Upcoming Webinar: Targeted Protein Degradation - New Modalities and Design Technologies
Collaborative Drug
MAY 18, 2024
Upcoming Webinar: Targeted Protein Degradation - New Modalities and Design Technologies
Targeted Protein Degradation Related Topics 
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Recent Highlights in Targeted Protein Degradation
Drug Hunter
JUNE 29, 2023
In Wednesday’s Flash Talk webinar , we covered recent highlights in targeted protein degradation, with lots of great questions from the audience. KT-333 and KT-003) AR degraders and ER degraders from Arvinas (bavdegalutamide/ARV-110, ARV-766, and ARV-471) MDM2 degraders from Kymera (e.g.
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CDD Exhibiting at the 6th Targeted Protein Degradation Summit, Boston, October 31- November 2.
Collaborative Drug
OCTOBER 27, 2023
CDD Exhibiting at the 6th Targeted Protein Degradation Summit, Boston, October 31- November 2.
Recorded Webinar: Targeted Protein Degradation - New Modalities and Design Technologies
Collaborative Drug
JUNE 21, 2024
Recorded Webinar: Targeted Protein Degradation - New Modalities and Design Technologies
Exploiting the Cullin E3 Ligase Adaptor Protein SKP1 for Targeted Protein Degradation
Covalent Modifiers
FEBRUARY 2, 2024
Nomura ACS Chemical Biology 2024 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. Huang, Ingrid E.
Exploiting the Cullin E3 Ligase Adaptor Protein SKP1 for Targeted Protein Degradation
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.
Covalency in PROTACs: Mechanisms and applications [@RPNowak]
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).
The Roles of Degrons in Targeted Protein Degradation | BMG LABTECH
BMG Labtech
MARCH 17, 2025
At the most fundamental level you can think of a degron as a sequence of amino acids or a structural motif that can facilitate the degradation of protein substrates.
A covalent BTK ternary complex compatible with targeted protein degradation
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.
Scientists generate new targeted protein degradation system that tunes a cell’s own proteins
Broad Institute
MARCH 14, 2024
Scientists generate new targeted protein degradation system that tunes a cell’s own proteins By Leah Eisenstadt March 14, 2024 Breadcrumb Home Scientists generate new targeted protein degradation system that tunes a cell’s own proteins Researchers have engineered a compact degron tag that can be precisely edited into a cell’s genome, enabling scientists (..)
Genentech takes up a deal to make ‘molecular glue’ drugs
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.
Targeted protein degradation: turning undruggable targets into druggable targets
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.
Discovery of a DCAF11-dependent cyanoacrylamide-containing covalent degrader of BET-proteins
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.
Pervasive aggregation and depletion of host and viral proteins in response to cysteine-reactive electrophilic compounds
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.
Recruitment of FBXO22 for targeted degradation of NSD2 [@CherylArrowsmi1]
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).
Seagen partners with Nurix to create new kind of cancer drug
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.
Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2
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.
Covalent PROTAC design method based on a sulfonyl pyridone probe
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.
Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2
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.
Degrader Radar, Apr. ’23: DCAF1, on CNS Degraders, and More
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.
Exploration of the Tunability of BRD4 Degradation by DCAF16 Trans-labelling Covalent Glues
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.
Chemical Specification of E3 Ubiquitin Ligase Engagement by Cysteine-Reactive Chemistry
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.
New platform set to accelerate early-stage targeted protein degradation
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?
Molecules of the Month – June 2023
Drug Hunter
JULY 21, 2023
“compound 13” – A DCAF1 binder applied to targeted protein degradation, identified through high-throughput screening and optimization by Novartis.
AI in Drug Discovery - A Highly Opinionated Literature Review (Part III)
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 (..)
Attacking Cancers Using Novel Methods of Targeted Protein Degradation
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.
Drug Hunter Journal Club: March 2023
Drug Hunter
APRIL 23, 2023
BCCov “A covalent BTK ternary complex compatible with targeted protein degradation” Nat.
Discovery of electrophilic degraders that exploit SNAr chemistry
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.
Kinase-impaired BTK mutations are susceptible to clinical-stage BTK and IKZF1/3 degrader NX-2127
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.
SMR Meeting: Molecular Glues
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.
Evotec Achieves Key Milestones in Its Collaboration with Bristol Myers Squibb On Targeted Protein Degradation
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.
Targeted protein degradation and next-generation degraders | BMG LABTECH
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.
Patent Highlights: Allosteric AR Modulators, Glycogen Synthase Inhibitors, and More
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.
Cell-based protein degrader assays for microplates | BMG LABTECH
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.
Sygnature Discovery and UBE Corporation successfully identify potent SHP2 Degrader Compounds
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.
Oncology Market Outlook 2024
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
Q3 2024 Newsletter – Metabolism of degraders, gut metabolites, qNMR and more
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.
SMR Meeting: Molecular Glues
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.
CBTS Supergroup Meetings
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 (..)
Molecular glues: new solutions for undruggable proteins | BMG LABTECH
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.
SMR Meeting: Molecular Glues
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.
SMR Meeting: Molecular Glues
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.
Sosei Heptares and Captor Therapeutics Enter Strategic Technology Collaboration Focused on Targeted GPCR Degradation as Novel Approach for Drug Design
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.
Cullgen Announces “Featured Article” Publication of First in Class TRK Protein Degraders in Journal of Medicinal Chemistry
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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