Peptide Publications Archive
Showing items in Cyclic Peptides · Clear filter
Silencing the Warhead
Derda Lab
Covalent genetically encoded peptide libraries hold enormous promise for discovering irreversible inhibitors, but installing reactive electrophilic warheads under basic conditions causes those warheads to quench …
Expanding Cyclic Space
Duan Lab
Designing cyclic peptides that incorporate non-canonical amino acids against dynamic protein interfaces is a compelling strategy, but the combinatorial explosion of sequence space makes structure-guided …
Mapping Macrocycle Motion
Sun & Yudin Labs
Conventional NMR methods force dynamic macrocycles into a single averaged structure, obscuring the multiple conformers that govern permeability and activity. A new integrative framework combining …
Degraders Beat Hypoxia
Tavassoli Lab
Conventional PROTACs rely on small-molecule warheads, leaving protein–protein interaction targets beyond reach. By converting a cyclic peptide HIF-1α inhibitor into a VHL-recruiting degrader, researchers uncovered …
Bicyclic Kinase Trap
Suga Lab
Bicyclic peptides that incorporate a thioisoindole bridge offer tighter conformational constraint than standard macrocycles, yet building them fast enough to work inside a high-throughput mRNA …
Choosing Conformations
Yudin Lab
Macrocyclic peptides can fold into multiple conformations, but chemists have lacked a reliable chemical handle for selecting one over another. A late-stage lactone-opening reaction now …
Cycling on Bacteria
Tharp Lab
Cell-surface display of cyclic peptide libraries offers a fluorescence-sortable alternative to phage display, but generating stable macrocycles directly on living bacteria has resisted clean, bioorthogonal …
Electrochemical Biaryl Stapling
Hugh Nakamura Lab
Biaryl-bridged cyclic peptides from ribosomally synthesized and post-translationally modified peptides offer compelling drug-like properties, yet their rigid ring systems have made systematic analog synthesis almost …
Boronic Glycan Hunters
Suga Lab
Glycans drive cancer progression yet resist the synthetic binders that proteins attract so readily. A new platform combining genetic code reprogramming with mRNA display now …
Tuning Integrin Selectivity
Wang and Hu Lab
RGD peptides have long struggled to distinguish between closely related integrin subtypes, limiting their diagnostic precision. A new conformational tuning strategy, varying cross-linker length and …
Aldehyde Backbone Bending
Suga Lab
α-Amino-γ-lactam residues impose backbone constraints that can boost membrane permeability, yet no method existed for installing them post-translationally inside a display system. Now, an aldehyde-triggered …
Stapling With PMDA
Zhang and Li Groups
Peptide stapling typically demands exotic amino acids, cysteine handles, or metal catalysts, each carrying trade-offs in selectivity or modularity. A new pyromellitic dianhydride linker sidesteps …
Mushroom Toxins Decoded
Süssmuth Lab
Cortinarins are bicyclic peptides from toxic Cortinarius mushrooms that have resisted independent biological study for decades. A new total synthesis now unlocks milligram quantities of …
Tricycles from Display
Jongkees Lab
Tricyclic peptides offer tighter binding, better selectivity, and longer serum lifetimes than simpler macrocycles, but generating single regioisomers at the high dilution of mRNA display …
Light-Forged Macrocycles
Scanlan & Muttenthaler Labs
A photochemical thiol–yne reaction cyclizes neuropeptides under mild conditions, swapping the vulnerable disulfide bridge for a stable vinyl sulfide. One resulting oxytocin analogue proves more …
Wnt5a Competitor
Suga Lab
Diffuse intrinsic pontine glioma, DIPG, kills most children within two years of diagnosis and resists virtually every treatment tried so far. Now, a macrocyclic peptide …
Integrity Shapes Selection
Hampton and Liu labs
When a protein target is tethered to a solid support for phage display, does the immobilization chemistry matter? Researchers at Texas A&M engineered three structurally …
Peptide Reveals Oligomers
Gandy, Arancio, Ehrlich, Guérin, Lubell, and Rahimipour Labs
A multi-institutional team supervised jointly by Sam Gandy, Ottavio Arancio, and Michelle Ehrlich, published in Alzheimer's Dement., turned a designed cyclic D,L-α-peptide into a …
Locking Out RAS
Therrien Lab
Resistance to approved RAS inhibitors emerges rapidly in patients, driven by secondary mutations at the Switch-II and cyclophilin-A binding pockets. A team at Université de …
Yeast Finds Inhibitors
Angelini Lab
Yeast display technology, long used to evolve antibodies, can now rapidly surface macrocyclic peptide inhibitors of human angiotensin-converting enzyme 2 with potencies in the low-nanomolar …
Chameleonic Proline Rings
Palma Lab
A new family of all-peptide macrocycles built from alternating L- and D-proline tetramers flips between two distinct conformations depending on solvent, solves long-standing functionalization challenges …
Ansamers Target Integrins
Yao Lab
Bicyclic peptides derived from the amanitin scaffold can exist as non-interconvertible conformational isomers called ansamers, and the two mirror-like forms can differ by orders of …
Scalable Azapeptide Macrocycles
Lubell Lab
A convergent solution-phase strategy for a potent macrocyclic azapeptide CD36 modulator sidesteps preparative chromatography entirely, delivering 100 mg of >99%-pure material by swapping an oligomer-prone …
Activating Native Termini
Raj Lab
Thiazoline and thiazole macrocycles embedded in bioactive marine peptides have long required pre-built specialty building blocks that slow synthesis and risk epimerization. A new palladium-mediated …