Covalent Modifiers

NOVEMBER 7, 2024

Nowak Annual Reports in Medicinal Chemistry , 2024 [link] Proteolysis targeting chimeras (PROTACs) are hetero-bifunctional molecules that remove disease-causing proteins through the means of targeted protein degradation (TPD).

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Covalent Modifiers

JULY 9, 2025

link] Targeted protein degradation (TPD) is an emerging therapeutic approach for the selective elimination of disease-related proteins. While molecular glue degraders exhibit drug-like properties, their discovery has traditionally been serendipitous and often requires post-hoc rationalization. 2025 , e202508427.

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Covalent Modifiers

MARCH 3, 2023

Calabrese Nat Commun 14 , 1189, 2023 [link] Targeted protein degradation using heterobifunctional chimeras holds the potential to expand target space and grow the druggable proteome. Bridging covalent ligand discovery with chimeric degrader design has emerged as a potential mechanism to advance both fields.

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BMG Labtech

MARCH 17, 2025

At the most fundamental level you can think of a degron as a sequence of amino acids or a structural motif that can facilitate the degradation of protein substrates.

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Targeted Protein Degradation Engineering Research Drugs 52

The Pharma Data

JUNE 12, 2025

Expanding Targeted Protein Degradation in Hematologic Malignancies Targeted protein degradation is a powerful therapeutic approach designed to destroy disease-driving proteins within cells, thereby inhibiting their ability to contribute to disease progression.

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BioPharma Drive: Drug Pricing

SEPTEMBER 20, 2023

Targeted protein degradation has emerged as one of the more competitive areas of pharmaceutical research in recent years as scientists develop new ways to reach difficult-to-drug targets.

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Broad Institute

MARCH 14, 2024

Scientists generate new targeted protein degradation system that tunes a cell’s own proteins By Leah Eisenstadt March 14, 2024 Breadcrumb Home Scientists generate new targeted protein degradation system that tunes a cell’s own proteins Researchers have engineered a compact degron tag that can be precisely edited into a cell’s genome, enabling scientists (..)

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Drug Target Review

JULY 6, 2023

Unlike traditional drug discovery, which focuses on inhibiting or activating proteins, TPD offers a more precise and efficient way to alter cellular pathways. 1 The concept of TPD was first demonstrated with a heterobifunctional small molecule to degrader a protein of interest in the early 2000s. How does TPD work? Nature News.

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Targeted Protein Degradation Small Molecule Clinical Trials Science 98

Covalent Modifiers

JANUARY 7, 2025

Second, we highlight various recent examples of protein functionalization using NASA/ArNASA chemistry, such as visualization of membrane proteins including therapeutically important G-protein coupled receptors, gel-based ligand screening assays, photochemical control of protein activity, and targeted protein degradation.

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Covalent Modifiers

MAY 31, 2024

Winter, Bioorganic & Medicinal Chemistry Letters , 2024 [link] Targeted protein degradation is mediated by small molecules that induce or stabilize protein–protein interactions between targets and the ubiquitin–proteasome machinery. Gary Tin, Marko Cigler, Matthias Hinterndorfer, Kevin D. Gygi, Georg E.

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BioPharma Drive: Drug Pricing

SEPTEMBER 7, 2023

The alliance, which aims to combine Seagen’s antibody expertise with Nurix’s targeted protein degradation research, comes as the larger biotech awaits its acquisition by Pfizer to close.

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Targeted Protein Degradation Drugs Research 189

Covalent Modifiers

NOVEMBER 2, 2023

Ashley R Julio, Flowreen Shikwana, Cindy Truong, Nikolas R Burton, Emil Dominguez, Alexandra Turmon, Jian Cao, Keriann Backus bioRxiv 2023.10.30.564067; doi: [link] Protein homeostasis is tightly regulated, with damaged or misfolded proteins quickly eliminated by the proteasome and autophagosome pathways.

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Targeted Protein Degradation Small Molecule Regulations 189

Covalent Modifiers

JULY 5, 2024

link] Targeted protein degradation (TPD) is an emerging therapeutic strategy that would benefit from new chemical entities with which to recruit a wider variety of ubiquitin E3 ligases to target proteins for proteasomal degradation. Tabor, J.R., Nat Chem Biol (2024).

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Covalent Modifiers

OCTOBER 19, 2023

The qualified inhibitors of SOCS2 could find attractive applications as chemical probes to understand the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation.

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Covalent Modifiers

DECEMBER 6, 2023

This approach showcases the potential of nucleophilic amino acid labeling probes, particularly for proteins lacking easily accessible cysteine residues, opening new possibilities for covalent PROTAC design and targeted protein degradation therapies.

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Covalent Modifiers

FEBRUARY 16, 2024

The qualified inhibitors of SOCS2 could find attractive applications as chemical probes to understand the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation.

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Targeted Protein Degradation Drugs 189

Drug Hunter

MAY 21, 2023

This article highlights six recent articles of interest in the field of targeted protein degradation including but not limited to potentially new ligases, recruiting motifs, and a discussion on the feasibility of CNS-penetrant degraders.

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Covalent Modifiers

OCTOBER 10, 2023

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.

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Covalent Modifiers

OCTOBER 3, 2023

3c06622 Targeted protein degradation relies on small molecules that induce new protein–protein interactions between targets and the cellular protein degradation machinery. Chouchani, Mikołaj Słabicki, Eric S. Fischer, Benjamin L. Ebert, Stephen M. Hinshaw, and Nathanael S.

