RPEP-01130 · 2006Semax (ACTH 4-10 analog) showed specific binding to rat brain tissue and increased brain-derived neurotrophic factor (BDNF) protein levels, confirming receptor-mediated neurotrophin enhancement as the mechanism for its nootropic and neuroprotective activities.
Dolotov, Oleg V; Karpenko, Ekaterina A; Seredenina, Tamara S; Inozemtseva, Lyudmila S; Levitskaya, Natalia G; Zolotarev, Yuriy A; Kamensky, Andrey A; Grivennikov, Igor A; Engele, Juergen; Myasoedov, Nikolay F · Animal Study
RPEP-01131 · 2006Lactoferricin B killed neuroblastoma cells in culture and significantly reduced xenograft tumor growth in nude mice — the first in-vivo demonstration of lactoferricin anticancer efficacy against a pediatric solid tumor.
Eliassen, Liv Tone; Berge, Gerd; Leknessund, Arild; Wikman, Mari; Lindin, Inger; Løkke, Cecilie; Ponthan, Frida; Johnsen, John Inge; Sveinbjørnsson, Baldur; Kogner, Per; Flaegstad, Trond; Rekdal, Øystein · Animal Study
RPEP-01132 · 2006Peripheral gut peptides (GLP-1, PYY, CCK, ghrelin) converge on the hypothalamic melanocortin system (POMC/AgRP neurons) as the central integration point, with melanocortin neurons serving as the final common pathway translating gut signals into eating behavior.
Ellacott, Kate L J; Halatchev, Ilia G; Cone, Roger D · Review
RPEP-01133 · 2006GHS-R1a in pituitary cells signaled through calcium mobilization, PKC, and MAPK pathways with receptor desensitization upon chronic ghrelin stimulation — comprehensive receptor characterization guiding GH secretagogue drug optimization.
Falls, H Douglas; Dayton, Brian D; Fry, Dennis G; Ogiela, Christopher A; Schaefer, Verlyn G; Brodjian, Sevan; Reilly, Regina M; Collins, Christine A; Kaszubska, Wiweka · In Vitro
RPEP-01134 · 2006Thymosin alpha-1 directly suppressed proliferation and induced apoptosis in human leukemia cell lines (HL-60, K562, Raji) through caspase activation, demonstrating direct cytotoxic anti-leukemic activity alongside its known immune enhancement.
Fan, Ying-zhe; Chang, Hui; Yu, Ye; Liu, Jing; Wang, Rui · In Vitro
RPEP-01135 · 2006Recombinant bovine lactoferricin B expressed as a fusion protein in E. coli retained antimicrobial activity after enzymatic cleavage, establishing a scalable bacterial expression system for commercial antimicrobial peptide production.
Feng, Xing-jun; Wang, Jian-hua; Shan, An-shan; Teng, Da; Yang, Ya-lin; Yao, Yi; Yang, Guan-pin; Shao, Yan-chun; Liu, Shuo; Zhang, Fan · In Vitro
RPEP-01136 · 2006The oral vasopressin V1a receptor antagonist SRX251 selectively reduced aggressive behavior in hamsters without affecting social investigation, communication, motor activity, or sexual motivation. The anti-aggression effect was dose-dependent: higher doses produced greater reductions in both the number of bites and the time before biting an intruder. The effect lasted over 6 hours and wore off by 12 hours.
Importantly, a comparison drug (Manning compound) that blocks the same receptor but poorly penetrates the brain had no effect on aggression — confirming that the anti-aggression action requires blocking vasopressin V1a receptors in the brain, not just in the body. This selectivity — reducing aggression without sedation or loss of normal social behavior — is what makes V1a antagonists potentially useful as targeted anti-violence medications.
Ferris, Craig F; Lu, Shi-Fang; Messenger, Tara; Guillon, Christophe D; Heindel, Ned; Miller, Marvin; Koppel, Gary; Robert Bruns, F; Simon, Neal G · Animal Study
RPEP-01137 · 2006Neuropeptides including VIP, alpha-MSH/KPV, and CGRP promote immune tolerance through generation of regulatory T cells (Tregs) and suppression of pro-inflammatory dendritic cell activation — a novel immunosuppressive pathway with therapeutic potential for autoimmunity and transplantation.
