RPEP-01253 · 2007Antimicrobial peptide selectivity for bacteria depends on preferential electrostatic binding to anionic bacterial membrane lipids (PG, CL) over zwitterionic human membrane lipids (PC, SM), with hydrophobic insertion depth determining killing efficiency — the molecular basis for therapeutic selectivity.
Lad, Mitaben D; Birembaut, Fabrice; Clifton, Luke A; Frazier, Richard A; Webster, John R P; Green, Rebecca J · In Vitro
RPEP-01255 · 2007Enhanced GLP-1 and PYY responses with suppressed ghrelin after RYGB mediated sustained appetite reduction and weight loss, with gut hormone changes persisting years post-surgery — establishing hormonal modification (not just restriction) as the primary mechanism of bariatric success.
le Roux, Carel W; Welbourn, Richard; Werling, Malin; Osborne, Alan; Kokkinos, Alexander; Laurenius, Anna; Lönroth, Hans; Fändriks, Lars; Ghatei, Mohammad A; Bloom, Stephen R; Olbers, Torsten · Clinical Trial
RPEP-01256 · 2007VIP suppressed Th17 cell differentiation and IL-17 production in autoimmune inflammation models, specifically targeting the pathogenic Th17 response that drives rheumatoid arthritis, EAE (MS model), and other autoimmune diseases — precision anti-autoimmune peptide therapy.
Leceta, Javier; Gomariz, Rosa P; Martinez, Carmen; Carrión, Mar; Arranz, Alicia; Juarranz, Yasmina · Animal Study
RPEP-01258 · 2007Rice protein hydrolysate (broken down rice protein) showed strong ACE-inhibiting activity in the lab (IC50 of 0.14 mg/ml) and significantly lowered systolic blood pressure in hypertensive rats after a single oral dose of 600 mg/kg.
Researchers isolated the specific peptide responsible: a four-amino-acid sequence Thr-Gln-Val-Tyr (TQVY). This purified peptide inhibited ACE with an IC50 of 18.2 μM and significantly lowered blood pressure in hypertensive rats at just 30 mg/kg — a 20-fold lower dose than the crude hydrolysate.
Li, Guan-Hong; Qu, Ming-Ren; Wan, Ju-Zhen; You, Jin-Ming · Animal Study
RPEP-01260 · 2007Fmoc-diphenylalanine self-assembled into nanofibrillar hydrogels supporting 3D cell culture with maintained viability and function, demonstrating that extremely simple dipeptides can create functional tissue engineering scaffolds through molecular self-organization.
Liebmann, Thomas; Rydholm, Susanna; Akpe, Victor; Brismar, Hjalmar · In Vitro
RPEP-01261 · 2007ApoAIV enhanced CCK-mediated satiety signaling for synergistic food intake reduction in rats, with the interaction involving CCK-A receptor pathways — demonstrating cooperation between lipid transport proteins and gut peptides for integrated appetite control.
Lo, Chun Min; Zhang, Dian Ming; Pearson, Kevin; Ma, Liyun; Sun, William; Sakai, Randall R; Davidson, W Sean; Liu, Min; Raybould, Helen E; Woods, Stephen C; Tso, Patrick · Animal Study
RPEP-01262 · 2007Systematic optimization produced novel GH secretagogue compounds with high nanomolar potency at the ghrelin receptor, improved pharmacological properties, and validated GH release in animal models — advancing the GH secretagogue drug pipeline.
Lu, Zhijian; Tata, James R; Cheng, Kang; Wei, Liente; Chan, Wanda W-S; Butler, Bridget; Schleim, Klaus D; Jacks, Thomas M; Hickey, Gerard; Patchett, Arthur A · Animal Study
RPEP-01263 · 2007Alpha-MSH-derived peptides (KPV, ACTH fragments) constitute a new anti-inflammatory drug class operating through NF-κB inhibition, regulatory T-cell induction, and melanocortin receptor-dependent/independent pathways — applicable to IBD, arthritis, allergic, and neuroinflammatory diseases.
Luger, Thomas A; Brzoska, Thomas · Review
RPEP-01265 · 2007GHRP-6 stimulation in ACTH-dependent Cushing's from lung carcinoid showed preserved GH response with ectopic ACTH source characteristics, demonstrating GH secretagogue testing utility for diagnosing ectopic versus pituitary ACTH production in Cushing's syndrome.
