Browse more peptide research, methods and limitations.
Structural studies revealed two lactoferricin-derived peptides interact with model membranes differently: the more amphipathic variant penetrated deeper, correlating with stronger antimicrobial activity — providing structural basis for potency differences.
Nguyen, Leonard T; Schibli, David J; Vogel, Hans J · In Vitro
Protein preload before duodenal fat perfusion in healthy men amplified satiety, enhanced CCK/GLP-1 release, and reduced subsequent energy intake compared to fat alone — supporting strategic macronutrient sequencing for appetite management.
Oesch, Sibylle; Degen, Lukas; Beglinger, Christoph · RCT
Right ventricular overload independently contributed to BNP and ANP elevation in heart failure patients, demonstrating that natriuretic peptide levels reflect total biventricular cardiac stress — not just left ventricular dysfunction.
Passino, Claudio; Maria Sironi, Anna; Favilli, Brunella; Poletti, Roberta; Prontera, Concetta; Ripoli, Andrea; Lombardi, Massimo; Emdin, Michele · Clinical Trial
X-ray crystal structures of a high-affinity macrocyclic peptide mimetic bound to Grb2 SH2 domain revealed specific hydrogen bonds and hydrophobic contacts driving picomolar binding — providing the structural blueprint for optimizing this cancer drug scaffold.
Phan, Jason; Shi, Zhen-Dan; Burke, Terrence R; Waugh, David S · In Vitro
Glycosylation of opioid and other neuropeptides enhanced BBB penetration, metabolic stability, and analgesic potency after peripheral administration, establishing glycopeptides as a practical strategy for delivering peptide drugs to the brain.
Polt, Robin; Dhanasekaran, Muthu; Keyari, Charles M · Review
Ghrelin-leptin cross-talk through the brain-gut axis constitutes the core energy balance system, integrating with GLP-1, PYY, NPY, and melanocortin circuits — obesity results from disruption of this integrated network.
Popovic, Vera; Duntas, Leonidas H · Review
PYY3-36 reduces food intake through peripheral Y2 receptor-mediated hypothalamic appetite suppression, with clinical development challenges including dose-limiting nausea, route-dependent efficacy, and need for sustained-release formulations.
Renshaw, D; Batterham, R L · Review
S. aureus developed lactoferricin B resistance through serial passage with sub-MIC concentrations, involving membrane composition changes, but resistant strains showed reduced growth fitness — antimicrobial peptide resistance is achievable but costly for bacteria.
Samuelsen, Orjan; Haukland, Hanne H; Jenssen, Håvard; Krämer, Manuela; Sandvik, Kjersti; Ulvatne, Hilde; Vorland, Lars H · In Vitro
S. aureus small colony variants were naturally resistant to lactoferricin B, with resistance associated with altered cell membrane composition and metabolic state — identifying a clinically important bacterial subtype (found in chronic infections) that evades antimicrobial peptide killing.
Samuelsen, Orjan; Haukland, Hanne Husom; Kahl, Barbara C; von Eiff, Christof; Proctor, Richard A; Ulvatne, Hilde; Sandvik, Kjersti; Vorland, Lars H · In Vitro
Thymosin alpha-1-cBLyS fusion protein expressed in E. coli combined T-cell immune enhancement (thymosin alpha-1) with B-cell stimulation (BLyS), creating a dual-arm immunostimulatory molecule for potential comprehensive immunotherapy.
Shen, Qiong; Tian, Ruiyang; Ma, Wenzhe; Yuan, Qinsheng; Gong, Yi · In Vitro
Cystatin C, a small protein produced by all nucleated cells and filtered by the kidneys, proved to be a far stronger predictor of death and cardiovascular events in elderly people than the traditional kidney marker creatinine. Among 4,637 elderly community-dwelling participants followed for up to 9 years, higher cystatin C levels showed a clear dose-response relationship with all-cause mortality. Those in the highest cystatin C category (quintile 5c) had a 2.58-fold increased risk of death compared to the lowest quintile. The highest cystatin C concentration (≥1.29 mg/L) was independently associated with a 2.27-fold increased risk of cardiovascular death, a 1.48-fold increased risk of heart attack, and a 1.47-fold increased risk of stroke after adjusting for multiple variables. In contrast, the highest creatinine quintile was not independently associated with any of these three outcomes.
Shlipak, Michael G; Sarnak, Mark J; Katz, Ronit; Fried, Linda F; Seliger, Stephen L; Newman, Anne B; Siscovick, David S; Stehman-Breen, Catherine · Cohort
Thymosin alpha-1 activated peritoneal macrophages to tumoricidal phenotype with increased reactive oxygen species and nitric oxide production, enabling direct tumor cell killing — confirming thymosin alpha-1's macrophage activation as a consistent antitumor mechanism.