Ganea, Doina; Gonzalez-Rey, Elena; Delgado, Mario · Review
RPEP-01138 · 2006Dimeric KPV peptide (CKPV)2 inhibited endotoxin-induced host responses including fever, TNF-α/IL-6 release, and organ damage in mice, with enhanced anti-inflammatory potency compared to monomeric alpha-MSH — demonstrating improved efficacy through KPV dimerization.
Gatti, Stefano; Carlin, Andrea; Sordi, Andrea; Leonardi, Patrizia; Colombo, Gualtiero; Fassati, Luigi R; Lipton, James M; Catania, Anna · Animal Study
RPEP-01139 · 2006Ghrelin's complete food intake and energy homeostasis biology: meal-related regulation, orexigenic hypothalamic signaling, energy expenditure effects, adiposity promotion, GI motility control, and bidirectional therapeutic potential (antagonists for obesity, agonists for cachexia).
Gil-Campos, Mercedes; Aguilera, Concepción María; Cañete, Ramón; Gil, Angel · Review
RPEP-01140 · 2006GH secretagogues modulate HPA axis regulation through interactions with GABAergic, mineralocorticoid, and somatotropic pathways — explaining cortisol co-release during GH stimulation and the stress-axis implications of chronic GH secretagogue use.
Giordano, Roberta; Pellegrino, Micaela; Picu, Andreea; Bonelli, Lorenza; Balbo, Marcella; Berardelli, Rita; Lanfranco, Fabio; Ghigo, Ezio; Arvat, Emanuela · Review
RPEP-01141 · 2006Plasma apelin levels differentiated between cardiac and pulmonary disease causes and provided complementary prognostic information alongside natriuretic peptides — a new peptide biomarker for cardiopulmonary disease characterization.
Goetze, Jens Peter; Rehfeld, Jens F; Carlsen, Jørn; Videbaek, Regitze; Andersen, Claus B; Boesgaard, Soeren; Friis-Hansen, Lennart · Cross Sectional
RPEP-01142 · 2006Macrocyclic peptidomimetics intercepted S. aureus agr quorum sensing system, disrupting bacterial cell-to-cell communication and virulence factor production — an anti-virulence approach that disarms rather than kills bacteria, reducing resistance selection pressure.
Gorske, Benjamin C; Blackwell, Helen E · In Vitro
RPEP-01145 · 2006Kappa-opioid (dynorphin) and mu-opioid (endorphin/enkephalin) systems differentially regulated sucrose preference versus food-reinforced operant behavior in mice — different opioid families mediate different components of food reward and palatable eating.
Hayward, Michael D; Schaich-Borg, Alexandra; Pintar, John E; Low, Malcolm J · Animal Study
RPEP-01146 · 2006Ghrelin reduced hepatic insulin sensitivity (increased gluconeogenesis) while showing different effects on peripheral insulin sensitivity in mice, demonstrating tissue-specific ghrelin-insulin interactions with implications for diabetes pathophysiology.
Heijboer, A C; van den Hoek, A M; Parlevliet, E T; Havekes, L M; Romijn, J A; Pijl, H; Corssmit, E P M · Animal Study
RPEP-01147 · 2006The gut-brain glucose regulatory axis operates through incretin peptides (GLP-1, GIP), neural signals, and other gut hormones to control glucose metabolism — pharmacological exploitation has produced GLP-1 agonists and DPP-4 inhibitors as major diabetes drug classes.
Heijboer, A C; Pijl, H; Van den Hoek, A M; Havekes, L M; Romijn, J A; Corssmit, E P M · Review
RPEP-01148 · 2006Single SC injection of CJC-1295 maintained elevated pulsatile GH secretion and IGF-1 for days in healthy subjects, with dose-dependent duration of action — validating once-weekly (or less) dosing for sustained GH-axis restoration in the first human clinical trial.
