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

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

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.

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

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

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

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.

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Targeted Protein Degradation Bioinformatics Disease Drugs 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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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.

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Targeted Protein Degradation Small Molecule Science Disease 52

Drug Target Review

JULY 23, 2024

Shortly after finishing my studies, I landed my first job in industry working on cell biology research for several disease indications. TPD engages the body’s natural protein recycling system by selectively eliminating disease-causing proteins, ultimately addressing the root cause of disease.

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Small Molecule Targeted Protein Degradation Science Disease 116

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.

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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.

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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.

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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

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.

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Targeted Protein Degradation Small Molecule Drug Development Disease 40

Drug Target Review

JULY 5, 2024

Since brain organoids can be derived from either diseased or healthy patients, they can recapitulate human (patho)physiology making them a better choice compared to mammalian cell systems that often fail to recapitulate the human phenotype. Both drugs increased the percentage of mature myelinating oligodendrocytes compared to control groups.

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Drugs Targeted Protein Degradation 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

JULY 22, 2021

(NYSE: PFE) today announced a global collaboration to develop and commercialize ARV-471, an investigational oral PROTAC® (PROteolysis TArgeting Chimera) estrogen receptor protein degrader. The estrogen receptor is a well-known disease driver in most breast cancers. Chief Executive Officer at Arvinas.

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Targeted Protein Degradation Therapies Clinical Trials Treatment 52

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

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

SugarCone Biotech

OCTOBER 6, 2024

These are in development for neurodegenerative diseases. 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.

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Targeted Protein Degradation International Engineering Therapies 67

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

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

By Jonathan Montagu, CEO of HotSpot Therapeutics, as part of the From The Trenches feature of LifeSciVC In the perpetual and never-ending race by the healthcare sector to unearth new approaches and therapeutics to address disease, one area in which we are seeing novel innovation is in the targeting of transcription factors.

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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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Marketing Licensing Licensing Targeted Protein Degradation 103