Results 101 to 110 of about 13,875 (179)

Developments and challenges in hit progression within fragment-based drug discovery. [PDF]

Nat Commun
Grosjean H, Biggin PC.
europepmc   +1 more source

Design, Synthesis, and Evaluation of Novel Thiazole-Based Peptidomimetic Compounds as Potent SARS-CoV-2 Main Protease Covalent Inhibitors. [PDF]

ACS Infect Dis
Yin W, Kong WP, Leung SL, Liang Z, Chen YW, Wong KY.   +5 more
europepmc   +1 more source

A Modular Synthesis of C5‐Sulfenyl Thiazoles via an Intermolecular Pummerer Rearrangement: An Underexplored Scaffold for Medicinal Chemistry

Angewandte Chemie, EarlyView.
Modular access to underexplored C5‐sulfenyl thiazoles via an intermolecular Pummerer rearrangement is reported. The methodology exhibits a broad functional group tolerance enabling the seamless design of trisubstituted thiazole cores bearing a sulfur handle for further elaboration.
Joe L. Smy, Theo C. Webb, Barnaby W. Greenland, S. Mark Roe, John Spencer, Storm Hassell‐Hart   +5 more
wiley   +2 more sources

Unleashing the power of DNA-encoded libraries for challenging targets in drug discovery. [PDF]

Pharm Sci Adv
Du N, Li Y, Lou Q, Zhang G, Li Y, Li Y.
europepmc   +1 more source

Proteome‐Wide Target Identification Using Reactive Metallo‐Scaffolds (r‐mS): A Platform for Metallodrug Discovery

Angewandte Chemie, EarlyView.
Re‐envisioning the Ligandable Proteome: Reactive Metallo‐Scaffolds (r‐mS) combine non‐covalent protein engagement by a metallo‐scaffold with covalent cysteine capture through a tethered chloroacetamide warhead. Chemoproteomic profiling reveals unique enzyme engagement including ligases, kinases and methyltransferases, highlighting opportunities for ...
Jessica E. Waters, Harry Wilders, George S. Biggs, Mika Kintzel, Emma E. Cawood, Jonathan Bailey, Sarah Maslen, Yew Mun Yip, Mason Wakley, Ioannis G. Riziotis, Thomas W. Rees, Joanna Redmond, J. Mark Skehel, David House, Jacob Bush, Jeannine Hess   +15 more
wiley   +2 more sources

Direct-to-Biology: Streamlining the Path From Chemistry to Biology in Drug Discovery. [PDF]

ChemMedChem
Hübner AF, Barthels F.
europepmc   +1 more source

Disulfide tethering reveals cryptic pockets in oncogenic KRAS. [PDF]

Commun Chem
Balius TE, Dyba M, Kumari V, Denson JP, Yi M, Sharma AK, Prakash P, Alberico E, Messing S, Wall V, Chan AH, Simanshu DK, Nissley DV, McCormick F, Esposito D, Maciag AE, Turner DM.   +16 more
europepmc   +1 more source

NMR-Based Fragment Screening for RNA-Targeted Drug Discovery. [PDF]

Molecules
Petersen RJ, Wang Y.
europepmc   +1 more source

Fusion Strategy of DNA-Encoded Libraries Drives Discovery of Allosteric Inhibitors of SARS-CoV‑2 RdRp. [PDF]

JACS Au
Li L, Wang X, Ding P, Shen X, Hu H, Wang X, Jin R, Wu X, Zhang Y, Lu W, Yue J, Xu HE, Yin W, Xu Y, Lu X.   +14 more
europepmc   +1 more source

The Current Toolbox for Covalent Inhibitors: From Hit Identification to Drug Discovery. [PDF]

JACS Au
You M, Liu H, Li C.
europepmc   +1 more source