RPEP-00694 · 2001Lacritin is a newly identified secreted glycoprotein that is highly expressed in human lacrimal gland, moderately in salivary glands, and slightly in thyroid, with no detectable expression in more than 50 other tissues examined.
Recombinant lacritin enhanced unstimulated (constitutive) secretion from lacrimal acinar cells in culture, promoted ductal cell proliferation, and stimulated signaling through tyrosine phosphorylation and calcium release in corneal epithelial cells. It binds several extracellular matrix proteins including collagen IV, laminin-1, and fibronectin. The lacritin gene maps to chromosome 12q13 and consists of five exons with no alternative splicing.
Sanghi, S; Kumar, R; Lumsden, A; Dickinson, D; Klepeis, V; Trinkaus-Randall, V; Frierson, H F; Laurie, G W ·
RPEP-00695 · 2001Prodynorphin knockout mice were viable and fertile with altered pain and reward responses, providing a definitive genetic tool for studying dynorphin's specific roles across pain, addiction, mood, and immune function.
Sharifi, N; Diehl, N; Yaswen, L; Brennan, M B; Hochgeschwender, U · Animal Study
RPEP-00696 · 2001BPC-157 at 10 μg/kg and 10 ng/kg IP produced anxiolytic effects comparable to diazepam in both the shock probe/burying test (reduced defensive burying) and light/dark test (increased light exploration) in rats.
Sikiric, P; Jelovac, N; Jelovac-Gjeldum, A; Dodig, G; Staresinic, M; Anic, T; Zoricic, I; Ferovic, D; Aralica, G; Buljat, G; Prkacin, I; Lovric-Bencic, M; Separovic, J; Seiwerth, S; Rucman, R; Petek, M; Turkovic, B; Ziger, T · Animal Study
RPEP-00697 · 2001BPC-157 attenuated cysteamine-induced colon and duodenal lesions, including in gastrectomized rats, demonstrating acid-independent healing and extending its protective effects to the entire gut.
Sikiric, P; Seiwerth, S; Grabarevic, Z; Balen, I; Aralica, G; Gjurasin, M; Komericki, L; Perovic, D; Ziger, T; Anic, T; Prkacin, I; Separovic, J; Stancic-Rokotov, D; Lovric-Bencic, M; Mikus, D; Staresinic, M; Aralica, J; DiBiaggio, N; Simec, Z; Turkovic, B; Rotkvic, I; Mise, S; Rucman, R; Petek, M; Sebecic, B; Ivasovic, Z; Boban-Blagaic, A; Sjekavica, I · Animal Study
RPEP-00698 · 2001The octanoyl modification on Ser3 stabilizes a turn structure in ghrelin's N-terminal active core (first 5 residues), explaining its essential role in receptor binding and activation at the structural level.
Silva Elipe, M V; Bednarek, M A; Gao, Y D · In Vitro
RPEP-00699 · 2001The GHS-R family includes the active GHS-R1a (ghrelin receptor, constitutively active) and the orphan GHS-R1b splice variant, with constitutive activity suggesting baseline signaling roles and inverse agonist therapeutic potential.
Smith, R G; Leonard, R; Bailey, A R; Palyha, O; Feighner, S; Tan, C; Mckee, K K; Pong, S S; Griffin, P; Howard, A · In Vitro
RPEP-00700 · 2001BPC-157 attenuated both intratracheal HCl-induced lung lesions and associated gastric damage in rats, demonstrating cytoprotective effects extending beyond the GI tract to the respiratory system.
Stancic-Rokotov, D; Slobodnjak, Z; Aralica, J; Aralica, G; Perovic, D; Staresinic, M; Gjurasin, M; Anic, T; Zoricic, I; Buljat, G; Prkacin, I; Sikiric, P; Seiwerth, S; Rucman, R; Petek, M; Turkovic, B; Kokic, N; Jagic, V; Boban-Blagaic, A · Animal Study
RPEP-00701 · 2001GH secretagogues simultaneously activate GHRH neurons and suppress somatostatin neurons in the hypothalamus, creating a dual accelerator-plus-brake-release mechanism for amplified GH secretion.
Tannenbaum, G S; Bowers, C Y · Animal Study
RPEP-00702 · 2001Plasma BNP correlated with soluble Fas (apoptosis marker) in CHF patients, and sFas independently predicted prognosis, establishing a link between natriuretic peptide signaling and cardiac programmed cell death.
