Research and News Archive

SPAAC Reactions
Joel P. Schneider, Yixin Xie, and Tania L. Lopez-Silva at the National Cancer Institute, report a new positively charged azidoamino acid for strain-promoted azide–alkyne cycloaddition...
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Human Serum Albumin
Human serum albumin, HSA, is the most abundant protein in human blood plasma. It plays a critical role in the native transportation of numerous drugs, metabolites, nutrients, and small molecules...
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Tyrosine Phosphorylation
The family of NF-κB transcriptional activators controls the expression of many genes, including those involved in cell survival and development. The family consists of...
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Pargamicin A
Researchers in the Del Valle Group, published in Organic Letters, report the total synthesis and configurational assignment of pargamicin A, a highly oxidized nonribosomal peptide...
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Glycan Biology
Glycan-binding proteins, GBPs, are widely used reagents for basic research and clinical applications. These reagents allow for the identification and manipulation of glycan determinants...
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Drug Candidate
In this article, published in Chemical Science, members of the James S. Nowick group show that the antibiotic teixobactin is a promising drug candidate...
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Stereoselectivity
In this article we show that stereoselective peptide catalysis is feasible in complex environments, including cell lysates...
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Anticancer Protein
Cancer is one of the leading causes of mortality in the world. Unfortunately, the present anticancer chemotherapeutics display high cytotoxicity...
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Peptides and Proteins
Transforming growth factor-β (TGF-β) plays important roles in wound healing. The activity of TGF-β is initiated upon the binding of the growth factor...
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Cyclic Peptides
The synthesis of large numbers of cyclic peptides─required, for example, in screens for drug development─is currently limited by the need of chromatographic...
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Ribosomal synthesis
Aromatic cyclic β2,3-amino acids (cβAAs), such as 2-aminobenzoic acid and 3-aminothiophene-2-carboxylic acid, are building blocks that can induce unique folding...
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PKC Disruptors
Protein Kinase C (PKC) is a member of the AGC subfamily of kinases and regulates a wide array of signaling pathways and physiological processes...
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“Imprint-and-Report” DCLs
Sensor arrays using synthetic receptors have found great utility in analyte detection, resulting from their ability to distinguish analytes based on differential signals via...
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Kinase inhibitors
Leucine-Rich Repeat Kinase 2 (LRRK2) is a large, multidomain protein with dual kinase and GTPase function that is commonly mutated in both familial and idiopathic...
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Protease Inhibitors
Aberrant levels of cathepsin L (Cts L), a ubiquitously expressed endosomal cysteine protease, have been implicated in many diseases such as cancer and diabetes...
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Antibacterial Hydrogels
Herein, it is demonstrated that a peptide derived from mussel foot protein-5, a key protein in mussel adhesion, displays antibacterial properties, a yet unreported...
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Protein Interactions
In plants, transcription of selfish genetic elements such as transposons and DNA viruses is suppressed by RNA-directed DNA methylation...
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Protein Mimic
Members of the Arora lab constructed a synthetic Sos protein mimic that engages the wild-type and oncogenic forms of nucleotide-bound Ras and modulates downstream kinase signaling...
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Rippled β-Sheet Motif
In this conspectus, the authors give an overview of the early history of the rippled β-sheet and provide a detailed structural description/definition of this motif...
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Cyclic Peptides
Despite recent success in computational design of structured cyclic peptides, de novo design of cyclic peptides that bind to any protein functional site remains difficult...
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Ion Channels
The design of peptides that assemble in membranes to form functional ion channels is challenging. Specifically, hydrophobic interactions must be...
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B-cell Epitope
Herein, researchers in the Kaumaya lab describe a novel PD-1 B-cell peptide epitope vaccine (amino acid 92–110; PD1-Vaxx) linked to a measles virus fusion peptide...
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Peptide Cancer Vaccines
In this article, Professor Pravin Kaumaya reviews his lab's approaches and strategies that focus on B-cell epitope cancer vaccines...
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Production Technology
The production of peptides as active pharmaceutical ingredients (APIs) by recombinant technologies is of emerging interest. A reliable production platform, however...
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Protein Synthesis
Chemical protein synthesis is a powerful avenue for accessing homogeneously modified proteins, but access to large targets has proved challenging...
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Peptide Libraries
Herein is described a divergent late-stage approach to generating macrocyclic peptide libraries with unnatural pharmacophores from readily available starting material...
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Peptide Synthesis
Despite six decades of efforts to synthesize peptides and proteins bearing multiple disulfide bonds, this synthetic challenge remains an unsolved problem...
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Peptide-Based Vaccines
In this Review, the authors discuss peptide-based vaccines and their potential in three therapeutic areas: infectious disease, Alzheimer’s disease, and cancer...