Ionescu, Madalina; Frohman, Lawrence A · Clinical Trial
RPEP-01149 · 2006NMR comparison of 15-residue lactoferricin-derived peptides in membrane-mimetic environments showed helix amphipathicity and depth of membrane insertion correlated with antimicrobial activity — structural determinants of killing potency identified.
Jing, Weiguo; Svendsen, John S; Vogel, Hans J · In Vitro
RPEP-01150 · 2006All three opioid receptor types (mu, delta, kappa) were demonstrated in the guinea pig cochlea by RT-PCR, immunohistochemistry, and autoradiography, establishing the complete molecular basis for opioid peptide signaling in the auditory system.
Jongkamonwiwat, Nopporn; Phansuwan-Pujito, Pansiri; Casalotti, Stefano O; Forge, Andrew; Dodson, Hilary; Govitrapong, Piyarat · Animal Study
RPEP-01151 · 2006GKPV (alpha-MSH 10-13) immobilized on surfaces retained NF-κB inhibitory activity against TNF-α-stimulated inflammation in vitro, demonstrating that KPV-related peptides can function as bioactive anti-inflammatory coatings for medical devices and implants.
Kelly, J M; Moir, A J G; Carlson, K; Yang, Y; MacNeil, S; Haycock, J W · In Vitro
RPEP-01152 · 2006Lactoferricin B was expressed in E. coli by fusing it with an anionic peptide that neutralized its antibacterial activity during production, allowing the host bacteria to survive while manufacturing the antimicrobial peptide — a practical biotechnology solution.
Kim, Ha-Kun; Chun, Dae-Sik; Kim, Joon-Sik; Yun, Cheol-Ho; Lee, Ju-Hoon; Hong, Soon-Kwang; Kang, Dae-Kyung · In Vitro
RPEP-01153 · 2006Antibodies against poorly immunogenic prothymosin alpha were developed through peptide immunization strategies, enabling immunochemical detection of this thymosin alpha-1 precursor in tissues and cells for research applications.
Klimentzou, Persefoni; Paravatou-Petsotas, Maria; Zikos, Christos; Beck, Alexander; Skopeliti, Margarita; Czarnecki, Jan; Tsitsilonis, Ourania; Voelter, Wolfgang; Livaniou, Evangelia; Evangelatos, Gregory P · In Vitro
RPEP-01154 · 2006Chemoenzymatic design of daptomycin-related acidic lipopeptides created hybrid antibiotics with modified activity profiles, revealing SAR rules for the daptomycin macrocyclic core and advancing next-generation cyclic lipopeptide antibiotic design.
Kopp, Florian; Grünewald, Jan; Mahlert, Christoph; Marahiel, Mohamed A · In Vitro
RPEP-01155 · 2006RYGB produced significantly greater postprandial GLP-1 and PYY3-36 increases and greater ghrelin suppression than gastric banding, with hormonal changes correlating with superior weight loss — gut hormone modification, not restriction alone, explains bypass superiority.
Korner, Judith; Inabnet, William; Conwell, Irene M; Taveras, Carmen; Daud, Amna; Olivero-Rivera, Lorraine; Restuccia, Nancy L; Bessler, Marc · Cross Sectional
RPEP-01156 · 2006Despite being isolated in 1977, delta sleep-inducing peptide (DSIP) remains poorly understood. Its gene, protein precursor, and receptor have never been identified, and its role as a sleep factor is 'extremely poorly documented.' The authors hypothesize that a DSIP-like peptide — not DSIP itself — may be responsible for the observed biological activity. Key evidence: DSIP structural analogs (but not DSIP itself) promoted slow-wave sleep in rabbits and rats, and a naturally occurring peptide structurally similar to DSIP also promoted slow-wave sleep while its mirror-image isomer suppressed sleep.
Kovalzon, Vladimir M; Strekalova, Tatyana V · Review
RPEP-01157 · 2006BPC-157 promoted tendon-to-bone healing at the Achilles detachment site in rats, improving both normal healing AND opposing corticosteroid-impaired healing — demonstrating efficacy in the clinically challenging scenario of tendon repair during steroid therapy.
