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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Targeted Protein Degradation Disease Drugs 200

Covalent Modifiers

OCTOBER 19, 2023

[link] The Src homology 2 (SH2) domain recognizes phosphotyrosine (pY) post translational modifications in partner proteins to trigger downstream signaling. Drug discovery efforts targeting the SH2 domains have long been stymied by the poor drug-like properties of phosphate and its mimetics.

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Targeted Protein Degradation Drugs 208

Covalent Modifiers

FEBRUARY 16, 2024

[link] The Src homology 2 (SH2) domain recognizes phosphotyrosine (pY) post translational modifications in partner proteins to trigger downstream signaling. Drug discovery efforts targeting the SH2 domains have long been stymied by the poor drug-like properties of phosphate and its mimetics.

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Targeted Protein Degradation Drugs 189

Drug Hunter

APRIL 23, 2023

BCCov “A covalent BTK ternary complex compatible with targeted protein degradation” Nat. Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples. Get ahead now by requesting a trial. already a member?

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Targeted Protein Degradation Drugs Trials 130

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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Targeted Protein Degradation Small Molecule Computational Chemistry Bioinformatics 139

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. ’23: DCAF1, on CNS Degraders, and More appeared first on Drug Hunter.

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Targeted Protein Degradation Trials Therapies Disease 131

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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Targeted Protein Degradation Small Molecule Drugs 182

Drug Hunter

JULY 21, 2023

With the popular success of diabetes and weight-loss peptide drugs from Novo (e.g. vorasidenib – An oral first-in-class dual IDH1/IDH2 inhibitor with efficacy in Phase III trials for IDH-mutant grade 2 gliomas, discovered through structure-based drug design (SBDD) of a prior mIDH inhibitor, developed by Agios and Servier.

Structure Based Drug Design (SBDD) 227

Structure Based Drug Design (SBDD) Targeted Protein Degradation Clinical Trials Trials 227

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?

Targeted Protein Degradation 52

Targeted Protein Degradation DNA Engineering Drugs 52

SugarCone Biotech

OCTOBER 6, 2024

Because Trf1 is degraded as part of the degradation of the internalized protein complex, these EGFR-bright cells become iron-starved and die as a consequence. They have taken this drug into normal primates and have shown the drug is well tolerated. Wow - a very clever strategy.

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Targeted Protein Degradation International Engineering Therapies 67

Covalent Modifiers

FEBRUARY 1, 2024

Therefore, understanding mechanisms by which acquired mutations in BTK confer drug resistance and developing new therapies to overcome resistance are critically important. 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.

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Targeted Protein Degradation Clinical Trials Trials Science 173

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.

Targeted Protein Degradation 40

Targeted Protein Degradation Therapies Disease Drugs 40

The Pharma Data

DECEMBER 16, 2020

TWO NOVEL SOLID TUMOUR TARGETS FROM THE PARTNERSHIP TRANSITION INTO DRUG DISCOVERY. TARGETS IDENTIFIED AND VALIDATED THROUGH EVOTEC’S PROPRIETARY PANOMICS PLATFORM. This has enabled the generation of a pipeline of novel first-in-class targeted protein degradation projects.

Targeted Protein Degradation 40

Targeted Protein Degradation Bioinformatics Disease Drugs 40

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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Targeted Protein Degradation Computational Chemistry Trials Licensing 130

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.

Targeted Protein Degradation 40

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.

Targeted Protein Degradation 52

Targeted Protein Degradation Small Molecule Treatment Disease 52

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.

Targeted Protein Degradation 52

Targeted Protein Degradation Small Molecule Science Disease 52

Drug Target Review

OCTOBER 4, 2023

Antibody-drug conjugates (ADCs) have been a groundbreaking approach to cancer treatment with their ability to deliver cytotoxic drugs directly to diseased cells while sparing healthy tissues. 1 However, efforts proved less effective than the original drugs, owing mostly to insufficient toxicity against cancer cells.

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Small Molecule Drugs Immune Response Targeted Protein Degradation 126

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. The role of NMR spectroscopy in drug metabolism studies. Novel fecal metabolites of inavolisib (GDC-0077).

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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.

Targeted Protein Degradation 40

Targeted Protein Degradation Therapies Disease Drugs 40

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. Conventional drug development has often focused on finding small molecules that fit the active site of a protein.