Shrivastava, Pratima; Singh, Sukh Mahendra; Singh, Nisha · Animal Study
Adolescent nicotine exposure produced lasting increases in CRF-like and NPY-like immunoreactivity in amygdala and hypothalamic stress regions in adult rats, correlating with increased anxiety — adolescent nicotine permanently alters brain stress peptide systems.
Slawecki, Craig J; Thorsell, Annika K; El Khoury, Aram; Mathé, Aleksander A; Ehlers, Cindy L · Animal Study
GH secretagogue development spans from GHRP-6 discovery through systematic optimization (hexarelin, GHRP-2, ipamorelin for selectivity; MK-677 for oral activity) to ghrelin identification as the natural ligand — two decades of reverse pharmacology driving clinical drug development.
Smith, Roy G · Review
Serial NT-proBNP and BNP measurements over 2 years post-MI in the OPTIMAAL trial substudy tracked cardiac recovery trajectory and predicted late cardiac events, supporting prolonged natriuretic peptide monitoring for post-infarction risk stratification.
Squire, Iain B; Ørn, Stein; Ng, Leong L; Manhenke, Cord; Shipley, Lorraine; Aarsland, Torbjorn; Dickstein, Kenneth · Cohort
High-dose endomorphin-1 anti-analgesia in ventral PAG was mediated by direct NMDA receptor activation, while endomorphin-2 worked through dynorphin A release → kappa/NMDA pathways — two endogenous mu-agonists producing pain through distinct mechanisms.
Terashvili, Maia; Wu, Hsiang-En; Leitermann, Randy J; Sun, Han-Sen; Clithero, Andrew D; Tseng, Leon F · Animal Study
The novel selective CRF1 agonist cortagine enabled clear dissection of CRF receptor roles: CRF1 activation drives anxiety/depression-like behavior while CRF2 activation promotes stress coping — precise tools for receptor-specific psychiatric drug development.
Todorovic, Cedomir; Jahn, Olaf; Tezval, Hossein; Hippel, Cathrin; Spiess, Joachim · Review
Children with anorexia nervosa demonstrated disrupted entero-insular axis responses: abnormal GLP-1, insulin, glucose, and gut peptide dynamics after meals compared to healthy controls — gut hormone dysfunction may perpetuate the disease beyond psychological factors.
Tomasik, Przemyslaw J; Sztefko, Krystyna; Starzyk, Jerzy; Rogatko, Iwona; Szafran, Zdzisław · Clinical Trial
Somatostatin subtype-2 receptor antagonist BIM-23627 partially reversed glucocorticoid-induced catabolism in rats by reducing somatostatin's GH-inhibitory tone, improving GH/IGF-1 axis activity and reducing muscle and bone loss from chronic steroids.
Tulipano, Giovanni; Rossi, Elena; Culler, Michael D; Taylor, John E; Bonadonna, Stefania; Locatelli, Vittorio; Cocchi, Daniela; Giustina, Andrea · Animal Study
Lactoferrampin's candidacidal activity was localized to a cluster of positively charged residues that interact electrostatically with negatively charged yeast membranes, with charge-reducing mutations eliminating activity — defining the minimal antifungal pharmacophore.
van der Kraan, Marieke I A; Nazmi, Kamran; Teeken, Afke; Groenink, Jasper; van 't Hof, Wim; Veerman, Enno C I; Bolscher, Jan G M; Nieuw Amerongen, Arie V · In Vitro
Transmission electron microscopy revealed lactoferrin-derived peptides disrupted C. albicans membranes through complete bilayer destruction and E. coli through pore-like lesions — visually distinct killing mechanisms for yeast versus bacteria.
van der Kraan, Marieke I A; van Marle, Jan; Nazmi, Kamran; Groenink, Jasper; van 't Hof, Wim; Veerman, Enno C I; Bolscher, Jan G M; Nieuw Amerongen, Arie V · In Vitro
Testosterone supplementation increased GH and IGF-1 in healthy older men through enhanced basal secretion but did not potentiate GHRP-2 or GHRH stimulation responses — testosterone and GH secretagogues work through independent, non-synergistic GH-axis pathways.
Veldhuis, Johannes D; Keenan, Daniel M; Mielke, Kristi; Miles, John M; Bowers, Cyril Y · RCT
Low pulse pressure independently predicted mortality in advanced chronic heart failure and was associated with higher BNP/NT-proBNP, identifying a combined hemodynamic-peptide risk profile for the highest-risk patients.