Krivic, Andrija; Anic, Tomislav; Seiwerth, Sven; Huljev, Dubravko; Sikiric, Predrag · Animal Study
RPEP-01158 · 2006Obese subjects showed comparable food intake stimulation from GHRP-2 as lean controls, demonstrating preserved ghrelin appetite sensitivity despite obesity — challenging the ghrelin resistance hypothesis and confirming appetite stimulation is a persistent GHS class effect.
Laferrère, Blandine; Hart, Allison B; Bowers, Cyril Y · RCT
RPEP-01160 · 2006Obese subjects demonstrated attenuated postprandial PYY3-36 release compared to lean controls, with reduced PYY correlating with diminished subjective satiety — PYY deficiency contributes to impaired meal-related fullness signaling in obesity.
le Roux, C W; Batterham, R L; Aylwin, S J B; Patterson, M; Borg, C M; Wynne, K J; Kent, A; Vincent, R P; Gardiner, J; Ghatei, M A; Bloom, S R · Clinical Trial
RPEP-01161 · 2006Bariatric surgery produced comprehensive gut hormone profile transformation: elevated GLP-1, PYY3-36, and oxyntomodulin with suppressed ghrelin, creating an anorectic hormonal milieu that facilitates weight loss and improves glucose metabolism beyond mechanical restriction.
le Roux, Carel W; Aylwin, Simon J B; Batterham, Rachel L; Borg, Cynthia M; Coyle, Frances; Prasad, Vyas; Shurey, Sandra; Ghatei, Mohammad A; Patel, Ameet G; Bloom, Stephen R · Clinical Trial
RPEP-01163 · 2006Naloxone blocked Selank's depriming effect on apomorphine-induced dopaminergic behavioral manifestations, directly confirming opioid system involvement in Selank's anxiolytic mechanism — linking its anti-anxiety action to enkephalin protection.
Meshavkin, V K; Kost, N V; Sokolov, O Yu; Zolotarev, Yu A; Myasoedov, N F; Zozulya, A A · Animal Study
RPEP-01165 · 2006Topical copper tripeptide complex (GHK-Cu) significantly accelerated healing after CO2 laser resurfacing in a double-blind, vehicle-controlled RCT, with faster re-epithelialization and improved skin quality — clinical validation of GHK-Cu for post-procedure skin recovery.
Miller, Timothy R; Wagner, Jon D; Baack, Bret R; Eisbach, Karl J · RCT
RPEP-01166 · 2006GHS-R gene polymorphism (Leu72Met) was significantly associated with bulimia nervosa in Japanese women, providing genetic evidence linking ghrelin receptor variation to eating disorder susceptibility.
Miyasaka, K; Hosoya, H; Sekime, A; Ohta, M; Amono, H; Matsushita, S; Suzuki, K; Higuchi, S; Funakoshi, A · Cross Sectional
RPEP-01167 · 2006Tyr-d-Arg-Phe-Sar analgesia at the spinal level involved both direct mu-1 opioid receptor activation and endogenous dynorphin B release, with anti-dynorphin antibodies partially blocking the effect — confirming dual direct + endogenous amplification mechanism.
Mizoguchi, Hirokazu; Ito, Kanenori; Watanabe, Hiroyuki; Watanabe, Chizuko; Katsuyama, Sou; Fujimura, Tsutomu; Sakurada, Tsukasa; Sakurada, Shinobu · Animal Study
RPEP-01168 · 2006Complete 2006 mapping of gut peptide appetite regulation: GLP-1 and PYY3-36 as top obesity targets, with CCK, oxyntomodulin, amylin, and PP providing complementary satiety signals — ghrelin as the sole orexigenic gut peptide.
Murphy, Kevin G; Dhillo, Waljit S; Bloom, Stephen R · Review
RPEP-01169 · 2006Ghrelin addresses cardiopulmonary cachexia through triple mechanism: GH-mediated anabolism, appetite stimulation to reverse wasting, and direct cardiac/pulmonary tissue protection — the most comprehensive single-agent approach to this devastating complication.
