The novel peptide PEP-Z-2 potentially treats renal fibrosis in vivo and in vitro by regulating TGF-β/Smad/AKT/MAPK signaling.

Renal fibrosis is a process in which excessive deposition of extracellular matrix leads to an increase in tissue hardness and gradual destruction of the renal parenchyma. Chronic kidney disease (CKD) commonly progresses to end-stage renal disease (ESRD), ultimately leading to renal failure. This disease has high incidence and mortality rates, but to date, effective treatment options are lacking.

Beclin-1-Derived Peptide MP1 Attenuates Renal Fibrosis by Inhibiting the Wnt/-Catenin Pathway.

Renal fibrosis is distinguished by the abnormal deposition of extracellular matrix and progressive loss of nephron function, with a lack of effective treatment options in clinical practice. In this study, we discovered that the Beclin-1-derived peptide MP1 significantly inhibits the abnormal expression of fibrosis and epithelial-mesenchymal transition-related markers, including -smooth muscle actin, fibronectin, collagen I, matrix metallopeptidase 2, Snail1, and vimentin both in vitro and in vivo. H&E staining was employed to evaluate renal function, while serum creatinine (Scr) and blood urea nitrogen (BUN) were used as main indices to assess pathologic changes in the obstructed kidney.

Exploring the Dual Functions of Distal Acyl Group Direction in Various Nucleophilic Environments.

A universal glycosylation strategy could significantly simplify glycoside synthesis. One approach to achieving this goal is through acyl group direction for the corresponding 1,2-, 1,3-, 1,4-, or 1,6- glycosylation; however, this approach has been challenging for glycosidic bonds that require distal -acyl group direction. We developed an approach in weakly nucleophilic environments for selective 1,4- glycosylation directed by the -4--acyl group.

β-l-Rhamnosylation and β-d-Mannosylation Mediated by 4--Ester Groups in a Weakly Nucleophilic Environment.

-4--Acyl group directed β-rhamnosylation and β-mannosylation are achieved in a carborane or BARF anion formed weakly nucleophilic environment with the assistance of a 2,3-orthocarbonate group. The 4--acyl group plays a critical role in directing the β-selectivity, and the weakly coordinating anion is essential to amplify this direction. The orthocarbonate group could be readily removed with 1,3-propanediol in the presence of BF·EtO.

The CaMKII Inhibitory Peptide AIP Alleviates Renal Fibrosis Through the TGF-/Smad and RAF/ERK Pathways.

Renal fibrosis is characterized by the excessive deposition of extracellular matrix that destroys and replaces the functional renal parenchyma, ultimately leading to organ failure. It is a common pathway by which chronic kidney disease can develop into end-stage renal disease, which has high global morbidity and mortality, and there are currently no good therapeutic agents available. Calcium/calmodulin-dependent protein kinase II (CaMKII) has been indicated to be closely related to the occurrence of renal fibrosis, and its specific inhibitory peptide, autocamtide-2-related inhibitory peptide (AIP), was shown to directly bind the active site of CaMKII.

A novel and low-toxic peptide DR3penA alleviates pulmonary fibrosis by regulating the MAPK/miR-23b-5p/AQP5 signaling axis.

Pulmonary fibrosis (PF) is a pathological change caused by repeated injuries and repair dysfunction of the alveolar epithelium. Our previous study revealed that the residues Asn3 and Asn4 of peptide DR8 (DHNNPQIR-NH) could be modified to improve stability and antifibrotic activity, and the unnatural hydrophobic amino acids -(4-pentenyl)-Ala and d-Ala were considered in this study. DR3penA (DH-(4-pentenyl)-ANPQIR-NH) was verified to have a longer half-life in serum and to significantly inhibit oxidative damage, epithelial-mesenchymal transition (EMT) and fibrogenesis and .

DR7dA, a Novel Antioxidant Peptide Analog, Demonstrates Antifibrotic Activity in Pulmonary Fibrosis and .

Pulmonary fibrosis (PF), which is characterized by enhanced extracellular matrix (ECM) deposition, is an interstitial lung disease that lacks an ideal clinical treatment strategy. It has an extremely poor prognosis, with an average survival of 3-5 years after diagnosis. Our previous studies have shown that the antioxidant peptide DR8 (DHNNPQIR-NH), which is extracted and purified from rapeseed, can alleviate PF and renal fibrosis.

Peptide DR8 analogs alleviate pulmonary fibrosis via suppressing TGF-β1 mediated epithelial-mesenchymal transition and ERK1/2 pathway in vivo and in vitro.

