相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。Solution Conformations Shed Light on PROTAC Cell Permeability
Yoseph Atilaw et al.
ACS MEDICINAL CHEMISTRY LETTERS (2021)
Rationalizing PROTAC-Mediated Ternary Complex Formation Using Rosetta
Nan Bai et al.
JOURNAL OF CHEMICAL INFORMATION AND MODELING (2021)
PROTACs and Building Blocks: The 2D Chemical Space in Very Early Drug Discovery
Giuseppe Ermondi et al.
MOLECULES (2021)
Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation
Michael J. Bond et al.
RSC CHEMICAL BIOLOGY (2021)
Degradation of proteins by PROTACs and other strategies
Yang Wang et al.
ACTA PHARMACEUTICA SINICA B (2020)
Assessing the Cell Permeability of Bivalent Chemical Degraders Using the Chloroalkane Penetration Assay
Caroline A. Foley et al.
ACS CHEMICAL BIOLOGY (2020)
Structure-Based Design of a Macrocyclic PROTAC
Andrea Testa et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)
Fundamental aspects of DMPK optimization of targeted protein degraders
Carina Cantrill et al.
DRUG DISCOVERY TODAY (2020)
Assays and technologies for developing proteolysis targeting chimera degraders
Xingui Liu et al.
FUTURE MEDICINAL CHEMISTRY (2020)
Targeted protein degradation: current and future challenges
Alexander Hanzl et al.
CURRENT OPINION IN CHEMICAL BIOLOGY (2020)
Degraders early developability assessment: face-to-face with molecular properties
Giuseppe Ermondi et al.
DRUG DISCOVERY TODAY (2020)
Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance
Xin Lin et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)
Phosphorylation-Inducing Chimeric Small Molecules
Sachini U. Siriwardena et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)
Understanding and Improving the Membrane Permeability of VH032-Based PROTACs
Victoria G. Klein et al.
ACS MEDICINAL CHEMISTRY LETTERS (2020)
Systematic Investigation of the Permeability of Androgen Receptor PROTACs
Duncan E. Scott et al.
ACS MEDICINAL CHEMISTRY LETTERS (2020)
Two Decades under the Influence of the Rule of Five and the Changing Properties of Approved Oral Drugs
Michael D. Shultz
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five' chemical space: Recent progress and future challenges
Scott D. Edmondson et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2019)
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
William Farnaby et al.
NATURE CHEMICAL BIOLOGY (2019)
Arvinas’s PROTACs pass first safety and PK analysis
Asher Mullard
NATURE REVIEWS DRUG DISCOVERY (2019)
The PROTAC technology in drug development
Yutian Zou et al.
CELL BIOCHEMISTRY AND FUNCTION (2019)
Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)
Jiantao Hu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
Vittoria Zoppi et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
AUTACs: Cargo-Specific Degraders Using Selective Autophagy
Daiki Takahashi et al.
MOLECULAR CELL (2019)
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
Blake E. Smith et al.
NATURE COMMUNICATIONS (2019)
Drug-Membrane Permeability across Chemical Space
Roberto Menichetti et al.
ACS CENTRAL SCIENCE (2019)
SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate
Michael J. Roy et al.
ACS CHEMICAL BIOLOGY (2019)
Developing degraders: principles and perspectives on design and chemical space
Hannah J. Maple et al.
MEDCHEMCOMM (2019)
Targeted Degradation of a Hypoxia-Associated Non-coding RNA Enhances the Selectivity of a Small Molecule Interacting with RNA
Matthew G. Costales et al.
CELL CHEMICAL BIOLOGY (2019)
PROTACs: great opportunities for academia and industry
Xiuyun Sun et al.
SIGNAL TRANSDUCTION AND TARGETED THERAPY (2019)
Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyI)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyppyrrolidine-2-carboxamide (VH298)
Pedro Soares et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds
Kwok-Ho Chan et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?
Ian Churcher
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action
Kristin M. Riching et al.
ACS CHEMICAL BIOLOGY (2018)
Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs
Sainan An et al.
EBIOMEDICINE (2018)
Lipophilic Permeability Efficiency Reconciles the Opposing Roles of Lipophilicity in Membrane Permeability and Aqueous Solubility
Matthew R. Naylor et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation
Philipp M. Cromm et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2018)
Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead
Daniel P. Bondeson et al.
CELL CHEMICAL BIOLOGY (2018)
Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders
Scott J. Hughes et al.
STRUCTURE-BASED DRUG DESIGN: INSIGHTS FROM ACADEMIA AND INDUSTRY (2017)
How Big Is Too Big for Cell Permeability?
