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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Targeted Protein Degradation Disease Drugs 71

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

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 79

Drug Hunter

JULY 21, 2023

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

Structure Based Drug Design (SBDD) 227

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 Licensing Licensing 130

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

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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Targeted Protein Degradation DNA Engineering Science 52

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.

Targeted Protein Degradation 40

Targeted Protein Degradation Therapies Disease Drugs 40

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.

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

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 115

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 52

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

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 52

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. Advances in Diagnostic Tools and Therapeutic Approaches for Gliomas: A Comprehensive Review.

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Targeted Protein Degradation Drugs Disease FDA Approval 64

LifeSciVC

OCTOBER 28, 2024

During this time, novel science-heavy platforms were “hot” and well-funded: CRISPR, gene therapy, CAR-T, Targeted Protein Degradation, oligo/mRNAs, next gen chemistry, ADCs, Radiopharm, bispecifics… Truly an amazing period, and Atlas started and backed a number of great stories during this period (e.g.,

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Licensing Licensing Marketing Targeted Protein Degradation 92

The Pharma Data

SEPTEMBER 15, 2020

“ Amgen addresses important scientific questions to advance care and improve the lives of patients with serious diseases, including oncology, inflammation and cardiometabolic diseases, among others,” said Flavius Martin , vice president of Oncology, Inflammation and Site Head at Amgen South San Francisco.

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Targeted Protein Degradation Molecular Biology Small Molecule Science 52

The Pharma Data

JANUARY 31, 2021

Joint drug discovery program to focus on a single ion channel that is a well-validated target for neurological diseases. They are well established drug targets, particularly in neurological and cardiovascular diseases, but many remain undrugged or poorly drugged, and may be tractable to structure-based approaches.

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

Elrig

MARCH 22, 2023

Therapeutic oligos, such as ASOs, siRNAs, and other mRNA-targeted therapeutics, have emerged as an exciting modality with the potential to address a variety of previously untreatable conditions. 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 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. This targeted delivery allows enhanced therapeutic efficacy while reducing the harmful side effects commonly associated with traditional chemotherapy.

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Small Molecule Drugs Immune Response Targeted Protein Degradation 126

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 Hunter

AUGUST 21, 2023

Obtaining adequate drug exposure in the brain is key to treating CNS diseases effectively. Prodrugs Remain in “Proof-of-Concept” Stages Prodrug strategies for CNS deliver have also been applied with varying success , with the most famous example being L-Dopa for Parkinson’s disease. Figure 18.

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Drugs Disease Targeted Protein Degradation Screening Hits 206