Machado, M C; Sá, S V; Goldbaum, T S; Catania, M; Campos, V C; Corrêa-Giannella, M L; Giannella-Neto, D; Salgado, L R · Case Report
RPEP-01266 · 2007Peripheral opioid analgesia from immune cell-derived peptides can be enhanced by: recruiting more opioid-producing leukocytes, increasing per-cell opioid release, or applying peripherally-restricted opioid agonists — achieving pain control without CNS side effects.
Machelska, Halina · Review
RPEP-01267 · 2007GI neuroendocrine satiety regulation integrates gut peptide signals (GLP-1, PYY, CCK, oxyntomodulin, ghrelin), enteric neural pathways, and central melanocortin/NPY circuits for comprehensive food intake control — gut peptide drugs leading the obesity treatment pipeline.
Maljaars, J; Peters, H P F; Masclee, A M · Review
RPEP-01268 · 2007Amidino-TAPA, a novel dermorphin tetrapeptide analog, produced antinociception partly mediated by endogenous opioid peptide release (confirmed by antiserum blocking), extending the drug-endogenous amplification mechanism to a new opioid drug class.
Mizoguchi, Hirokazu; Watanabe, Chizuko; Watanabe, Hiroyuki; Moriyama, Kaori; Sato, Bunsei; Ohwada, Keiko; Yonezawa, Akihiko; Sakurada, Tsukasa; Sakurada, Shinobu · Animal Study
RPEP-01269 · 2007Weight loss in overweight women modified gut hormone profiles: increased postprandial ghrelin (hunger) and reduced PYY satiety responses — hormonal changes that favor weight regain, explaining the biological basis of yo-yo dieting and weight loss plateau.
Moran, Lisa J; Noakes, Manny; Clifton, Peter M; Wittert, Gary A; Le Roux, Carel W; Ghatei, Mohammed A; Bloom, Stephen R; Norman, Robert J · Clinical Trial
RPEP-01270 · 2007By 2007, ghrelin receptor drug development included peptide agonists, peptidomimetics (MK-677, capromorelin), non-peptide agonists, inverse agonists, and biased ligands targeting GH deficiency, cachexia, gastroparesis, and obesity — the most diverse GPCR drug pipeline.
Moulin, Aline; Ryan, Joanne; Martinez, Jean; Fehrentz, Jean-Alain · Review
RPEP-01271 · 2007Second-generation trisubstituted triazole GHS-R ligands showed improved binding affinity, functional potency, and GH release in vivo compared to first-generation compounds — continued optimization of this novel non-peptide chemical class for GH secretagogue drug development.
Moulin, Aline; Demange, Luc; Bergé, Gilbert; Gagne, Didier; Ryan, Joanne; Mousseaux, Delphine; Heitz, Annie; Perrissoud, Daniel; Locatelli, Vittorio; Torsello, Antonio; Galleyrand, Jean-Claude; Fehrentz, Jean-Alain; Martinez, Jean · In Vitro
RPEP-01272 · 2007Thymosin alpha-1 synergizes with IFN-alpha, IFN-gamma, IL-2, and IL-12 to amplify T-cell, NK cell, and dendritic cell responses through complementary signaling pathways — explaining why combination therapy outperforms monotherapy for infections and cancer.
Naylor, Paul H; Quadrini, Karen; Garaci, Enrico; Rasi, Guido; Hadden, John W · Review
RPEP-01275 · 2007The appetite signaling chain: food → gut peptide release (GLP-1, PYY, CCK, ghrelin) → enteric nerve detection → vagal afferent transmission → brainstem integration (NTS) → hypothalamic processing (arcuate) → behavioral output — the complete food-to-decision neural-humoral pathway.
Näslund, Erik; Hellström, Per M · Review
RPEP-01276 · 2007Hydroxyproline-containing di- and tripeptides from orally ingested gelatin hydrolysate were detected in human plasma, with food-grade collagen hydrolysate producing higher peptide blood levels than gelatin — confirming oral collagen peptide bioavailability.