Pulmonary fibrosis is a chronic progressive lung disease that lacks effective treatments in clinic. It is characterized by repair disorder of epithelial cells, formation of fibroblast foci as well as destruction of alveolar structure. Previously we first determined that parent peptide DR8 (DHNNPQIR-NH) has anti-fibrotic activity in bleomycin-induced mice.

Potent Antimicrobial and Antibiofilm Activities of Feleucin-K3 Analogs Modified by α-(4-Pentenyl)-Ala against Multidrug-Resistant Bacteria.

The dramatic increase in antimicrobial resistance (AMR) highlights an urgent need to develop new antimicrobial therapies. Thus, antimicrobial peptides (AMPs) have emerged as promising novel antibiotic alternatives. Feleucin-K3 is an amphiphilic α-helical nonapeptide that has powerful antimicrobial activity.

The antimicrobial peptide YD attenuates inflammation miR-155 targeting CASP12 during liver fibrosis.

The antimicrobial peptide APKGVQGPNG (named YD), a natural peptide originating from CBSYD1, exhibited excellent antibacterial and antioxidant properties . These characteristics are closely related to inflammatory responses which is the central trigger for liver fibrosis. However, the therapeutic effects of YD against hepatic fibrosis and the underlying mechanisms are rarely studied.

Feleucin-K3 Analogue with an α-(4-Pentenyl)-Ala Substitution at the Key Site Has More Potent Antimicrobial and Antibiofilm Activities and .

The development of antimicrobial compounds is now regarded as an urgent problem. Antimicrobial peptides (AMPs) have great potential to become novel antimicrobial drugs. Feleucin-K3 is an α-helical cationic AMP isolated from the skin secretion of the Asian bombinid toad species and has antimicrobial activity.

Peptide DR8 suppresses epithelial-to-mesenchymal transition via the TGF-β/MAPK signaling pathway in renal fibrosis.

Aims: Renal fibrosis is a progressive disease that leads to renal dysfunction and end-stage renal failure, and there is currently no specific treatment. Our previous study showed that the 8-residue peptide DR8 (DHNNPQIR) exhibits potent antioxidant and antifibrotic properties, and accumulating evidence suggests that oxidative stress contributes greatly to fibrosis. The effects and mechanisms of DR8 on renal fibrosis remain unknown.

CPF-C1 analog with effective antimicrobial and antibiofilm activities against Staphylococcus aureus including MRSA.

The evolution of Staphylococcus aureus (S. aureus) with the ability to acquire and develop resistance to antibiotics has been described as a distinct strain emergence event. Methicillin-resistant S.

Protective effect of peptide DR8 on bleomycin-induced pulmonary fibrosis by regulating the TGF-β/MAPK signaling pathway and oxidative stress.

Pulmonary fibrosis (PF) is a fatal and irreversible lung disease that eventually causes respiratory failure, lung dysfunction and death. The peptide DHNNPQIR-NH (DR8) has been reported to possess potent antioxidant activity, and an imbalance of oxidation/antioxidation is a crucial mechanism that causes PF. Here, we studied the ability of DR8 to improve PF and further explored the pathway in which DR8 plays a critical role.

p53 as a double-edged sword in the progression of non-alcoholic fatty liver disease.

Non-alcoholic fatty liver disease (NAFLD) derives from the accumulation of hepatic lipids, which leads to liver steatosis and then triggers non-alcoholic steatohepatitis, sometimes worsening to hepatic fibrosis, cirrhosis, and hepatocellular carcinoma. Although the molecular mechanisms of NAFLD have been intensively investigated, its pathogenesis remains poorly understood and needs to be clarified. Tumor-suppressor factor p53 has a crucial role in many signaling pathways that induce apoptosis and has become an emerging focus for liver disease research.

Potent effects of amino acid scanned antimicrobial peptide Feleucin-K3 analogs against both multidrug-resistant strains and biofilms of Pseudomonas aeruginosa.

Pseudomonas aeruginosa is particularly difficult to treat because it possesses a variety of resistance mechanisms and because it often forms biofilms. Antimicrobial peptides represent promising candidates for future templates of antibiotic-resistant bacterial infections due to their unique mechanism of antimicrobial action. In this study, we first found that the antimicrobial peptide Feleucin-K3 has potent antimicrobial activity against not only the standard strain of P.

Rapeseed protein-derived antioxidant peptide RAP alleviates renal fibrosis through MAPK/NF-κB signaling pathways in diabetic nephropathy.

