Covalent Modifiers

OCTOBER 21, 2023

Seong Ho Hong , Akane Osa , Ingrid E Wertz , Daniel Nomura bioRxiv 2023.10.20.563371; doi: [link] Targeted protein degradation with Proteolysis Targeting Chimeras (PROTACs) is a powerful therapeutic modality for eliminating disease-causing proteins through targeted ubiquitination and proteasome-mediated degradation.

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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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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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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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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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SugarCone Biotech

OCTOBER 6, 2024

Cell surface degraders are weird but cool. There is an emerging class of therapeutics, brilliant really, that make use of cell surface proteins that will respond to antibody binding by moving quickly inside the cell and then shuttling over to lysosomes for degradation. Rennert, SugarCone Biotech LLC.

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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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Drug Hunter

APRIL 23, 2023

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

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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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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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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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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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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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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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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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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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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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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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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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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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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

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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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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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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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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BMG Labtech

APRIL 16, 2024

Promising future Molecular glues offer exciting opportunities for targeted protein degradation and new ways to reach some of the estimated 85% of undruggable targets in the proteome. 2 Close cousins Both molecular glues and PROteolysis TArgeting Chimeras ( PROTACs ) are targeted-protein degraders.

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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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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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The Pharma Data

DECEMBER 21, 2020

Targeted protein degradation (TPD) is an approach whereby the body’s natural process for degrading proteins is diverted using small molecule drugs to eliminate disease-causing proteins. . TOKYO and CAMBRIDGE, England , Dec. No further financial details are disclosed. ” About Sosei Heptares.

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The Pharma Data

OCTOBER 15, 2020

a leading biotechnology company developing small molecule therapeutics based on its proprietary uSMITE platform of targeted protein degradation technology, today announced that the company’s internal program to develop selective degraders that target key proteins within the TRK family has been published by the Journal of Medicinal Chemistry. “In

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The Pharma Data

JULY 22, 2021

This collaboration has the potential to be transformational, as it combines our leadership in targeted protein degradation with Pfizer’s global capabilities and deep expertise in breast cancer. The companies will equally share worldwide development costs, commercialization expenses, and profits.

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The Pharma Data

SEPTEMBER 25, 2020

. Monte Rosa Therapeutics has raised $96m in Series B financing to support further develop of its pipeline of small-molecule protein degraders. The company, which was originally formed as a spinout from Cancer Research UK-funded research at the Institute of Cancer Research, specialises in targeted protein degradation.

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Drug Target Review

JULY 23, 2024

Focusing on my time as Head of Research at Kymera, I’ve been fortunate to break new ground in drug discovery and development by advancing the science of targeted protein degradation (TPD) and progressing an industry leading pipeline to solve critical health problems that traditional medicines cannot address.

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The Pharma Data

DECEMBER 15, 2020

Nasdaq: ARVN), a clinical-stage biotechnology company creating a new class of drugs based on targeted protein degradation using its PROTAC ® Discovery Engine, today announced the pricing of an underwritten public offering of 5,714,286 shares of its common stock at a price of $70.00 NEW HAVEN, Conn.,

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