Voors, Adriaan A; Petrie, Colin J; Petrie, Mark C; Charlesworth, Andrew; Hillege, Hans L; Zijlstra, Felix; McMurray, John J; van Veldhuisen, Dirk J · Cohort
Patients with Crohn's disease of the ileum (small intestine) have a specific deficiency of alpha-defensin antimicrobial peptides (HD5 and HD6) produced by Paneth cells. This reduction was independent of how inflamed the tissue was — meaning the defensin drop isn't just a consequence of inflammation, but may be a cause of the disease. Critically, the defensin deficiency was specific to ileal Crohn's — it was not seen in Crohn's of the colon, ulcerative colitis, or pouchitis. Eight other Paneth cell products were unchanged or increased, making this a highly specific peptide deficiency. Transgenic mice with reduced HD5 levels (comparable to those in Crohn's patients) showed pronounced changes in gut microbiota, confirming that low defensin levels functionally alter the gut ecosystem.
Wehkamp, Jan; Salzman, Nita H; Porter, Edith; Nuding, Sabine; Weichenthal, Michael; Petras, Robert E; Shen, Bo; Schaeffeler, Elke; Schwab, Matthias; Linzmeier, Rose; Feathers, Ryan W; Chu, Hiutung; Lima, Heriberto; Fellermann, Klaus; Ganz, Tomas; Stange, Eduard F; Bevins, Charles L · Human Tissue Study
The tetrameric (four-copy) RGD peptide labeled with copper-64 showed significantly higher integrin binding affinity than monomeric or dimeric versions, likely due to a polyvalency effect. In mice with glioma xenografts, tumor uptake was rapid and high — 9.93 ± 1.05 %ID/g at 30 minutes — with slow washout (4.56 ± 0.51 %ID/g at 24 hours). Blood clearance was fast (0.21 %ID/g at 4 hours), and the probe was excreted mainly through the kidneys. Blocking experiments with excess RGD confirmed that tumor uptake was specifically mediated through integrin αvβ3. Dosimetry estimates suggested acceptable radiation exposure for potential human use, with an effective dose of 0.0164 mSv/MBq.
Wu, Yun; Zhang, Xianzhong; Xiong, Zhengming; Cheng, Zhen; Fisher, Darrell R; Liu, Shuang; Gambhir, Sanjiv S; Chen, Xiaoyuan ·
GH-releasing peptides in heart failure models improved cardiac contractility, reversed cachexia, suppressed stress hormones (norepinephrine, cortisol), and reduced cardiomyocyte apoptosis — quadruple mechanism benefit addressing four major heart failure components.
Xu, Xiang-Bin; Pang, Jin-Jiang; Cao, Ji-Min; Ni, Chao; Xu, Rong-Kun; Peng, Xiao-Zhong; Yu, Xiao-Xia; Guo, Shu; Chen, Meng-Chin; Chen, Chen · Animal Study
Serial changes in BNP, ANP, norepinephrine, and aldosterone after MI in the Val-HeFT RCT substudy predicted ventricular remodeling and clinical outcomes — neurohormonal trajectory (pattern over time) provided prognostic information beyond single baseline measurements.
Yan, Raymond T; White, Michel; Yan, Andrew T; Yusuf, Salim; Rouleau, Jean L; Maggioni, Aldo P; Hall, Christian; Latini, Roberto; Afzal, Rizwan; Floras, John; Masson, Serge; McKelvie, Robert S · RCT
BNP elevation combined with myocardial integrated backscatter echocardiography improved detection of cardiac sarcoidosis, with BNP reflecting myocardial inflammation-induced cardiac stress in this difficult-to-diagnose condition.
Yasutake, Hiroko; Seino, Yoshihiko; Kashiwagi, Mutsumi; Honma, Hiroshi; Matsuzaki, Tsuyako; Takano, Teruo · Cross Sectional
Antimicrobial peptides with dual spermicidal and microbicidal properties could serve as vaginal microbicide contraceptives — simultaneously preventing STIs (HIV, HSV, gonorrhea) and pregnancy through a single peptide-based topical product.
Yedery, R D; Reddy, K V R · Review
Met-enkephalin (OGF) through the OGFr receptor promoted differentiation of human cancer cells toward more mature phenotypes, reducing proliferative capacity — adding differentiation induction to its known growth-inhibitory anti-cancer mechanism.
Zagon, Ian S; McLaughlin, Patricia J · In Vitro
SS-31, a cell-permeable peptide targeting the inner mitochondrial membrane, prevented mitochondrial depolarization and apoptosis in neuronal cells exposed to oxidative stress — demonstrating precision subcellular peptide targeting for protecting the cell's energy source.