Ohara, Hiroki; Matsumoto, Hitoshi; Ito, Kyoko; Iwai, Koji; Sato, Kenji · Clinical Trial
RPEP-01277 · 2007Noopept (proline-containing dipeptide) restored spatial memory in brain-lesioned rats and increased hippocampal BDNF immunoreactivity, establishing BDNF upregulation as the neurotrophic mechanism for Noopept's cognitive-enhancing and neuroprotective activities.
Ostrovskaya, Rita U; Gruden, Marina A; Bobkova, Natalya A; Sewell, Robert D E; Gudasheva, Tatyana A; Samokhin, Alexander N; Seredinin, Sergey B; Noppe, Wim; Sherstnev, Vladimir V; Morozova-Roche, Ludmilla A · Animal Study
RPEP-01278 · 2007Thymosin alpha-1 activated IKK and p38 MAPK signaling pathways in immune cells, identifying these kinase cascades as the specific intracellular mediators of its immunostimulatory effects — molecular targets for optimizing thymosin alpha-1 therapy.
Peng, Xiao; Zhang, Ping; Wang, Xin; Chan, Justin; Zhu, Mingwei; Jiang, Meisheng; Tuthill, Cynthia; Wan, Yinsheng; Dragoi, Ana Maria; Chu, Wen-Ming · In Vitro
RPEP-01279 · 2007Bremelanotide activates female sexual function through MC3R/MC4R in hypothalamic/limbic sexual circuits, enhancing desire and arousal through dopaminergic and oxytocinergic pathway modulation — the comprehensive CNS mechanism supporting its clinical development for female HSDD.
Pfaus, James; Giuliano, François; Gelez, Hélène · Review
RPEP-01280 · 2007Thymosin beta 4 (Tβ4) promoted hair growth in multiple rat and mouse models, including a transgenic mouse that overexpresses Tβ4. The researchers identified the mechanism: Tβ4 stimulates follicle stem cell growth, migration, differentiation, and protease production. These are the same cellular processes Tβ4 is known to activate in wound healing — cell movement, new blood vessel formation, and tissue remodeling — applied specifically to hair follicle biology.
Philp, Deborah; St-Surin, Sharleen; Cha, Hee-Jae; Moon, Hye-Sung; Kleinman, Hynda K; Elkin, Michael · Animal Study
RPEP-01281 · 2007Comprehensive LC-MS profiling of O. affinis identified modified, linearized, and novel macrocyclic cyclotide variants beyond previously known members, revealing unexpected chemical diversity in a single plant species for expanded drug scaffold options.
Plan, Manuel Rey R; Göransson, Ulf; Clark, Richard J; Daly, Norelle L; Colgrave, Michelle L; Craik, David J · In Vitro
RPEP-01282 · 2007APP transgenic mice (an Alzheimer's model) treated with Cerebrolysin for 1 and 3 months showed a significant increase in BrdU-positive cells and doublecortin-positive neuroblasts in the hippocampal subgranular zone compared to vehicle-treated APP mice.
Cerebrolysin also decreased TUNEL-positive and activated caspase-3-positive neural progenitor cells, indicating reduced apoptosis (programmed cell death). Notably, the number of proliferating cells (PCNA-positive) was unchanged, and the ratio of cells converting into neurons versus astroglia stayed the same.
This pattern suggests Cerebrolysin doesn't increase the birth rate of new cells but rather keeps them alive longer by preventing apoptosis, effectively rescuing the neurogenesis deficit seen in these Alzheimer's model mice.
Rockenstein, Edward; Mante, Michael; Adame, Anthony; Crews, Leslie; Moessler, Herbert; Masliah, Eliezer ·
RPEP-01284 · 2007Thymosin alpha-1 uniquely balances immune activation (pathogen defense via TLR-mediated Th1 enhancement) with immune tolerance (autoimmune prevention via IDO-mediated Treg generation) — an endogenous immune calibrator, not just a simple immune booster.
Romani, Luigina; Bistoni, Francesco; Montagnoli, Claudia; Gaziano, Roberta; Bozza, Silvia; Bonifazi, Pierluigi; Zelante, Teresa; Moretti, Silvia; Rasi, Guido; Garaci, Enrico; Puccetti, Paolo · Review
RPEP-01285 · 2007Quinazolinone ghrelin receptor antagonists showed oral bioavailability, reduced food intake, and improved glucose tolerance in animal models — positioning orally active ghrelin blockade as a dual-mechanism drug approach for treating both diabetes and obesity simultaneously.
