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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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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Collaborative Drug

OCTOBER 27, 2023

CDD Exhibiting at the 6th Targeted Protein Degradation Summit, Boston, October 31- November 2.

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Targeted Protein Degradation 77

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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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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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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Drug Discovery World

JULY 19, 2024

Biotechnology company Draupnir Bio has received equity investments totalling €12 million to support the company’s work in the field of targeted protein degradation (TPD).

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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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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 Discovery World

APRIL 3, 2024

In the last few years, immunotherapies like immune checkpoint inhibitors, vaccines and cell and gene therapies have revolutionised the treatment of cancer, and targeted drugs like monoclonal antibodies (mAbs), poly-ADP ribose polymerase (PARP) inhibitors and targeted protein degraders are also playing an important role.

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Drug Discovery World

FEBRUARY 13, 2024

The study ‘Kinase Impaired BTK Mutations Are Susceptible to Clinical Stage BTK and IKZF1/3 Degrader NX-2127’ elucidates a previously unappreciated oncogenic scaffold function of BTK responsible for clinical resistance to enzymatic inhibitors.

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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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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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Drug Discovery World

OCTOBER 16, 2023

Professor Henrik Daub , Founder and CSO, NEOsphere Biotechnologies looks at the advancements taking place in proteomics and how targeted protein degradation represents a promising approach for developing new treatments for life-threatening diseases. PROTAC targeted protein degraders: the past is prologue.

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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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Drug Hunter

APRIL 23, 2023

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

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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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Drug Discovery World

FEBRUARY 13, 2023

Nello Mainolfi, Founder, President and CEO of Kymera Therapeutics, said: “X-Chem has been a valued partner in helping us to unlock challenging disease targets that can be only or best addressed by targeted protein degradation.

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Drug Discovery World

NOVEMBER 4, 2022

PhoreMost and targeted protein degradation (TPD) specialists Arvinas have agreed a multi-target collaboration. Under the terms of the agreement, PhoreMost will deploy its phenotypic screening platform, SITESEEKER, toward multiple high-value therapeutic targets.

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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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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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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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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

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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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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Drug Discovery World

JANUARY 15, 2024

VantAI and Blueprint Medicines VantAI and Blueprint Medicines have entered into an amended and restated collaboration and license agreement to design and advance novel targeted protein degrader therapies to address important areas of medical need.

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Drug Discovery World

MARCH 22, 2023

Oxford Drug Design and PhoreMost advance novel cancer therapeutics Oxford Drug Design has been engaged by PhoreMost to accelerate a targeted protein degradation discovery programme for novel cancer therapeutics.

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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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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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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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Drug Discovery World

OCTOBER 6, 2022

Scientific and technological breakthroughs are on the horizon in areas such as targeted protein degradation, cell antigene therapies to customise drugs and monoclonal antibodies being modified in new ways.” . However, the commercialisation of research could improve 8. Volume 23 – Issue 4, Fall 2022. References: .

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Drug Discovery World

DECEMBER 27, 2023

and seizure liability testing What are the benefits of a target safety assessment?

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