207) carrying doxorubicin that target LH-RH receptors on prostate, breast, ovarian, and endometrial cancers; somatostatin analogs (AN-162, AN-238) targeting somatostatin receptors on prostate, mammary, pancreatic, colorectal, gastric, and brain cancers; and bombesin/GRP analogs (AN-215) targeting bombesin receptors. All three approaches suppressed tumor growth and metastases in preclinical models. The LH-RH conjugate AN-152 reached clinical trials: in phase I testing in women with ovarian or endometrial cancer, it showed disease stabilization and objective tumor responses. Phase II trials were underway at the time of publication, with additional trials pending in prostate, pancreatic, and bladder cancers.

Schally, Andrew V; Engel, Jorg B; Emons, Gunter; Block, Norman L; Pinski, Jacek · Review

RPEP-01866 · 2011

Tesamorelin GHRH Peptide Boosts Natural Growth Hormone Pulses Without Affecting Insulin Sensitivity

Tesamorelin 2 mg daily for 2 weeks significantly increased: - Mean overnight GH (+0.5 μg/liter, p = 0.004) - Average GH peak area (p = 0.001) - Basal GH secretion (+0.008 μg/liter·min, p = 0.008) - IGF-1 (+181 μg/liter, p < 0.0001) Critically, insulin-stimulated glucose uptake (measured by gold-standard euglycemic clamp) was not significantly affected (p = 0.61), and fasting glucose remained stable (p = 0.93). This demonstrates that GHRH-mediated GH augmentation preserves insulin sensitivity, unlike exogenous GH administration which can worsen insulin resistance.

Stanley, Takara L; Chen, Cindy Y; Branch, Karen L; Makimura, Hideo; Grinspoon, Steven K ·

RPEP-01867 · 2011

How Ghrelin and CCK Work Together to Control Your Hunger and Fullness Signals

This review maps how gut peptides from the stomach and upper small intestine work together to control hunger and fullness. Ghrelin, produced in stomach X/A-like cells, is the only known peripheral hormone that stimulates appetite. Cholecystokinin (CCK) from the duodenum is its main counterpart, suppressing appetite. These two peptides interact directly, creating a regulatory network at the first point of nutrient contact. Several other peptides — including leptin, urocortin 2, amylin, and GLP-1 — amplify CCK's satiety signal through synergistic interactions. The review also highlights newer peptides discovered in the same stomach cells as ghrelin: obestatin (from the pro-ghrelin gene) and nesfatin-1 (from the nucleobindin2 gene), both under investigation for appetite regulation.

Stengel, Andreas; Taché, Yvette · Review

RPEP-01871 · 2011

Two Neuropeptides Could Address Both Inflammation and Nerve Damage in MS

VIP (vasoactive intestinal peptide) and PACAP (pituitary adenylate cyclase-activating peptide) have dual properties that make them attractive therapeutic candidates for multiple sclerosis: they are both potent anti-inflammatory agents and neuroprotective molecules. Both peptides showed significant activity in the EAE (experimental autoimmune encephalomyelitis) animal model of MS. Current MS drugs primarily target the immune system and work well at early stages but do little to prevent the neurodegeneration that causes permanent disability. VIP and PACAP could potentially address both components — calming the autoimmune attack and directly protecting nerve cells from damage. The review extensively maps the structure-activity relationships of these peptides with their receptors, laying groundwork for designing improved analogs.

Tan, Yossan-Var; Waschek, James A · Review

RPEP-01874 · 2011

B-Type Natriuretic Peptide as Both a Diagnostic Tool and Treatment for Heart Disease in Infants and Children

The natriuretic peptide system (including ANP and BNP) regulates fluid balance and blood vessel resistance. BNP assays serve diagnostic and prognostic purposes across various pediatric clinical scenarios including heart failure, congenital heart disease, and post-surgical management. Recombinant BNP (nesiritide) produced through DNA technology is available for therapeutic use. The review covers BNP physiology, diagnostic applications in pediatrics, and emerging reports of recombinant BNP treatment in the pediatric population.

Tobias, Joseph D ·

RPEP-01875 · 2011

Neuropeptide Y Injected Into a Key Brain Region Reduces Anxiety in Rats — But Through Different Receptors for Different Fears

Infusing neuropeptide Y (NPY) directly into the lateral septum — a brain region rich in NPY and involved in anxiety regulation — reduced anxiety-related behavior in rats across two of three behavioral tests. In the novelty-induced suppression of feeding test, NPY-treated rats ate sooner in an unfamiliar environment (an anxiety measure independent of appetite changes). In the shock-probe burying test, NPY reduced defensive burying behavior. However, NPY had no effect on the elevated plus-maze. Critically, blocking the Y1 receptor with the antagonist BIBO 3304 reversed NPY's anti-anxiety effect in the feeding test but not in the shock-probe test. This suggests NPY reduces different types of anxiety through different receptor mechanisms in the lateral septum — Y1-dependent for some anxiety behaviors and Y1-independent for others.

Trent, Natalie L; Menard, Janet L · Animal Study

RPEP-01880 · 2011

GHRH and GHRP-2 Peptides Override Growth Hormone Feedback Differently in Men and Women

In a randomized crossover study of 25 healthy older adults, sex differences, sex steroid supplementation (estradiol in women, testosterone in men), and combined GHRH/GHRP-2 peptide infusion each independently and significantly controlled GH autofeedback dynamics. Dual-peptide stimulation elevated nadir GH concentrations independently of sex steroids and sex (P=0.001). Women showed greater peak GH responses to the dual-peptide agonists than men (P=0.016). Sex steroid treatment augmented peak GH recovery during saline infusion (P<0.001). All three factors — sex, sex steroids, and peptide drive — independently augmented peak GH recovery (each P≤0.005).

Veldhuis, Johannes D; Erickson, Dana; Miles, John M; Bowers, Cyril Y ·

RPEP-01889 · 2011

Oxytocin Reduces Pain by Boosting Natural Opioid Peptides in the Brain's Pain Control Center

Four key findings emerged: (1) Pain stimulation increased PAG concentrations of oxytocin, leucine-enkephalin, methionine-enkephalin, and β-endorphin, but not dynorphin A(1-13). (2) Blocking oxytocin receptors in the PAG decreased levels of the three enkephalins/endorphin but not dynorphin. (3) The pain-relieving effect of oxytocin in the PAG was reversed by naloxone, an opioid receptor antagonist. (4) Exogenous oxytocin administration increased PAG levels of leucine-enkephalin, methionine-enkephalin, and β-endorphin, but not dynorphin. Together, this demonstrates that oxytocin's pain-modulating role in the PAG is mediated through enkephalin and endorphin peptides, but not dynorphin.

Yang, Jun; Liang, Jin-Ying; Li, Peng; Pan, Yan-Juan; Qiu, Pei-Yong; Zhang, Jing; Hao, Fang; Wang, Da-Xin ·