Rudolph, Joachim; Esler, William P; O'connor, Stephen; Coish, Philip D G; Wickens, Philip L; Brands, Michael; Bierer, Donald E; Bloomquist, Brian T; Bondar, Georgiy; Chen, Libing; Chuang, Chih-Yuan; Claus, Thomas H; Fathi, Zahra; Fu, Wenlang; Khire, Uday R; Kristie, James A; Liu, Xiao-Gao; Lowe, Derek B; McClure, Andrea C; Michels, Martin; Ortiz, Astrid A; Ramsden, Philip D; Schoenleber, Robert W; Shelekhin, Tatiana E; Vakalopoulos, Alexandros; Tang, Weifeng; Wang, Lei; Yi, Lin; Gardell, Stephen J; Livingston, James N; Sweet, Laurel J; Bullock, William H · Animal Study
RPEP-01286 · 2007In a head-to-head comparison of 428 patients with glucocorticoid-induced osteoporosis, the peptide drug teriparatide increased lumbar spine bone density by 7.2% over 18 months, compared to 3.4% with the bisphosphonate alendronate (p<0.001). The difference was already significant by 6 months.
Most strikingly, teriparatide dramatically reduced new vertebral fractures: only 0.6% of teriparatide patients suffered a new vertebral fracture versus 6.1% of alendronate patients (p=0.004) — a 10-fold difference. Nonvertebral fracture rates were similar between groups. Teriparatide did cause more elevated calcium levels as a side effect.
Saag, Kenneth G; Shane, Elizabeth; Boonen, Steven; Marín, Fernando; Donley, David W; Taylor, Kathleen A; Dalsky, Gail P; Marcus, Robert · Randomized Controlled Trial
RPEP-01287 · 2007MAX1 beta-hairpin peptide hydrogel demonstrated inherent broad-spectrum antibacterial activity against gram-positive and gram-negative bacteria through its cationic amphipathic surface structure — a self-sterilizing wound dressing biomaterial requiring no added antibiotic agents.
Salick, Daphne A; Kretsinger, Juliana K; Pochan, Darrin J; Schneider, Joel P · In Vitro
RPEP-01288 · 2007Melanocortin agonists (bremelanotide, melanotan II) treat sexual dysfunction in both sexes through central MC3R/MC4R activation: ED in men and HSDD/FSAD in women — the only drug class targeting desire/arousal centrally for both genders.
Shadiack, Annette M; Sharma, Shubh D; Earle, Dennis C; Spana, Carl; Hallam, Trevor J · Review
RPEP-01289 · 2007The BNP/ANP ratio correlated better with mitral regurgitation severity than either peptide alone, with the ratio reflecting the disproportionate ventricular stress from volume overload — a refined biomarker approach for valvular heart disease assessment.
Shimamoto, Ken; Kusumoto, Miyako; Sakai, Rieko; Watanabe, Hirota; Ihara, Syunichi; Koike, Natsuka; Kawana, Masatoshi · Cross Sectional
RPEP-01290 · 2007Ghrelin receptor agonists demonstrate multi-system anti-aging potential: restoring GH/IGF-1 axis, improving body composition (lean mass/fat ratio), enhancing cardiac function, boosting immune competence, and supporting cognitive function in aging models — comprehensive geroscience intervention.
Smith, Roy G; Sun, Yuxiang; Jiang, Hong; Albarran-Zeckler, Rosie; Timchenko, Nikolai · Review
RPEP-01291 · 2007The endocannabinoid system modulates appetite through gut-brain signaling interactions with CCK, GLP-1, ghrelin, and leptin, regulating food intake via vagal afferents and hypothalamic circuits — explaining cannabis appetite effects and informing cannabinoid-gut peptide drug combinations.
Storr, Martin A; Sharkey, Keith A · Review
RPEP-01294 · 2007Adrenomedullin maintains endothelial barrier integrity through Rac1-mediated adherens junction stabilization, preventing vascular leak during inflammation — the molecular basis for AM's protective role in sepsis and for AM-targeting therapy (adrecizumab) development.