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Stapled Peptides
Diabetes is characterized by pancreas dysfunction and is commonly associated with obesity. Hypoglycemic agents capable of improving β-cell function...
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Protein-Protein Interactions
Herein is reported the first application of protein-observed fluorine (PrOF) NMR to the tandem bromodomains of BRD4 and BRDT to quantify the selectivity of their...
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Lariat Peptides
Many lariat peptide natural products exhibit interesting biological activities, and some, such as griselimycin and didemnin B, are membrane permeable...
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Endosomal Escape
Endocytic pathways are practical routes for the intracellular delivery of biomacromolecules. Along with this, effective strategies for endosomal cargo release...
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Oxime Ligation
The current review will focus on the authors’ use of peptide ligation to optimize PPI antagonists directed against several targets...
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Tyr-Lock Peptide
High-throughput screening for inhibitors of TDP1 activity resulted in the discovery of a new class of knotted cyclic peptides...
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DNA nanotechnology
DNA nanotechnology is an emerging field that promises fascinating opportunities for the manipulation and imaging of proteins on a cell surface...
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Cyclic Peptide Ligands
Herein is identified three cyclic peptide ligands of K-Ras(G12D) using an integrated in vitro translation−mRNA display selection platform...
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Peptidomimetic Uptake
Researchers in the Arora Lab observed that the cellular uptake of peptides is critically determined by the cell line-specifically, they noted that peptides show better uptake...
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Antimicrobial Synergy
Authors Chelcie Eller and Ron Raines find that human LL-37 and human RNase 1 can act synergistically to kill Gram-negative bacterial cells...
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Social Media Guide
An ACS editorial that provides scientists a guide to navigating and using social media to share ideas and enhance connections...
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Membrane-Lytic Peptides
Herein is described the use of peptide backbone N-methylation as a new strategy to transform membrane-lytic peptides (MLPs) into cytocompatible intracellular delivery vehicles...
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Frog-skin Peptides
In this study, the researchers investigated naturally occurring peptides derived from frog skin secretions for selectivity and activity toward melanocortin receptors...
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Flow SPPS
Flow‐based approaches to solid phase peptide synthesis (SPPS) have been pursued since the method's early days, with anticipated gains in...
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Bioorthogonal Conjugation
This minireview intends provides an up‐to‐date overview on the various bioorthogonal strategies implemented for the conjugation of transition organometallic entities...
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Coronavirus Inhibitors
The novel coronavirus disease COVID-19 that emerged in 2019 is caused by the virus SARS CoV-2 and named for its close genetic similarity to SARS CoV-1...
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Anti-infective Peptoids
This feature article highlights the progress that has been made towards the development of novel anti-infective peptoids...
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Targeting Malaria
Herein is a review of ongoing research aimed at developing constrained peptides targeting protein-protein interactions pertinent to malaria pathogenesis.
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Disrupt Ubiquitination
The ubiquitin–proteasome system (UPS) is a highly regulated protein disposal process critical to cell survival. Inhibiting the pathway induces proteotoxic stress and can be an effective cancer treatment.
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Cell Permeability
In a larger collaborative effort, these researchers have combined the strategies to identify the first examples of all-D α-helical stapled and stitched peptides.
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Peptide Hydrogels
Herein, a noninteracting multiphase molecular assembly approach is developed to crystallize tofacitinib, a potent JAK1/3 inhibitor, within a shearthinning self-assembled fibrillar peptide hydrogel network...
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Antimicrobial Peptides
Church et al. report a tunable chemical genetics approach for enhancing genetic code expansion in different wild-type bacterial strains..
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Protein Stability
Abundant n → π* interactions between adjacent backbone carbonyl groups are predicted to play an important role in dictating the structure of proteins...
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Modified Amino Acids
Herein, Wang et al. present a photoredox-catalyzed asymmetric method for the preparation of enantiopure β-thiolated/selenolated amino acids using a simple chiral auxiliary...
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Mapping SARS-CoV-2
Given the ongoing SARS-CoV-2 pandemic, identification of immunogenic targets against the coronavirus spike glycoprotein will provide crucial advances towards the development of diagnostic tools...
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COVID-19 Therapeutics
In this review, the researchers summarize peptide and peptide based therapeutics that target one main entry pathway of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)...
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Stapled Peptides
This colloborative work between the Garner and Kritzer labs shows their continued efforts to develop and characterization of a cell-penetrant lactam stapled peptide for targeting cellular eIF4E...
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Tyrosine Sulfation
Researchers at the University of Sydney have shown that the evasin protein ACA-01 from the Amblyomma cajennense tick can be posttranslationally sulfated at two tyrosine residues...
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Micelle-assisted Reactions
This publication shows that micelle-assisted reaction can facilitate native chemical ligations between a peptide-thioester and a Cys-peptide modified by a lipid-like moiety...