Introduction: Kidney fibrosis is the main pathologic change in diabetic nephropathy (DN), which is the major cause of end-stage renal disease. Current therapeutic strategies slow down but cannot reverse the progression of renal dysfunction in DN. Plant-derived bioactive peptides in foodstuffs are widely used in many fields because of their potential pharmaceutical and nutraceutical benefits.

Novel antimicrobial peptide CPF-C1 analogs with superior stabilities and activities against multidrug-resistant bacteria.

As numerous clinical isolates are resistant to most conventional antibiotics, infections caused by multidrug-resistant bacteria are associated with a higher death rate. Antimicrobial peptides show great potential as new antibiotics. However, a major obstacle to the development of these peptides as useful drugs is their low stability.

Catalytic Asymmetric Michael Reaction of 5H-Oxazol-4-Ones with α,β-Unsaturated Acyl Imidazoles.

The asymmetric Michael reaction between 5H-oxazol-4-ones and α,β-unsaturated acyl imidazoles is reported. A novel 2-benzo[b]thiophenyl-modified chiral ProPhenol species is synthesized and used as a ligand, leading to good enantioselectivities in this asymmetric conjugate addition reaction. Furthermore, the introduction of phenol additives as achiral co-ligands is found to improve the reaction's chemical yields, diastereoselectivities, and enantioselectivities.

Catalytic Asymmetric [3 + 2] Cyclization Reactions of 3-Isothiocyanato Oxindoles and Alkynyl Ketones Via an in Situ Generated Magnesium Catalyst.

A highly enantioselective formal [3 + 2] cycloaddition reaction between 3-isothiocyanato oxindoles and alkynyl ketones is reported for the first time. An oxazoline-OH type chiral ligand derived from o-hydroxy-phenylacetic acid is employed to generate an effective magnesium catalyst in the current cyclization reaction and give serials of chiral spirooxindoles with good chemical yields and enantioselectivities.

Antimicrobial activities and action mechanism studies of transportan 10 and its analogues against multidrug-resistant bacteria.

The increased emergence of multidrug-resistant bacteria is perceived as a critical public health threat, creating an urgent need for the development of novel classes of antimicrobials. Cell-penetrating peptides that share common features with antimicrobial peptides have been found to have antimicrobial activity and are currently being considered as potential alternatives to antibiotics. Transportan 10 is a chimeric cell-penetrating peptide that has been reported to transport biologically relevant cargoes into mammalian cells and cause damage to microbial membranes.

Cell penetrating peptide TAT can kill cancer cells via membrane disruption after attachment of camptothecin.

Attachment of traditional anticancer drugs to cell penetrating peptides is an effective strategy to improve their application in cancer treatment. In this study, we designed and synthesized the conjugates TAT-CPT and TAT-2CPT by attaching camptothecin (CPT) to the N-terminus of the cell penetrating peptide TAT. Interestingly, we found that TAT-CPT and especially TAT-2CPT could kill cancer cells via membrane disruption, which is similar to antimicrobial peptides.

Design of novel analogues of short antimicrobial peptide anoplin with improved antimicrobial activity.

Currently, novel antibiotics are urgently required to combat the emergence of drug-resistant bacteria. Antimicrobial peptides with membrane-lytic mechanism of action have attracted considerable interest. Anoplin, a natural α-helical amphiphilic antimicrobial peptide, is an ideal research template because of its short sequence.

Antimicrobial activities and membrane-active mechanism of CPF-C1 against multidrug-resistant bacteria, a novel antimicrobial peptide derived from skin secretions of the tetraploid frog Xenopus clivii.

Hospital-acquired infections caused by multidrug-resistant bacteria pose significant challenges for treatment, which necessitate the development of new antibiotics. Antimicrobial peptides are considered potential alternatives to conventional antibiotics. The skin of Anurans (frogs and toads) amphibians is an extraordinarily rich source of antimicrobial peptides.

Dual antifungal properties of cationic antimicrobial peptides polybia-MPI: membrane integrity disruption and inhibition of biofilm formation.

With the increasing emergence of resistant fungi, the discovery and development of novel antifungal therapeutics were urgently needed. Compared with conventional antibiotics, the limited propensity of AMPs to induce resistance in pathogens has attracted great interest. In the present study, the antifungal activity and its mechanism-of-action of polybia-MPI, a cationic peptide from the venom of Social wasp Polybia Paulista was investigated.