Temmesfeld-Wollbrück, Bettina; Hocke, Andreas C; Suttorp, Norbert; Hippenstiel, Stefan · Review
RPEP-01295 · 2007SS-31 (mitochondria-targeted peptide) prevented mitochondrial depolarization and apoptosis in pancreatic islet cells, preserved glucose-stimulated insulin secretion, and improved glycemic control in diabetic animals — protecting the beta-cells that diabetes progressively destroys.
Thomas, Dolca A; Stauffer, Craig; Zhao, Kesheng; Yang, Hua; Sharma, Vijay K; Szeto, Hazel H; Suthanthiran, Manikkam · Animal Study
RPEP-01296 · 2007Multimerized fusion expression of lactoferricin derivative LfcinB15-W4,10 in E. coli achieved increased recombinant peptide yield through multiple tandem copies per fusion protein — a scalable manufacturing approach for commercial antimicrobial peptide production.
Tian, Zi-Gang; Teng, Da; Yang, Ya-Lin; Luo, Jin; Feng, Xing-Jun; Fan, Ying; Zhang, Fan; Wang, Jian-Hua · In Vitro
RPEP-01298 · 2007Ghrelin analog BIM-28125 partially reversed methylprednisolone-induced growth suppression in rats, increasing body weight gain and longitudinal bone growth during concurrent steroid treatment — supporting ghrelin-based therapy for steroid-treated children's growth.
Tulipano, Giovanni; Taylor, John E; Halem, Heather A; Datta, Rakesh; Dong, Jesse Z; Culler, Michael D; Bianchi, Irene; Cocchi, Daniela; Giustina, Andrea · Animal Study
RPEP-01300 · 2007Peripheral ER-alpha activation selectively altered GH secretory burst waveform (mass, amplitude, duration) without changing overall GH output in women — demonstrating estrogen modulates the QUALITY of GH release, not just quantity, with functional implications for GH bioactivity.
Veldhuis, Johannes D; Keenan, Daniel M; Bowers, Cyril Y · Clinical Trial
RPEP-01301 · 2007Controlled E2 repletion demonstrated tripartite estrogen regulation of GH secretion: enhanced GH secretagogue (GHRP) pathway sensitivity, reduced somatostatin inhibition, and modified GH autonegative feedback — three independent estrogen-GH control mechanisms confirmed.
Veldhuis, Johannes D; Cosma, Mihaela; Erickson, Dana; Paulo, Remberto; Mielke, Kristi; Farhy, Leon S; Bowers, Cyril Y · Clinical Trial
RPEP-01302 · 2007BPC-157 in IBD clinical trials supported by expanded animal evidence: heals colitis/fistulas/strictures, modulates NO and prostaglandin systems, promotes angiogenesis, and shows cytoprotection across multiple GI inflammation models — updated pre-clinical support for advancing clinical development.
Vuksic, Tihomir; Zoricic, Ivan; Brcic, Luka; Sever, Marko; Klicek, Robert; Radic, Bozo; Cesarec, Vedran; Berkopic, Lidija; Keller, Neike; Blagaic, Alenka Boban; Kokic, Neven; Jelic, Ivan; Geber, Juraj; Anic, Tomislav; Seiwerth, Sven; Sikiric, Predrag · Animal Study
RPEP-01303 · 2007Bovine lactoferricin expressed in Pichia methanolica yeast retained antimicrobial activity after purification, establishing methylotrophic yeast as a eukaryotic expression platform for commercial-scale antimicrobial peptide manufacturing.
Wang, Haikuan; Zhao, Xinhuai; Lu, Fuping · In Vitro
RPEP-01304 · 2007Acidic partner-mediated tandem gene fusion in E. coli achieved high-level antimicrobial peptide expression with retained bioactivity after cleavage — a practical manufacturing approach for commercial-scale antimicrobial peptide production.
Wang, Yun-Qi; Cai, Ji-Ye · In Vitro
RPEP-01306 · 2007Two neuropeptides — Substance P (SP) and CGRP — work together to drive airway inflammation. After ozone exposure in guinea pigs, both SP and CGRP increased with the same timing and location pattern, with a strong correlation between their expression levels.
Critically, CGRP was shown to upregulate the Substance P receptor (NK-1R) at both mRNA and protein levels in lung tissue. This means CGRP doesn't just cause inflammation on its own — it amplifies Substance P's inflammatory effects by increasing the number of receptors SP can activate. This upregulation was mediated through PKA, Calmodulin-dependent Kinase, and Tyrosine Protein Kinase pathways.