Nagaya, Noritoshi; Kojima, Masakazu; Kangawa, Kenji · Review
RPEP-01170 · 2006Adrenomedullin functions as a tumor progression factor primarily through angiogenesis promotion — stimulating tumor blood vessel formation, supporting cancer growth, and providing a targetable vulnerability for anti-cancer strategies.
Nakamura, Misa; Han, Bo; Nunobiki, Osamu; Kakudo, Kennichi · Review
RPEP-01172 · 2006GHS-R1a's constitutive activity, homo/hetero-oligomerization, and biased signaling create complex pharmacology requiring inverse agonists, biased ligands, or allosteric modulators rather than simple agonists/antagonists for effective obesity drug development.
Nogueiras, R; Perez-Tilve, D; Wortley, K E; Tschöp, M · Review
RPEP-01173 · 2006Rats prone to diet-induced obesity (DIO rats) showed significantly decreased spontaneous physical activity after 29 days on a high-fat diet, while diet-resistant (DR) rats maintained their activity levels. When orexin A was injected directly into the hypothalamus (paraventricular nucleus), DR rats showed a significantly greater increase in non-exercise activity thermogenesis (NEAT) compared to DIO rats.
This suggests that obesity-prone individuals may have reduced sensitivity to orexin's activity-promoting effects, creating a vicious cycle: a high-fat diet reduces spontaneous movement, and the brain's orexin system becomes less responsive to signals that would normally promote calorie-burning activity.
Novak, Colleen M; Kotz, Catherine M; Levine, James A · Animal Study
RPEP-01174 · 2006[Trp3,Arg5]-ghrelin(1-5), a modified pentapeptide, stimulated both GH secretion and food intake through GHS-R — demonstrating that ghrelin's full biological activity can be captured in just 5 amino acids with appropriate modifications.
Ohinata, Kousaku; Kobayashi, Kanako; Yoshikawa, Masaaki · Animal Study
RPEP-01176 · 2006PYY3-36 modulated thyrotropin (TSH) secretion in rats through hypothalamic/pituitary pathways, revealing a novel gut peptide-thyroid axis connection — the satiety system influences thyroid function beyond just appetite control.
Oliveira, K J; Paula, G S M; Costa-e-Sousa, R H; Souza, L L; Moraes, D C; Curty, F H; Pazos-Moura, C C · Animal Study
RPEP-01177 · 2006BPC-157 healed prolonged esophagitis and improved lower esophageal sphincter function in a rat reflux model with sphincter failure, addressing both mucosal damage AND the mechanical cause (sphincter dysfunction) of reflux disease.
Petrovic, Igor; Dobric, Ivan; Drvis, Petar; Shejbal, Drazen; Brcic, Luka; Blagaic, Alenka Boban; Batelja, Lovorka; Kokic, Neven; Tonkic, Ante; Mise, Stjepan; Baotic, Tomislav; Staresinic, Mario; Radic, Bozo; Jakir, Ana; Vuksic, Tihomir; Anic, Tomislav; Seiwerth, Sven; Sikiric, Predrag · Animal Study
RPEP-01178 · 2006Macrocyclic C5a antagonists achieved pharmacologically active transdermal penetration in rats, with measurable anti-inflammatory effects from topical application — establishing the feasibility of transdermal delivery for cyclic peptide anti-inflammatory drugs.
Proctor, Lavinia M; Woodruff, Trent M; Sharma, Prakirti; Shiels, Ian A; Taylor, Stephen M · Animal Study
RPEP-01179 · 2006GH secretagogue orexigenic effects were attenuated in aged rats and dogs, correlating with reduced hypothalamic GHS-R expression — age-related decline in receptor density blunts the appetite-stimulating side effect, potentially beneficial for elderly GHS therapy.
Rigamonti, Antonello E; Bonomo, Sara M; Scanniffio, Diego; Cella, Silvano G; Müller, Eugenio E · Animal Study
RPEP-01180 · 2006Testosterone administration inhibited GH secretagogue-stimulated GH release in both rats and dogs, likely through enhanced somatostatin tone, explaining the lack of synergy between testosterone and GH peptides and informing combination therapy design.