Tsutamoto, T; Wada, A; Maeda, K; Mabuchi, N; Hayashi, M; Tsutsui, T; Ohnishi, M; Fujii, M; Matsumoto, T; Yamamoto, T; Takayama, T; Kinoshita, M · Cross Sectional
RPEP-00703 · 2001The neuroendocrine response to critical illness is biphasic (acute activation → chronic suppression), and therapeutic intervention must be phase-appropriate: GH secretagogues/TRH benefit the chronic phase but acute-phase augmentation may be harmful.
Van den Berghe, G · Review
RPEP-00704 · 2001Estrogen is the proximate sex steroid sustaining GH secretion across the human lifespan, modulating GHRP sensitivity, somatostatin withdrawal, and GH feedback through specific neuroendocrine mechanisms that decline with menopause.
Veldhuis, J D; Evans, W S; Bowers, C Y; Anderson, S · Review
RPEP-00705 · 2001IV ghrelin infusion in healthy humans increased subjective appetite ratings and food intake significantly, alongside GH stimulation, providing the first proof that ghrelin is a human hunger hormone.
Wren, A M; Seal, L J; Cohen, M A; Brynes, A E; Frost, G S; Murphy, K G; Dhillo, W S; Ghatei, M A; Bloom, S R · RCT
RPEP-00706 · 2001ICV anti-beta-endorphin increased acute phase formalin pain, anti-leu-enkephalin increased late inflammatory phase pain, and anti-dynorphin affected both phases, demonstrating peptide-specific roles in endogenous pain modulation.
Wu, H; Hung, K; Ohsawa, M; Mizoguchi, H; Tseng, L F · Animal Study
RPEP-00707 · 2001Small intestinal ADM mRNA and protein were significantly upregulated during polymicrobial sepsis, with the gut releasing ADM into portal circulation, establishing the intestine as a major source of circulating ADM during sepsis.
Zhou, M; Chaudry, I H; Wang, P · Animal Study
RPEP-00708 · 2001Anxiety patients showed accelerated enkephalin degradation, and Selank's anxiolytic effect correlated with inhibition of enkephalin-degrading enzymes, preserving endogenous opioid-mediated anxiety relief.
Zozulya, A A; Kost, N V; Yu Sokolov, O; Gabaeva, M V; Grivennikov, I A; Andreeva, L N; Zolotarev, Y A; Ivanov, S V; Andryushchenko, A V; Myasoedov, N F; Smulevich, A B · Clinical Trial
RPEP-00711 · 2002The ghrelin-GHS system is a multi-functional endocrine network with validated roles in GH regulation, appetite control, adiposity, and cardiovascular function, with therapeutic implications across multiple medical specialties.
Arvat, Emanuela; Broglio, Fabio; Aimaretti, Gianluca; Benso, Andrea; Giordano, Roberta; Deghenghi, Romano; Ghigo, Ezio · Review
RPEP-00712 · 2002Both acylated ghrelin and des-acyl ghrelin inhibited apoptosis in cardiomyocytes and endothelial cells via ERK1/2 and PI3K/Akt pathways, with des-acyl ghrelin's activity demonstrating GHS-R-independent cardiovascular protection.
Baldanzi, Gianluca; Filigheddu, Nicoletta; Cutrupi, Santina; Catapano, Filomena; Bonissoni, Sara; Fubini, Alberto; Malan, Daniela; Baj, Germano; Granata, Riccarda; Broglio, Fabio; Papotti, Mauro; Surico, Nicola; Bussolino, Federico; Isgaard, Jorgen; Deghenghi, Romano; Sinigaglia, Fabiola; Prat, Maria; Muccioli, Giampiero; Ghigo, Ezio; Graziani, Andrea · In Vitro
RPEP-00713 · 2002Native bovine lactoferrin and derived peptides (lactoferricin) inhibited HIV entry into cells, with positively charged proteins/peptides showing the strongest activity, supporting milk-derived compounds as natural antivirals.
Berkhout, Ben; van Wamel, Jeroen L B; Beljaars, Leonie; Meijer, Dirk K F; Visser, Servaas; Floris, René · In Vitro
RPEP-00715 · 2002Thymosin alpha-1 demonstrates clinical efficacy across hepatitis B, hepatitis C (with IFN), cancer (with chemo), and potentially HIV, with excellent tolerability and a favorable safety profile across all studied indications.
Billich, Andreas · Review
RPEP-00716 · 2002Argireline (Ac-EEMQRR-NH₂), a synthetic six-amino-acid peptide, reduced wrinkle depth by up to 30% in healthy women volunteers after 30 days of topical application at 10% concentration in an oil-in-water emulsion.