Wu, Hong; Guan, Chaxiang; Qin, Xiaoqun; Xiang, Yang; Qi, Mingming; Luo, Ziqiang; Zhang, Changqing · Preclinical
RPEP-01307 · 2007Gastric/intestinal electrical stimulation modulated local expression of appetite peptides (ghrelin, CCK, PYY) in the gut wall of obese rats, demonstrating that neurostimulation devices directly reprogram local gut peptide production for appetite modification.
Xu, Junying; McNearney, Terry A; Chen, Jiande D Z · Animal Study
RPEP-01308 · 2007Opioid peptides modulated cancer cell migration, chemotaxis, invasion, and adhesion in a peptide-type and cancer-type dependent manner, suggesting the opioid system influences metastatic behavior — with implications for opioid drug use in cancer patients.
Zagon, Ian S; Rahn, Kristen A; McLaughlin, Patricia J · In Vitro
RPEP-01309 · 2007Post-mortem pericardial ANP and BNP levels differentiated cardiac from non-cardiac death causes in medico-legal autopsies, with BNP showing the best discrimination — establishing natriuretic peptides as forensic biomarkers for cardiac function assessment at death.
Zhu, Bao-Li; Ishikawa, Takaki; Michiue, Tomomi; Li, Dong-Ri; Zhao, Dong; Tanaka, Sayaka; Kamikodai, Yasunobu; Tsuda, Kohei; Okazaki, Shuji; Maeda, Hitoshi · Cross Sectional
RPEP-01312 · 2008Intranasal oxytocin in healthy men increased trust behavior AND prevented trust adaptation (trust reduction) after betrayal in a social investment game, shaping the neural circuitry of both trust formation and trust resilience — with implications for social anxiety and autism.
Baumgartner, Thomas; Heinrichs, Markus; Vonlanthen, Aline; Fischbacher, Urs; Fehr, Ernst · RCT
RPEP-01313 · 2008Post-meal fullness involves two phases: satiation (meal termination via vagal mechanoreception + CCK) and sustained satisfaction (inter-meal fullness via GLP-1, PYY, insulin, leptin) — distinguishing the immediate fullness signal from prolonged appetite suppression for targeted drug development.
Berthoud, H-R · Review
RPEP-01314 · 2008Endogenous opioid peptides regulate HPA axis stress reactivity through hypothalamic CRF and ACTH modulation, with opioid system disruption producing altered cortisol responses — explaining stress hormone dysregulation in chronic pain, addiction, and stress disorders.
Bilkei-Gorzo, Andras; Racz, Ildiko; Michel, Kerstin; Mauer, Daniela; Zimmer, Anne; Klingmüller, Dietrich; Zimmer, Andreas · Animal Study
RPEP-01315 · 2008GHS-R1a pharmacological tools (agonists, antagonists, inverse agonists) revealed the receptor controls both GH secretion and feeding behavior, with receptor modification studies suggesting these functions may be partially separable for therapeutic benefit.
Bresciani, E; Tamiazzo, L; Torsello, A; Bulgarelli, I; Rapetti, D; Caporali, S; Perrissoud, D; Moulin, A; Fehrentz, J A; Martinez, J; Locatelli, V · Review
RPEP-01317 · 2008LL-37 activated migration of HaCaT human keratinocytes through multiple mechanisms: phenotypic changes in actin dynamics, increased tyrosine phosphorylation of focal adhesion kinase (FAK) and paxillin, induction of Snail and Slug transcription factors (associated with cell motility), activation of matrix metalloproteinases, and engagement of MAPK and PI3K/Akt signaling pathways.
These effects were mediated through both EGFR transactivation and induction of the FPRL-1 G-protein-coupled receptor. In vivo, adenoviral delivery of LL-37 to excisional wounds in ob/ob diabetic mice significantly improved re-epithelialization and granulation tissue formation — demonstrating that LL-37's wound healing benefits translate from cell culture to a clinically relevant impaired-healing animal model.
Carretero, Marta; Escámez, María J; García, Marta; Duarte, Blanca; Holguín, Almudena; Retamosa, Luisa; Jorcano, Jose L; Río, Marcela Del; Larcher, Fernando ·