Zhao, Kesheng; Luo, Guoxiong; Giannelli, Serena; Szeto, Hazel H · In Vitro
PYY3-36 and GLP-1-mediated appetite suppression required proper mouse acclimatization and habituation to experimental conditions; non-acclimatized mice showed variable, unreliable anorectic responses — explaining conflicting literature results.
Abbott, C R; Small, C J; Sajedi, A; Smith, K L; Parkinson, J R C; Broadhead, L L; Ghatei, M A; Bloom, S R · Animal Study
Ghrelin directly excited ventral tegmental area (VTA) dopamine neurons and increased excitatory synaptic inputs while promoting food-seeking behavior — establishing the molecular neurocircuit linking the hunger hormone to the brain's reward/motivation system.
Abizaid, Alfonso; Liu, Zhong-Wu; Andrews, Zane B; Shanabrough, Marya; Borok, Erzsebet; Elsworth, John D; Roth, Robert H; Sleeman, Mark W; Picciotto, Marina R; Tschöp, Matthias H; Gao, Xiao-Bing; Horvath, Tamas L · Animal Study
CJC-1295 (long-acting GHRH analog with extended half-life through DPP-IV resistance) normalized pulsatile GH secretion and IGF-1 in GH-deficient rats with once-daily SC administration — practical sustained GH-axis restoration for potential clinical simplification.
Alba, Maria; Fintini, Danilo; Sagazio, Alessia; Lawrence, Betty; Castaigne, Jean-Paul; Frohman, Lawrence A; Salvatori, Roberto · Animal Study
A GH-releasing peptide binding both GHS-R and CD36 scavenger receptor upregulated sterol transporters (ABCA1, ABCG1) in macrophages, demonstrating GH peptides can modulate reverse cholesterol transport — linking GH secretagogues to cardiovascular lipid metabolism.
Avallone, Roberta; Demers, Annie; Rodrigue-Way, Amélie; Bujold, Kim; Harb, Diala; Anghel, Silvia; Wahli, Walter; Marleau, Sylvie; Ong, Huy; Tremblay, André · In Vitro
Linear amphipathic cationic antimicrobial peptides disrupt bacterial membranes through a detergent-like mechanism (carpet model) rather than specific pore formation, with antimicrobial potency governed by the same hydrophobic-charge balance as detergent activity.
Bechinger, Burkhard; Lohner, Karl · Review
Exubera was approved in 2006 as the first inhaled insulin and the first peptide hormone successfully delivered via the pulmonary route for clinical use. Clinical trials demonstrated that it was effective at controlling blood glucose, apparently safe, and preferred by patients compared to subcutaneous mealtime insulin injections. The review highlights that the lungs' rich vascularity, large surface area, and immunotolerant characteristics make them an ideal target for peptide delivery, overcoming the traditional barrier of poor bioavailability that had limited inhaled peptide drugs. The authors noted that Exubera could reduce injection burden for both type 1 and type 2 diabetes patients and encourage earlier insulin initiation.
Bellary, Srikanth; Barnett, Anthony H · Review
GH secretagogues effectively stimulated GH release in both young and old dogs, with maintained efficacy but quantitative age-related differences — supporting GH secretagogue therapeutic potential for age-related GH decline across species.
Bhatti, Sofie F M; Duchateau, Luc; Van Ham, Luc M L; De Vliegher, Sarne P; Mol, Jan A; Rijnberk, Ad; Kooistra, Hans S · Animal Study
BPC-157's protective effects against acute ethanol toxicity and chronic alcohol consumption were modulated by NO synthase inhibitor L-NAME, implicating the nitric oxide system as a mediating pathway in BPC-157's anti-alcohol therapeutic mechanism.
Boban-Blagaic, Alenka; Blagaic, Vladimir; Romic, Zeljko; Jelovac, Nikola; Dodig, Goran; Rucman, Rudolf; Petek, Marijan; Turkovic, Branko; Seiwerth, Sven; Sikiric, Predrag · Animal Study
GLP-1 and PYY3-36 progressively increased over months post-RYGB, with the rise correlating with reduced appetite and sustained weight loss — gut hormonal adaptation (not just restriction) explains bariatric surgery's long-term success.
Borg, C M; le Roux, C W; Ghatei, M A; Bloom, S R; Patel, A G; Aylwin, S J B · Cohort
Ghrelin's gastroprotective effect against ischemia-reperfusion injury was mediated through the prostaglandin/COX pathway, with COX inhibitors (indomethacin) blocking the protection — identifying the molecular mechanism for ghrelin's gastric mucosal defense.