Rigamonti, Antonello E; Cella, Silvano G; Giordani, Claudio; Bonomo, Sara M; Giunta, Marialuisa; Sartorio, Alessandro; Muller, Eugenio · Animal Study
RPEP-01181 · 2006Thymosin alpha-1 activated IDO-mediated tryptophan catabolism in dendritic cells, establishing a regulatory environment with balanced inflammation/tolerance that promotes protective Th1 immunity while maintaining regulatory T-cell suppression — sophisticated immune programming.
Romani, Luigina; Bistoni, Francesco; Perruccio, Katia; Montagnoli, Claudia; Gaziano, Roberta; Bozza, Silvia; Bonifazi, Pierluigi; Bistoni, Giovanni; Rasi, Guido; Velardi, Andrea; Fallarino, Francesca; Garaci, Enrico; Puccetti, Paolo · In Vitro
RPEP-01183 · 2006The review establishes that peptides, polypeptides, and antibodies are the leading molecular classes among antiangiogenic compounds. Two landmark approvals are highlighted: tumor necrosis factor (TNF/Beromun) as the first peptide drug registered for regional cancer treatment via selective tumor vasculature disruption, and bevacizumab (Avastin), an anti-VEGF-A antibody, as the first systemic antiangiogenic drug with significant survival benefit in advanced colorectal cancer when combined with chemotherapy.
The broader landscape includes cytokines, chemokines, antibodies targeting vascular growth factors and their receptors, soluble receptor decoys, fragments derived from extracellular matrix proteins (endostatin, tumstatin, etc.), and small synthetic peptides — many of which were in clinical trials at the time of publication.
Rüegg, Curzio; Hasmim, Meriem; Lejeune, Ferdy J; Alghisi, Gian Carlo ·
RPEP-01186 · 2006Ghrelin inhibited pentagastrin-stimulated gastric acid secretion through GHS-R1a in rats, demonstrating that the appetite-stimulating hormone simultaneously protects the stomach from acid damage — an integrated eat-and-protect function.
Sibilia, V; Muccioli, G; Deghenghi, R; Pagani, F; De Luca, V; Rapetti, D; Locatelli, V; Netti, C · Animal Study
RPEP-01187 · 2006BPC-157 (Pliva clinical trial designations: PL-10, PLD-116, PL 14736) for IBD is supported by extensive animal data: heals colitis/esophagitis/gastric lesions, provides cytoprotection, reduces inflammation through NO and prostaglandin pathways, and maintains gut integrity across multiple models.
Sikiric, P; Seiwerth, S; Brcic, L; Blagaic, A B; Zoricic, I; Sever, M; Klicek, R; Radic, B; Keller, N; Sipos, K; Jakir, A; Udovicic, M; Tonkic, A; Kokic, N; Turkovic, B; Mise, S; Anic, T · Animal Study
RPEP-01188 · 2006Natriuretic peptides protect both heart and kidneys through integrated mechanisms: cardiac vasodilation and anti-remodeling combined with renal natriuresis, vasorelaxation, and GFR modulation — establishing the cardiorenal protective axis exploited by sacubitril/valsartan.
Silver, Marc A · Review
RPEP-01189 · 2006BPC-157 accelerated healing of transected quadriceps muscle in rats with improved functional recovery and histological organization compared to controls, demonstrating efficacy for major skeletal muscle injury repair beyond tendon healing.
Staresinic, Mario; Petrovic, Igor; Novinscak, Tomislav; Jukic, Ivana; Pevec, Damira; Suknaic, Slaven; Kokic, Neven; Batelja, Lovorka; Brcic, Luka; Boban-Blagaic, Alenka; Zoric, Zdenka; Ivanovic, Domagoj; Ajduk, Marko; Sebecic, Bozidar; Patrlj, Leonardo; Sosa, Tomislav; Buljat, Gojko; Anic, Tomislav; Seiwerth, Sven; Sikiric, Predrag · Animal Study