Par Matsson et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
Nonclassical Size Dependence of Permeation Defines Bounds for Passive Adsorption of Large Drug Molecules
Cameron R. Pye et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
Structural basis of PROTAC cooperative recognition for selective protein degradation
Morgan S. Gadd et al.
NATURE CHEMICAL BIOLOGY (2017)
Small-Molecule PROTACS: New Approaches to Protein Degradation
Momar Toure et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
Passive Membrane Permeability in Cyclic Peptomer Scaffolds Is Robust to Extensive Variation in Side Chain Functionality and Backbone Geometry
Akihiro Furukawa et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer
Kanak Raina et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2016)
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
Michael Zengerle et al.
ACS CHEMICAL BIOLOGY (2015)
Improving the passive permeability of macrocyclic peptides: Balancing permeability with other physicochemical properties
Praew Thansandote et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2015)
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
Jing Lu et al.
CHEMISTRY & BIOLOGY (2015)
Exploring experimental and computational markers of cyclic peptides: Charting islands of permeability
Conan K. Wang et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2015)
Going Out on a Limb: Delineating The Effects of β-Branching, N-Methylation, and Side Chain Size on the Passive Permeability, Solubility, and Flexibility of Sanguinamide A Analogues
Andrew T. Bockus et al.
JOURNAL OF MEDICINAL CHEMISTRY (2015)
Catalytic in vivo protein knockdown by small-molecule PROTACs
Daniel P. Bondeson et al.
NATURE CHEMICAL BIOLOGY (2015)
Phthalimide conjugation as a strategy for in vivo target protein degradation
Georg E. Winter et al.
SCIENCE (2015)
Oral Druggable Space beyond the Rule of 5: Insights from Drugs and Clinical Candidates
Bradley Croy Doak et al.
CHEMISTRY & BIOLOGY (2014)
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
Carles Galdeano et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
Intracellular drug concentration and disposition - The missing link?
Michael M. Hann et al.
METHODS (2014)
P-Glycoprotein Mediated Efflux Limits the Transport of the Novel Anti-Parkinson's Disease Candidate Drug FLZ across the Physiological and PD Pathological In Vitro BBB Models
Qian Liu et al.
PLOS ONE (2014)
Rational design and synthesis of an orally bioavailable peptide guided by NMR amide temperature coefficients
Conan K. Wang et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2014)
Integrating Intramolecular Hydrogen Bonding (IMHB) Considerations in Drug Discovery Using ΔlogP As a Tool
Marina Shalaeva et al.
JOURNAL OF MEDICINAL CHEMISTRY (2013)
A Comprehensive Mathematical Model for Three-Body Binding Equilibria
Eugene F. Douglass et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2013)
Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1α Protein-Protein Interface
Inge Van Molle et al.
CHEMISTRY & BIOLOGY (2012)
The influence of lipophilicity in drug discovery and design
John A. Arnott et al.
EXPERT OPINION ON DRUG DISCOVERY (2012)
Getting physical in drug discovery II: the impact of chromatographic hydrophobicity measurements and aromaticity
Robert J. Young et al.
DRUG DISCOVERY TODAY (2011)
Discovery and Characterizatlion of Small Molecule Inhibitors of the BET Family Bromodomains
Chun-wa Chung et al.
JOURNAL OF MEDICINAL CHEMISTRY (2011)
Impact of linker length on the activity of PROTACs
Kedra Cyrus et al.
MOLECULAR BIOSYSTEMS (2011)
The Effect of Multiple N-Methylation on Intestinal Permeability of Cyclic Hexapeptides
Oded Ovadia et al.
MOLECULAR PHARMACEUTICS (2011)
Lipophilicity in drug discovery
Michael J. Waring
EXPERT OPINION ON DRUG DISCOVERY (2010)
Suppression of inflammation by a synthetic histone mimic
Edwige Nicodeme et al.
NATURE (2010)
Selective inhibition of BET bromodomains
Panagis Filippakopoulos et al.
NATURE (2010)
Improving oral bioavailability of peptides by multiple N-methylation: Somatostatin analogues
Eric Biron et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2008)
The influence of drug-like concepts on decision-making in medicinal chemistry
Paul D. Leeson et al.
NATURE REVIEWS DRUG DISCOVERY (2007)
Conformational flexibility, internal hydrogen bonding, and passive membrane permeability: Successful in silico prediction of the relative permeabilities of cyclic peptides
Taha Rezai et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2006)
Hydrogen bonding descriptors in the prediction of human in vivo intestinal permeability
S Winiwarter et al.
JOURNAL OF MOLECULAR GRAPHICS & MODELLING (2003)
An alkylsilyl-tethered, high-capacity solid support amenable to diversity-oriented synthesis for one-bead, one-stock solution chemical genetics
JA Tallarico et al.
JOURNAL OF COMBINATORIAL CHEMISTRY (2001)