Brzozowski, Tomasz; Konturek, Peter C; Sliwowski, Zbigniew; Pajdo, Robert; Drozdowicz, Danuta; Kwiecien, Slawomir; Burnat, Grzegorz; Konturek, Stanislaw J; Pawlik, Wieslaw W · Animal Study
Human beta-defensin-3 (hBD3) selectively damages bacterial membranes while leaving human cell membranes intact, and this selectivity is determined by the lipid composition of the target membrane. The peptide could only create lesions in membranes that resembled the outer membrane of susceptible bacteria (like E. coli and Salmonella), which contain negatively charged lipopolysaccharides. Membranes resembling resistant bacteria (like Proteus mirabilis) or human cells (with zwitterionic phospholipids) were not damaged. This explains both why hBD3 kills certain bacteria and why it doesn't harm human cells.
Böhling, Arne; Hagge, Sven O; Roes, Stefanie; Podschun, Rainer; Sahly, Hany; Harder, Jürgen; Schröder, Jens-Michael; Grötzinger, Joachim; Seydel, Ulrich; Gutsmann, Thomas · In Vitro
Rigorous binding and functional assays demonstrated adenosine does NOT activate GHS-R1a, contradicting two previous studies — the earlier reported adenosine-ghrelin receptor interaction was an experimental artifact, not a genuine physiological interaction.
Carreira, Marcos C; Camiña, Jesus P; Díaz-Rodríguez, Esther; Alvear-Perez, Rodrigo; Llorens-Cortes, Catherine; Casanueva, Felipe F · In Vitro
Lactoferricin-related peptides inhibited ACE-dependent vasoconstriction, adding blood pressure-lowering activity to the antimicrobial, anticancer, and immunomodulatory profile of this milk-derived peptide family.
Centeno, José M; Burguete, María C; Castelló-Ruiz, María; Enrique, María; Vallés, Salvador; Salom, Juan B; Torregrosa, Germán; Marcos, José F; Alborch, Enrique; Manzanares, Paloma · In Vitro
Comprehensive mapping of GI appetite hormones: ghrelin as the sole orexigenic signal; GLP-1, PYY3-36, oxyntomodulin, CCK, amylin, PP, and bombesin/GRP as anorexigenic signals — each acting through distinct receptors and pathways for integrated satiety control.
Chaudhri, Owais; Small, Caroline; Bloom, Steve · Review
Synthetic 20-amino-acid porcine lactoferricin peptide demonstrated broad-spectrum activity against gram-positive (S. aureus, Streptococcus) and gram-negative (E. coli) bacteria, validating porcine lactoferricin as another species source for antimicrobial peptide development.
Chen, Hsiao-Ling; Yen, Chih-Ching; Lu, Chien-Yu; Yu, Chia-Hen; Chen, Chuan-Mu · In Vitro
Updated cyclotide drug scaffold review covering recent advances: new grafting applications for diverse therapeutic targets, confirmed oral stability and bioavailability, expanded bioactivity profiles, and progress toward clinical macrocyclic peptide drugs.
Craik, David J; Cemazar, Masa; Daly, Norelle L · Review
GHRP-6 protected neurons from glutamate-induced excitotoxic death through survival signaling pathway activation, demonstrating direct GH-independent neuroprotection against the primary mechanism of stroke and neurodegenerative brain cell death.
Delgado-Rubín de Célix, Arancha; Chowen, Julie A; Argente, Jesús; Frago, Laura M · Animal Study
Intranasal bremelanotide (PT-141) significantly increased subjective sexual arousal, desire, and genital sensation in premenopausal women with sexual arousal disorder in a double-blind, placebo-controlled RCT — landmark evidence leading toward FDA approval for female sexual dysfunction.
Diamond, Lisa E; Earle, Dennis C; Heiman, Julia R; Rosen, Raymond C; Perelman, Michael A; Harning, Ronald · RCT
Semax upregulated BDNF mRNA and TrkB receptor expression in the rat hippocampus, providing the neurotrophic molecular mechanism for its documented cognitive enhancement and neuroprotective effects — BDNF is the brain's primary growth and survival factor.
Dolotov, Oleg V; Karpenko, Ekaterina A; Inozemtseva, Lyudmila S; Seredenina, Tamara S; Levitskaya, Natalia G; Rozyczka, Joanna; Dubynina, Elena V; Novosadova, Ekaterina V; Andreeva, Lyudmila A; Alfeeva, Lyudmila Yu; Kamensky, Andrey A; Grivennikov, Igor A; Myasoedov, Nikolay F; Engele, Jürgen · Animal Study