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Chemical Protein Synthesis
Herein is reported an operationally simple method to facilitate chemical protein synthesis by fully convergent and one-pot native chemical ligations...
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Targeting GPCRs
This recently published review discusses the current status of the peptide drugs targeting G protein-coupled receptors (GPCRs), with a focus on evolving strategies...
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β-Turn Mimics
Researchers report a simple reductive amination protocol to ligate two peptides, while simultaneously installing a β-turn mimic at the ligation junction...
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Fluorescent Peptide
Teixobactin is a nonribosomal antibiotic peptide that inhibits the biosynthesis of peptidoglycan and teichoic acid, however, teixobactin’s cellular site of action is unknown...
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Constrained Peptides
Guéret and colleagues describe a versatile method for inserting chiral motifs between the ends of omega loops. Peptides are synthesized using traditional SPPS...
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Coupling Agent Hazards
This case study of anaphylaxis induced by three uronium coupling agents, HATU, HBTU, and HCTU, is a cautionary note for researchers who handle peptide coupling agents frequently...
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Molecular Transporters
In this collaborative study, researchers have designed a new generation of peptides based on previously designed cyclic cell-penetrating peptides. They have evaluated their cytotoxicity as well as uptake behavior...
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C1B1 Inhibition
In this recent publication, Puhl et al. have employed random peptide phage display to screen and select peptides that bind to the calcium and integrin binding protein 1 (CIB1)...
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Aqueous SPPS
The growing interest in synthetic peptides has prompted the development of viable methods for their sustainable production. Currently, large amounts of toxic solvents are required for peptide assembly...
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Cyclotide Uptake
In this study, the recently developed chloroalkane penetration assay was combined with established assays to characterize the cellular uptake and cytosolic delivery of the prototypic cyclotide, kalata B1...
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Peptide Synthesis
In this recent Science publication, Hartrampf et al. report highly efficient chemistry matched with an automated fast-flow instrument for the direct manufacturing of peptide chains up to 164 amino acids long...
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Cyclotide Production
In this manuscript researchers in Dr. Craik's lab describe a strategy to improve the production of cyclotides, which are usually produced and cyclized synthetically at a high cost and environmental impact for large scale.
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Improved Thiol Protection
Photoremovable caging groups are useful for biological applications because the deprotection process can be initiated by illumination with light without the necessity of adding additional reagents...
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Peptide Self Assembly
Despite recent developments in two-dimensional self-assembly, most supramolecular 2D materials are assembled by tedious methodologies, with complex surface chemistry and small sizes...
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Peptide Mimics
Peptides have important biological functions. However, their susceptibility to proteolysis limits their applications...
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γ-Amino Acids Elongation
Because γ-amino acids generally undergo rapid self-cyclization upon esterification on the carboxyl group, for example, γ-aminoacyl-tRNA, there are no reports of the ribosomal elongation...
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Nanosheet Fabrication
Engineering free-standing 2D nanomaterials with compositional, spatial, and functional control across size regimes from the nano- to mesoscale represents a significant challenge....
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Hydrophobic Moieties
Trans amide bonds and fast cis–trans isomerization of Xaa-Pro bonds are crucial for the stability and folding rate of collagen, the most abundant protein in mammals...
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Platinum Nanoparticles
Hepatocellular carcinoma, HCC, is the sixth most frequent cancer and the second leading cause of death from cancer worldwide. Sorafenib is the most commonly used FDA‐approved systemic...
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Ice Nucleators
In a manuscript published in Langmuir, Yuki Kamijo and Ratmir Derda from the, University of Alberta, describe a screening system that employs the difference...
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Ghost Peptides
A major hurdle in chemical biology is the delivery of native proteins into the cytosol of mammalian cells. Published in ACS Chemical Biology, and presented...
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Octreotide Analogs
Somatostatin, SS, is a cyclic tetradecapeptide able to inhibit the release of growth hormone, GH, mainly through the binding to two G‐protein coupled...
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Enzyme Sequestration
Liquid-like droplets of biomacromolecules are emerging as a fundamental mechanism of cellular signaling, but designing synthetic mimics to form such...
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Short Peptides
Helical secondary and tertiary motifs are commonly observed as binding epitopes in natural and engineered protein scaffolds. While several strategies...
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Roads to Rome
Ribosomally synthesized and post-translationally modified peptides, RiPPs, are ubiquitous natural products. Bioactive RiPPs are produced from a precursor...
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Azapeptide Libraries
Aza‐propargylglycine, azaPra, peptides are branching points for the synthesis of azapeptide libraries. Researchers in the Lubell Lab, published in...
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Unprotected Peptides
Ring-closing metathesis, RCM, is an attractive reaction for the preparation of artificially designed peptides. Until now, RCM has been used for fully or partially protected...
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*Mar 23* Director, Peptide Chemistry, Reflexion Pharmaceuticals