The peptide works by mimicking botulinum toxin's mechanism: it inhibits neurotransmitter release by interfering with the SNARE complex — the protein machinery that cells use to release chemical signals at nerve endings. While Argireline's inhibitory potency was similar to botulinum toxin type A, its overall efficacy was lower, as expected for a topical peptide versus an injected neurotoxin.
Critically, Argireline showed no oral toxicity in vivo and caused no primary skin irritation even at high doses, establishing it as a non-toxic alternative to botulinum toxin injections for cosmetic wrinkle reduction.
Blanes-Mira, C; Clemente, J; Jodas, G; Gil, A; Fernández-Ballester, G; Ponsati, B; Gutierrez, L; Pérez-Payá, E; Ferrer-Montiel, A · Clinical Trial
RPEP-00717 · 2002Ghrelin displays endocrine (GH release) and non-endocrine (appetite stimulation, adipogenesis, cardioprotection) activities, with cardiovascular protection mediated by both acyl and des-acyl forms — a multi-system metabolic hormone.
Broglio, Fabio; Arvat, Emanuela; Benso, Andrea; Papotti, Mauro; Muccioli, Giampiero; Deghenghi, Romano; Ghigo, Ezio · Review
RPEP-00718 · 2002Ghrelin acts as a multi-system metabolic regulator beyond GH release, with validated roles in appetite, energy balance, gastric motility, pancreatic function, cardiovascular regulation, and immune modulation through widely distributed receptors.
Broglio, Fabio; Arvat, Emanuela; Benso, Andrea; Gottero, Cristina; Prodam, Flavia; Granata, Riccarda; Papotti, Mauro; Muccioli, Giampiero; Deghenghi, Romano; Ghigo, Ezio · Review
RPEP-00719 · 2002Natriuretic peptides serve dual roles as sensitive cardiac biomarkers AND active cardiovascular protectors, with evidence supporting both diagnostic utility and therapeutic potential through their vasodilatory, natriuretic, and neurohormonal-suppressive actions.
Clerico, Aldo · Review
RPEP-00720 · 2002The review established several key findings about defensins in lung biology:
• Humans produce at least 10 defensin molecules — 6 alpha-defensins and 4 beta-defensins — that are structurally and functionally similar
• Defensins kill a broad spectrum of microorganisms while permitting little resistance development
• Many defensin peptides can neutralize lipopolysaccharide (LPS) effects on macrophages and reduce proinflammatory cytokine release, providing protection against septic shock
• Protegrin-1 (a pig-derived minidefensin) served as a template for iseganan, which was in phase III clinical trials for oral mucositis from chemotherapy
• Prospective uses included respiratory pathogen control in cystic fibrosis and prevention of ventilator-associated pneumonia
• Major technical hurdle: synthesizing large quantities of complexly folded defensin peptides at scale
Cole, Alexander M; Waring, Alan J ·
RPEP-00721 · 2002Cyclotides combine exceptional structural stability (thermal, enzymatic, chemical resistance) with sequence-tolerant scaffolding capability, enabling design of stable peptide drugs through grafting bioactive sequences into the cyclotide framework.
Craik, David J; Simonsen, Shane; Daly, Norelle L · Review
RPEP-00723 · 2002Expanded CRF peptide family including urocortins reveals distinct CRF1 (anxiety/depression) and CRF2 (stress coping/appetite/cardiovascular) receptor functions, enabling receptor-specific drug development.
Dautzenberg, Frank M; Hauger, Richard L · Review
RPEP-00724 · 2002Urotensin-II plasma levels and its gene expression in heart and blood vessels were unchanged in patients with congestive heart failure compared to healthy controls. The peptide levels did not differ across measurement sites (pulmonary artery, left ventricle, coronary sinus, or arm vein), and even when severe heart failure patients received vasodilator therapy that significantly improved their hemodynamics (cardiac index up 78%, wedge pressure down 55%), urotensin-II levels stayed flat over 24 hours.
Gene expression of the urotensin-II precursor in heart tissue and blood vessels was also no different between end-stage heart failure patients and controls with normal heart function.
Dschietzig, Thomas; Bartsch, Cornelia; Pregla, Rainer; Zurbrügg, Heinz Robert; Armbruster, Franz Paul; Richter, Christoph; Laule, Michael; Romeyke, Elfrun; Neubert, Charlotte; Voelter, Wolfgang; Baumann, Gert; Stangl, Karl · Clinical Observational
RPEP-00725 · 2002Bovine lactoferricin inhibited tumor growth in immunodeficient mice, proving a direct cytotoxic antitumor mechanism independent of immune system activation, likely through cancer cell membrane disruption.
