Developing degraders: principles and perspectives on design and chemical space (Q92189593)

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27 April 2020

title

Developing degraders: principles and perspectives on design and chemical space (English)

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27 April 2020

1

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27 April 2020

Robert Felix

5

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27 April 2020

author name string

Nat Clayden

2

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27 April 2020

Anne Baron

3

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27 April 2020

Callum Stacey

4

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27 April 2020

publication date

12 August 2019

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27 April 2020

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27 April 2020

volume

10

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27 April 2020

issue

10

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27 April 2020

page(s)

1755-1764

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Creative Commons Attribution-NonCommercial 3.0 Unported

27 April 2020

copyright license

start time

12 August 2019

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April 2022 Public Data File from Crossref

copyright status

copyrighted

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PROTAC-Mediated Degradation of Bruton's Tyrosine Kinase Is Inhibited by Covalent Binding

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SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate

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Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer

23 February 2021

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Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

23 February 2021

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MDM2-recruiting PROTAC Offers Superior, Synergistic Anti-proliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

23 February 2021

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Two Decades under the Influence of the Rule of Five and the Changing Properties of Approved Oral Drugs

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Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach

23 February 2021

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Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action

23 February 2021

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Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs).

23 February 2021

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Quantifying the chameleonic properties of macrocycles and other high-molecular-weight drugs

23 February 2021

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Catalytic in vivo protein knockdown by small-molecule PROTACs.

23 February 2021

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DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation

23 February 2021

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Oral druggable space beyond the rule of 5: insights from drugs and clinical candidates.

23 February 2021

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Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

23 February 2021

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Structure of the human Cereblon-DDB1-lenalidomide complex reveals basis for responsiveness to thalidomide analogs

23 February 2021

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How proteins bind macrocycles.

23 February 2021

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Lead- and drug-like compounds: the rule-of-five revolution

23 February 2021

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Lenalidomide causes selective degradation of IKZF1 and IKZF3 in multiple myeloma cells

23 February 2021

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The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins

23 February 2021

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Getting in shape: controlling peptide bioactivity and bioavailability using conformational constraints

23 February 2021

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Design, synthesis and biological evaluation of nuclear receptor-degradation inducers.

23 February 2021

1 reference

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Intramolecular hydrogen bonding in medicinal chemistry

23 February 2021

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Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

23 February 2021

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Molecular properties that influence the oral bioavailability of drug candidates

23 February 2021

1 reference

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Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

23 February 2021

1 reference

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23 February 2021

Identifiers

DOI

10.1039/C9MD00272C

1 reference

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27 April 2020

1 reference

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27 April 2020

PubMed publication ID

31867093

1 reference