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ACS Fall 2023 First Disclosures  

Drug Hunter

The First Disclosures sessions at the 2023 ACS Fall Meeting in San Francisco, organized by Nikki Goodwin , presented a variety of new orally available small molecules. The post ACS Fall 2023 First Disclosures appeared first on Drug Hunter. Stay tuned!

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Structure-Based Optimization of Covalent, Small-Molecule Stabilizers of the 14-3-3?/ER? Protein–Protein Interaction from Nonselective Fragments

Covalent Modifiers

Arkin Journal of the American Chemical Society 2023 DOI: 10.1021/jacs.3c05161 Here, we show the structure-based optimization of the nonselective fragment toward selective and highly potent small-molecule stabilizers of the 14-3-3σ/ERα complex. Jeffrey Neitz, Adam R. Renslo, Christian Ottmann, Luc Brunsveld, and Michelle R.

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Golgi Neurosciences Partners with CDD Vault to Drive Innovation in Neurodegenerative Disease Treatment

Collaborative Drug

Milano, Italy and San Francisco, USA, August 29th, 2023 - Golgi Neurosciences S.r.l.,

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Exploration of the Tunability of BRD4 Degradation by DCAF16 Trans-labelling Covalent Glues

Covalent Modifiers

Ebert, Nathanael Gray bioRxiv 2023 [link] Small molecules that can induce protein degradation by inducing proximity between a desired target and an E3 ligase have the potential to greatly expand the number of proteins that can be manipulated pharmacologically. Rutter, Cyrus Y. Jin, Michelle Y. Wang, Shawn Xu, Anna M.

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Comprehensive Mapping of Electrophilic Small Molecule-Protein Interactions in Human Cells

Covalent Modifiers

ChemRxiv 2023 [link] Covalent chemistry is a versatile approach for expanding the ligandability of the human proteome. Cravatt, B.; Hayward, R.; DeMeester, K.; Ogasawara, D.; Schreiber, S.; Melillo, B.

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Phage Display of Two Distinct Warheads to Inhibit Challenging Proteins

Covalent Modifiers

Mengmeng Zheng and Jianmin Gao ACS Chemical Biology 2023 DOI: 10.1021/acschembio.3c00297 3c00297 Falling in between traditional small molecules and antibodies in size, peptides are emerging as a privileged therapeutic modality, one that can harness the benefits of both small molecule and antibody drugs.

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Metabolism of 2023 FDA Approved Small Molecules – PART 2

Metabolite Tales Blog

Table 1: Small molecule drugs approved by the FDA in 2023 with reported involvement of phase II mechanisms In vitro : In vivo differences Incubation of the SGLT2 (sodium-glucose co-transporter-2) inhibitor bexagliflozin in human liver microsomes points to metabolism through both oxidation and glucuronidation to 6 main metabolites.