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Sygnature Discovery

MARCH 7, 2023

Sygnature Discovery, the global integrated drug discovery company, has unveiled a new platform that facilitates the combinational high-throughput assembly and review of molecular degraders ( CHARMED ), in response to a sustained rise in demand for its multi-disciplinary expertise. What is the CHARMED platform?

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Drug Hunter

JULY 21, 2023

“compound 13” – A DCAF1 binder applied to targeted protein degradation, identified through high-throughput screening and optimization by Novartis.

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Practical Cheminformatics

JANUARY 16, 2024

Property Prediction Machine Learning Methods for Small Data Challenges in Molecular Science [link] Practical guidelines for the use of gradient boosting for molecular property prediction [link] Application of message passing neural networks for molecular property prediction [link] Molecular Similarity Molecular Similarity: Theory, Applications, and (..)

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Drug Hunter

APRIL 23, 2023

BCCov “A covalent BTK ternary complex compatible with targeted protein degradation” Nat.

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Covalent Modifiers

OCTOBER 8, 2024

Gray bioRxiv 2024.09.25.615094; doi: [link] Targeted covalent inhibition (TCI) and targeted protein degradation (TPD) have proven effective in pharmacologically addressing formerly ‘undruggable’ targets. Nix, Jianing Zhong, Mikołaj Słabicki, Eric S. Fischer, Benjamin L. Ebert, Nathanael S.

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Covalent Modifiers

FEBRUARY 1, 2024

We therefore set out to understand the nonenzymatic functions of BTK and explored targeted protein degradation to overcome the oncogenic scaffold function of mutant BTK. In this study, we found that a group of these mutants impair BTK kinase activity despite still enabling downstream BCR signaling.

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The Pharma Data

DECEMBER 16, 2020

Evotec and Bristol Myers Squibb (the successor in interest to Celgene ) initiated their long-term strategic drug discovery and development partnership in the field of targeted protein degradation in 2018 with the goal to identify novel drug targets.

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Zobio

MARCH 3, 2025

In person Molecular glues and targeted protein degraders are revolutionizing the field of drug discovery, offering promising solutions for a range of diseases, including cancer, infectious, inflammatory, and neurodegenerative diseases. The recent emergence of the molecular glue class of protein degraders is paving.

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Drug Hunter

JUNE 25, 2023

This edition includes Maze’s glycogen synthase 1 (GYS1) inhibitors that were recently licensed to Sanofi, allosteric androgen receptor (AR) modulators that may be of interest to targeted protein degradation researchers, and brain-penetrant HER2 and ROCK2 inhibitors.

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BMG Labtech

JUNE 17, 2024

Protein degradation in the cell Research over many years helped build a comprehensive picture of protein synthesis in the cell. However, knowledge of how proteins are broken down and how degradation contributes to cellular regulation is more recent.

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Targeted Protein Degradation Regulations Research Science 40

BMG Labtech

MAY 22, 2024

Options for cell-based protein degrader assays Interest is growing in the use of targeted-protein degradation to induce the breakdown of disease-causing proteins after treatment with small molecule drugs.

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Sygnature Discovery

SEPTEMBER 25, 2023

Sygnature Discovery identifies potent SHP2 degrader compounds using its proprietary targeted protein degrader platform, CHARMED, in collaboration with Japanese specialty chemical company, UBE Corporation.

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Fierce BioTech

MARCH 15, 2024

It addresses CAR-T therapies, KRAS, radiopharmaceuticals, & targeted protein degradation. It addresses CAR-T therapies, KRAS, radiopharmaceuticals, & targeted protein degradation. Blue Matter Consulting Resource Type Whitepaper BlueMatterConsulting_250x190 (1) (2).png

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Metabolite Tales Blog

OCTOBER 3, 2024

Hypha’s Q3 2024 Newsletter – Metabolism of degraders, gut metabolites, qNMR and more Focus topics for this edition: Metabolism of targeted protein degraders drugs such as PROTACs. Novel fecal metabolites of inavolisib (GDC-0077). The role of NMR spectroscopy in drug metabolism studies.

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Targeted Protein Degradation Drugs 52

Zobio

MARCH 3, 2025

In person Molecular glues and targeted protein degraders are revolutionizing the field of drug discovery, offering promising solutions for a range of diseases, including cancer, infectious, inflammatory, and neurodegenerative diseases. The recent emergence of the molecular glue class of protein degraders is paving.

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Molecular Design

JULY 6, 2025

I consider it essential to account for numbers of adjustable parameters and for correlations between descriptors (or features if you prefer) when building QSAR-like ML models, and I’m also concerned that the challenges presented by clustering in descriptor spaces are not properly acknowledged.

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Broad Institute

FEBRUARY 27, 2024

Past Speakers Speaker Topic Casey Krusemark Encoding chemicals and assays with DNA: Applications in Medicinal Chemistry and Biology Morgan Sheng Schizophrenia and bipolar disorder: from human genetics towards mechanisms and therapeutics Malvina Papanastasiou Structural insights into the LSD1 N-terminus using hydrogen/deuterium exchange-mass spectrometry (..)

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Zobio

MARCH 8, 2023

In person Molecular glues and targeted protein degraders are changing the landscape of drug discovery. They show great potential for treating diseases such as cancer, infectious, inflammatory, andneurodegenerative diseases, especially for those with “undruggable” pathogenic protein targets.

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