Eliassen, Liv Tone; Berge, Gerd; Sveinbjørnsson, Baldur; Svendsen, John S; Vorland, Lars H; Rekdal, Øystein · Animal Study
RPEP-00726 · 2002Adrenomedullin acts as both a pro-inflammatory stress responder and an anti-inflammatory tissue protector during disease, with its dual nature and temporal dynamics determining whether it helps or harms at each stage.
Elsasser, Ted H; Kahl, Stas · Review
RPEP-00728 · 2002Beta-endorphin levels predicted blood pressure response to hyperventilation in hypertensives: high endorphin = BP decrease; low endorphin with high norepinephrine/dynorphin = BP increase — opioids modulate cardiovascular stress response.
Fontana, Fiorella; Bernardi, Pasquale; Spampinato, Santi; Toro, Rosanna Di; Bugiardini, Raffaele · Clinical Trial
RPEP-00729 · 2002Synthetic peptidyl GH secretagogues inhibited proliferation of human CALU-1 lung carcinoma cells that express high levels of GHS receptors, demonstrating antiproliferative rather than growth-promoting activity in this cancer type.
Ghè, Corrado; Cassoni, Paola; Catapano, Filomena; Marrocco, Tiziana; Deghenghi, Romano; Ghigo, Ezio; Muccioli, Giampiero; Papotti, Mauro · In Vitro
RPEP-00730 · 2002Novel macrocyclic amino acids that constrain peptides into beta-strand conformations were developed as protease inhibitor templates, showing application in antiviral drug design against HIV and HCV proteases.
Glenn, Matthew P; Pattenden, Leonard K; Reid, Robert C; Tyssen, David P; Tyndall, Joel D A; Birch, Christopher J; Fairlie, David P · In Vitro
RPEP-00731 · 2002Ghrelin mRNA was detected in stomach (highest), intestine, pancreas, kidney, and other tissues, while GHS-R1a and GHS-R1b showed distinct but overlapping tissue distributions across virtually all major human organs.
Gnanapavan, Sharmilee; Kola, Blerina; Bustin, Stephen A; Morris, Damian G; McGee, Patrick; Fairclough, Peter; Bhattacharya, Satya; Carpenter, Robert; Grossman, Ashley B; Korbonits, Márta · In Vitro
RPEP-00732 · 2002ANP, BNP, and CNP are expressed in the cardiac conduction system (SA node, AV node, His bundle, Purkinje fibers) and may directly modulate heart rhythm, conduction, and arrhythmia susceptibility.
Hansson, Magnus · Review
RPEP-00734 · 2002The arcuate nucleus integrates peripheral metabolic signals through distinct neuronal populations: ghrelin mimetic activated neurons separate from those responding to leptin and insulin, which showed overlapping activation patterns.
Hewson, Adrian K; Tung, Loraine Y C; Connell, David W; Tookman, Laura; Dickson, Suzanne L · Animal Study
RPEP-00735 · 2002Prostate cancer cells expressed ghrelin, GHS-R1a, and GHS-R1b (autocrine system), with biphasic proliferative response: low ghrelin concentrations slightly stimulated while higher concentrations inhibited cell growth.
Jeffery, P L; Herington, A C; Chopin, L K · In Vitro
RPEP-00736 · 2002CCK/CCK-A receptor dysfunction is implicated in gallbladder and pancreatic diseases, while gastrin/CCK-B receptor abnormalities may contribute to GI cancer development, positioning these peptide systems as therapeutic targets.
Jensen, Robert T · Review
RPEP-00737 · 2002Chronic ipamorelin treatment maintained somatotroph GH-releasing responsiveness without desensitization, though GHRH and somatostatin receptor expression were modulated — adaptive changes that preserved overall drug effectiveness.
Jiménez-Reina, L; Cañete, R; de la Torre, M J; Bernal, G · Animal Study
RPEP-00739 · 2002Opioid gene knockouts reveal distinct, non-redundant roles: enkephalins in analgesia and reward, beta-endorphin in stress analgesia and respiratory control, dynorphins in pain and emotional regulation — each family has a specific functional niche.
Kieffer, Brigitte L; Gavériaux-Ruff, Claire · Review
RPEP-00740 · 2002Self-assembling peptide hydrogels maintained chondrocyte phenotype, supported cell division, and promoted extracellular matrix production (GAG, type II collagen), demonstrating functional cartilage tissue formation in a peptide scaffold.
Kisiday, J; Jin, M; Kurz, B; Hung, H; Semino, C; Zhang, S; Grodzinsky, A J · In Vitro
RPEP-00741 · 2002Ghrelin is the only known circulating orexigenic hormone, with meal-related fluctuations and interactions with leptin, insulin, and hypothalamic neuropeptides integrating peripheral and central appetite regulation.