Targeted Protein Degradation 40

Targeted Protein Degradation Small Molecule Drug Development Disease 40

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.

Targeted Protein Degradation 40

Targeted Protein Degradation Therapies Disease Drugs 40

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.

Targeted Protein Degradation 40

Targeted Protein Degradation Therapies Disease Drugs 40

The Pharma Data

DECEMBER 21, 2020

. Unique combination of novel technologies to enhance GPCR drug discovery and expand capabilities into wider drug target universe. Captor’s Optigradeä platform is focused on improving the selectivity and performance of first-generation degrader drugs. TOKYO and CAMBRIDGE, England , Dec.

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Targeted Protein Degradation Small Molecule Structure Based Drug Design (SBDD) Drugs 40

Drug Target Review

JULY 23, 2024

This laid the groundwork for my career in drug discovery using novel modalities like small molecule inhibitors, antibodies, RNA interference (RNAi) and, currently, small molecule protein degraders – which are opportunities to change how we think about medicines. I’ve already had a number of ‘rocking chair’ moments in my career.

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Small Molecule Targeted Protein Degradation Science Disease 116

Drug Target Review

JULY 5, 2024

1 Considerations for creating complex organoids Despite the numerous advantages of using brain organoids in drug discovery, some limitations should be considered. 1 Considerations for creating complex organoids Despite the numerous advantages of using brain organoids in drug discovery, some limitations should be considered.

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Targeted Protein Degradation Drugs Disease FDA Approval 64

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.

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Targeted Protein Degradation Small Molecule Science Disease 40

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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Targeted Protein Degradation Small Molecule Clinical Development Disease 40

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. Terms of the Collaboration.

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Targeted Protein Degradation Therapies Clinical Trials Treatment 52

The Pharma Data

JANUARY 31, 2021

Ion channels represent a large but under-exploited class of drug targets beyond G protein-coupled proteins (GPCRs). Collaboration combines Sosei Heptares’ leading structure-based drug design platform with Metrion Biosciences’ ion channel expertise.

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Structure Based Drug Design (SBDD) Targeted Protein Degradation Drugs Disease 52

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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Targeted Protein Degradation Engineering Clinical Trials Disease 40

Elrig

MARCH 22, 2023

Over the two days, we’ll bring together academia, industry, and the vendor community to discuss recent advancements in two ultra-exciting areas of drug discovery and biological research: therapeutic oligonucleotides and chemical biology. Right now, targeted protein degradation is a critical focus topic across both industry and academia.

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Targeted Protein Degradation Science Disease Laboratories 40

Drug Hunter

AUGUST 21, 2023

Obtaining adequate drug exposure in the brain is key to treating CNS diseases effectively. Recently, Dennis Koester gave us a crash course in CNS drug discovery in a Drug Hunter Flash Talk. Why Kp,uu is the Most Important Parameter in CNS Drug Discovery What Influences the Kp,uu of Drugs?

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Drugs Disease Targeted Protein Degradation Screening Hits 206

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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Targeted Protein Degradation Pharmaceuticals Research Treatment 147

Elrig

MARCH 13, 2025

Target Innovation & Novel Screening Technologies – Forum Round-Up In the rapidly evolving landscape of drug discovery, the identification and validation of novel therapeutic targets are pivotal to expanding the druggable genome and tackling unmet medical needs.

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Targeted Protein Degradation RNA Drugs Disease 52

LifeSciVC

FEBRUARY 5, 2025

Given this ever-increasing body of evidence, why is it that for so long, they have not been the focus of drug discovery? Lacking active sites entirely, transcription factors are instead largely regulated by post-translational modification, which in turn impacts changes in conformation, behavior, and interaction with other proteins.

Small Molecule 67

Small Molecule Targeted Protein Degradation Regulations Disease 67

LifeSciVC

OCTOBER 28, 2024

As context, biotech business models have largely had two flavors for decades: asset-centric investments focused on specific product opportunities and platforms (discovery engines) designed to create new drugs based on novel modalities, technologies, or biological insights. In each moment, we’ve seen a reversion to asset incrementalism (e.g.,

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Licensing Licensing Marketing Targeted Protein Degradation 91