Photochemical and Collision-Induced Cross-Linking of Asp, Glu, Asn, and Gln Residues in Peptide-Nitrile Imine Conjugate Ions in the Gas Phase DOI
Mikuláš Vlk,

Jiahao Wan,

Marianna Nytka

et al.

Journal of the American Society for Mass Spectrometry, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 27, 2024

Peptide conjugates furnished with a 2,5-diaryltetrazolecarbonyl tag at the C-terminal lysine, which we call peptide-

Language: Английский

Functional and Structural Polypharmacology of Indazole-based Privileged Ligands to Tackle the Undruggability of Membrane Transporters DOI Creative Commons
Sven Marcel Stefan, Sachin Puri, Muhammad Rafehi

et al.

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 287, P. 117234 - 117234

Published: Jan. 2, 2025

Language: Английский

Citations

1
Design and Synthesis of 7-(N-Aryl Pyrrolidinyl) Indoles as Potential DCAF15 Binders DOI Creative Commons
Ravi Devarajappa,

Scarlett Kiyeleko,

Sofiane Hocine

et al.

Reactions, Journal Year: 2025, Volume and Issue: 6(1), P. 20 - 20

Published: March 7, 2025

We describe the design and synthesis of a series 7-(N-aryl pyrrolidinyl) indoles oxo-analogs as isosteric mimics DCAF15 binder E7820, well-known member aryl sulfonamides known SPLAMs. The functionalization C-7 in was achieved by metal-catalyzed CH-activation with unexpected results. Binding assays revealed pyrrolidine N-aryl carboxylic acid analog to be equally active E7820.

Language: Английский

Citations

0
Precision peptide disruptors: The next generation of targeted therapeutics in oncology DOI Creative Commons

Bria O'Gorman,

Sean F. Cooke, Connor M. Blair

et al.

Cellular Signalling, Journal Year: 2025, Volume and Issue: unknown, P. 111783 - 111783

Published: April 1, 2025

Language: Английский

Citations

0
Exploring Macrocyclic Chemical Space: Strategies and Technologies for Drug Discovery DOI Creative Commons
Taegwan Kim,

Eunbee Baek,

Jonghoon Kim

et al.

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(5), P. 617 - 617

Published: April 24, 2025

Macrocycles have emerged as significant therapeutic candidates in drug discovery due to their unique capacity target complex and traditionally inaccessible biological interfaces. Their structurally constrained three-dimensional configurations facilitate high-affinity interactions with challenging targets, notably protein–protein However, despite potential, the synthesis optimization of macrocyclic compounds present considerable challenges related structural complexity, synthetic accessibility, attainment favorable drug-like properties, particularly cell permeability oral bioavailability. Recent advancements methodologies expanded chemical space accessible macrocycles, enabling creation diverse pharmacologically active compounds. Concurrent developments computational strategies further enhanced macrocycle design, providing valuable insights into predicting molecular properties essential for efficacy. Additionally, a deeper understanding macrocycles’ conformational adaptability, especially ability internally shield polar functionalities improve membrane permeability, has significantly informed rational design. This review discusses recent innovations that advanced over past five years. It emphasizes importance integrating these overcome existing challenges, illustrating how synergy expands potential diversity macrocycles. Selected case studies underscore practical impact integrated approaches, highlighting promising applications across biomedical targets.

Language: Английский

Citations

0
Photochemical and Collision-Induced Cross-Linking of Asp, Glu, Asn, and Gln Residues in Peptide-Nitrile Imine Conjugate Ions in the Gas Phase DOI
Mikuláš Vlk,

Jiahao Wan,

Marianna Nytka

et al.

Journal of the American Society for Mass Spectrometry, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 27, 2024

Peptide conjugates furnished with a 2,5-diaryltetrazolecarbonyl tag at the C-terminal lysine, which we call peptide-

Language: Английский

Citations

1