Kojima, Masayasu; Kangawa, Kenji · Review
RPEP-00742 · 2002Thymosin alpha-1 + famciclovir combination activated HBV-specific T-cell responses and achieved HBeAg seroconversion in some immune-tolerant chronic hepatitis B patients — a typically treatment-unresponsive population.
Lau, G K K; Nanji, A; Hou, J; Fong, D Y T; Au, W-S; Yuen, S-T; Lin, M; Kung, H-F; Lam, S-K · Clinical Trial
RPEP-00744 · 2002BNP correlated most strongly with NYHA heart failure classification and treatment response in outpatients, outperforming C-terminal ANP and N-terminal ANP as a monitoring biomarker.
Lee, Shang-Chiun; Stevens, Tracy L; Sandberg, Sharon M; Heublein, Denise M; Nelson, Susan M; Jougasaki, Michihisa; Redfield, Margaret M; Burnett, John C · Cross Sectional
RPEP-00745 · 2002Chronic HBV treatment should be individualized based on viral markers, liver status, and patient characteristics, with thymosin alpha-1 offering an immune-enhancing alternative/complement to antiviral drugs across different HBV subgroups.
Leung, Nancy · Review
RPEP-00746 · 2002Thymosin alpha-1 accelerated restoration of T-cell-mediated neutralizing antibody responses in immunocompromised hosts, demonstrating faster immune reconstitution through both immunomodulatory and direct intracellular mechanisms.
Li, Chun-lin; Zhang, Ting; Saibara, Toshiji; Nemoto, Yoshihisa; Ono, Masafumi; Akisawa, Naoaki; Iwasaki, Shinji; Maeda, Takashi; Onishi, Saburo · Animal Study
RPEP-00747 · 2002Endomorphin-1 and dynorphin A directly modulated alpha9/alpha10 nicotinic ACh receptors (not through opioid receptors), providing a molecular mechanism for opioid peptide modulation of auditory and vestibular function.
Lioudyno, M I; Verbitsky, M; Glowatzki, E; Holt, J C; Boulter, J; Zadina, J E; Elgoyhen, A B; Guth, P S · In Vitro
RPEP-00748 · 2002Pathological burn stress downregulated liver glucocorticoid receptors through inflammatory cytokine (TNF-α, IL-1, IL-6) action, explaining cortisol resistance and uncontrolled inflammation during severe trauma.
Liu, Du-hu; Su, Yong-ping; Zhang, Wei; Lou, Shu-fen; Ran, Xin-ze; Gao, Jing-sheng; Cheng, Tian-min · Animal Study
RPEP-00749 · 2002Adrenomedullin functions as a vasodilator, growth regulator, neurotransmitter, anti-inflammatory agent, and hormone modulator through CRLR/RAMP receptor complexes, with therapeutic implications across cardiovascular, inflammatory, and neoplastic diseases.
López, José; Martínez, Alfredo · Review
RPEP-00750 · 2002In a prospective study of 1,586 emergency department patients presenting with acute dyspnea, B-type natriuretic peptide (BNP) measured by bedside assay was more accurate than any historical finding, physical examination, or laboratory value for identifying congestive heart failure.
At a cutoff of 100 pg/mL, BNP had a diagnostic accuracy of 83.4%. At levels below 50 pg/mL, the negative predictive value was 96% — meaning very low BNP effectively rules out heart failure. Of the patients studied, 47% had heart failure, 49% had non-cardiac causes of dyspnea, and 5% had dyspnea from non-cardiac causes despite a history of left ventricular dysfunction. BNP added significant independent predictive power to other clinical variables in multivariate analysis.
Maisel, Alan S; Krishnaswamy, Padma; Nowak, Richard M; McCord, James; Hollander, Judd E; Duc, Philippe; Omland, Torbjørn; Storrow, Alan B; Abraham, William T; Wu, Alan H B; Clopton, Paul; Steg, Philippe G; Westheim, Arne; Knudsen, Catherine Wold; Perez, Alberto; Kazanegra, Radmila; Herrmann, Howard C; McCullough, Peter A ·
RPEP-00751 · 2002Thymosin alpha-1 significantly inhibited NMU-induced mammary carcinogenesis in Fisher rats, reducing both tumor incidence and multiplicity, demonstrating cancer prevention through immune enhancement.
Moody, Terry W; Tuthill, Cynthia; Badamchian, Mahnaz; Goldstein, Allan L · Animal Study