Peptide Publications Archive
Showing items in Cyclic Peptides · Clear filter
Locking Peptide Shape
Spring and Yudin Labs
Macrocyclic peptides fold into multiple conformations, frustrating efforts to fix their three-dimensional shape. A new rhodium-catalyzed strategy now builds a biaryl "dominant rotor" directly into …
SuFEx Locks Rings
Fan and Mi Teams
Metal-free macrocyclization has long been a bottleneck for DNA-encoded peptide libraries. A new SuFEx-based strategy closes rings in aqueous buffer within minutes, scales to 343 …
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 …