- Home
- Publications
- Publication Search
- Publication Details
Title
10 years into the resurgence of covalent drugs
Authors
Keywords
-
Journal
Future Medicinal Chemistry
Volume 13, Issue 2, Pages 193-210
Publisher
Future Science Ltd
Online
2020-12-05
DOI
10.4155/fmc-2020-0236
References
Ask authors/readers for more resources
Related references
Note: Only part of the references are listed.- KRAS G12C Game of Thrones, which direct KRAS inhibitor will claim the iron throne?
- (2020) Misako Nagasaka et al. CANCER TREATMENT REVIEWS
- Axicabtagene ciloleucel CD19 CAR-T cell therapy results in high rates of systemic and neurologic remissions in ten patients with refractory large B cell lymphoma including two with HIV and viral hepatitis
- (2020) Ahmed Abbasi et al. Journal of Hematology & Oncology
- Discovery of Lysine-Targeted eIF4E Inhibitors through Covalent Docking
- (2020) Xiaobo Wan et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Covalent-Fragment Screening of BRD4 Identifies a Ligandable Site Orthogonal to the Acetyl-Lysine Binding Sites
- (2020) Michael D. Olp et al. ACS Chemical Biology
- Cyanopyrrolidine Inhibitors of Ubiquitin Specific Protease 7 Mediate Desulfhydration of the Active-Site Cysteine
- (2020) Charlene Bashore et al. ACS Chemical Biology
- The Frequency of Ras Mutations in Cancer
- (2020) Ian A. Prior et al. CANCER RESEARCH
- Covalent fragment libraries in drug discovery
- (2020) Aaron Keeley et al. DRUG DISCOVERY TODAY
- Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer
- (2020) Jay B. Fell et al. JOURNAL OF MEDICINAL CHEMISTRY
- Alkynyl Benzoxazines and Dihydroquinazolines as Cysteine Targeting Covalent Warheads and Their Application in Identification of Selective Irreversible Kinase Inhibitors
- (2020) Kirsten McAulay et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Drug–protein adducts: past, present, and future
- (2020) Thomas A. Baillie MEDICINAL CHEMISTRY RESEARCH
- Crowdsourcing drug discovery for pandemics
- (2020) John Chodera et al. Nature Chemistry
- Fragment-based covalent ligand screening enables rapid discovery of inhibitors for the RBR E3 ubiquitin ligase HOIP
- (2019) Henrik Johansson et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Selective and reversible modification of kinase cysteines with chlorofluoroacetamides
- (2019) Naoya Shindo et al. Nature Chemical Biology
- PKAD: a database of experimentally measured pKa values of ionizable groups in proteins
- (2019) Swagata Pahari et al. Database-The Journal of Biological Databases and Curation
- Properties of FDA-approved small molecule protein kinase inhibitors
- (2019) Robert Roskoski PHARMACOLOGICAL RESEARCH
- The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K
- (2019) Elma Mons et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Covalent Inhibitors of Protein–Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues
- (2019) Luca Gambini et al. JOURNAL OF MEDICINAL CHEMISTRY
- Rapid covalent-probe discovery by electrophile-fragment screening
- (2019) Efrat Resnick et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- The Proteome-Wide Potential for Reversible Covalency at Cysteine
- (2019) Kristine Senkane et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- A Fast Ab Initio Predictor Tool for Covalent Reactivity Estimation of Acrylamides
- (2019) Ferruccio Palazzesi et al. Journal of Chemical Information and Modeling
- Systematic Studies on the Protocol and Criteria for Selecting a Covalent Docking Tool
- (2019) Chang Wen et al. MOLECULES
- Resistance mechanisms to osimertinib in EGFR-mutated non-small cell lung cancer
- (2019) Alessandro Leonetti et al. BRITISH JOURNAL OF CANCER
- Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy
- (2019) Carlo Baggio et al. JOURNAL OF MEDICINAL CHEMISTRY
- The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity
- (2019) Jude Canon et al. NATURE
- Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors
- (2019) Brian A. Lanman et al. JOURNAL OF MEDICINAL CHEMISTRY
- Recent Developments in Cell Permeable Deubiquitinating Enzyme Activity-Based Probes
- (2019) Daniel Conole et al. Frontiers in Chemistry
- Chemoproteomics-Enabled Covalent Ligand Screening Reveals ALDH3A1 as a Lung Cancer Therapy Target
- (2018) Jessica L. Counihan et al. ACS Chemical Biology
- High-Throughput Kinetic Analysis for Target-Directed Covalent Ligand Discovery
- (2018) Gregory B. Craven et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- The Taxonomy of Covalent Inhibitors
- (2018) Alfred Tuley et al. BIOCHEMISTRY
- Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor
- (2018) Matthew R. Janes et al. CELL
- Comparative Evaluation of Covalent Docking Tools
- (2018) Andrea Scarpino et al. Journal of Chemical Information and Modeling
- Docking of Covalent Ligands: Challenges and Approaches
- (2018) Christoph Sotriffer Molecular Informatics
- Kinase inhibitors: the road ahead
- (2018) Fleur M. Ferguson et al. NATURE REVIEWS DRUG DISCOVERY
- Let K-Ras activate its own inhibitor
- (2018) Alexander V. Statsyuk NATURE STRUCTURAL & MOLECULAR BIOLOGY
- The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors
- (2018) Rasmus Hansen et al. NATURE STRUCTURAL & MOLECULAR BIOLOGY
- Let K-Ras activate its own inhibitor
- (2018) Alexander V. Statsyuk NATURE STRUCTURAL & MOLECULAR BIOLOGY
- The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors
- (2018) Rasmus Hansen et al. NATURE STRUCTURAL & MOLECULAR BIOLOGY
- Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine
- (2018) Olesya A. Kharenko et al. JOURNAL OF MEDICINAL CHEMISTRY
- Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity
- (2018) Elena De Vita et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of covalent enzyme inhibitors using virtual docking of covalent fragments
- (2018) Sandipan Roy Chowdhury et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology
- (2018) Matthias Gehringer et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors
- (2018) Agustin Casimiro-Garcia et al. JOURNAL OF MEDICINAL CHEMISTRY
- Pharmacological targeting of RAS: Recent success with direct inhibitors
- (2018) John P. O’Bryan PHARMACOLOGICAL RESEARCH
- Therapeutic Potential of Nitrogen Mustard Based Hybrid Molecules
- (2018) Yiming Chen et al. Frontiers in Pharmacology
- “Inverse Drug Discovery” Strategy To Identify Proteins That Are Targeted by Latent Electrophiles As Exemplified by Aryl Fluorosulfates
- (2017) David E. Mortenson et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Selective lysine modification of native peptides via aza-Michael addition
- (2017) Hongli Chen et al. ORGANIC & BIOMOLECULAR CHEMISTRY
- Targeted Covalent Inhibitors for Drug Design
- (2016) Thomas A. Baillie ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Cathepsin K osteoporosis trials, pycnodysostosis and mouse deficiency models: Commonalities and differences
- (2016) Dieter Brömme et al. Expert Opinion on Drug Discovery
- Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions
- (2016) Paul A. Jackson et al. JOURNAL OF MEDICINAL CHEMISTRY
- Metabolically Labile Fumarate Esters Impart Kinetic Selectivity to Irreversible Inhibitors
- (2016) Balyn W. Zaro et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Identification of Covalent Binding Sites Targeting Cysteines Based on Computational Approaches
- (2016) Yanmin Zhang et al. MOLECULAR PHARMACEUTICS
- Proteome-wide covalent ligand discovery in native biological systems
- (2016) Keriann M. Backus et al. NATURE
- Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain
- (2016) Gizem Akçay et al. Nature Chemical Biology
- Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism
- (2016) P. Lito et al. SCIENCE
- Covalent tethering of fragments for covalent probe discovery
- (2016) Stefan G. Kathman et al. MedChemComm
- Intrinsic reactivity profile of electrophilic moieties to guide covalent drug design: N-α-acetyl-l-lysine as an amine nucleophile
- (2016) Upendra P. Dahal et al. MedChemComm
- Screening for covalent inhibitors using DNA-display of small molecule libraries functionalized with cysteine reactive moieties
- (2016) C. Zambaldo et al. MedChemComm
- Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State
- (2016) M. P. Patricelli et al. Cancer Discovery
- Novel reversible selective inhibitor of nuclear export shows that CRM1 is a target in colorectal cancer cells
- (2015) Mingshan Niu et al. CANCER BIOLOGY & THERAPY
- Identification and Characterization of an Irreversible Inhibitor of CDK2
- (2015) Elizabeth Anscombe et al. CHEMISTRY & BIOLOGY
- Identifying Drug-Target Selectivity of Small-Molecule CRM1/XPO1 Inhibitors by CRISPR/Cas9 Genome Editing
- (2015) Jasper E. Neggers et al. CHEMISTRY & BIOLOGY
- FDA Approval: Ibrutinib for Patients with Previously Treated Mantle Cell Lymphoma and Previously Treated Chronic Lymphocytic Leukemia
- (2015) R. A. de Claro et al. CLINICAL CANCER RESEARCH
- Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies
- (2015) Renato A. Bauer DRUG DISCOVERY TODAY
- Systematic Study of the Glutathione (GSH) Reactivity of N-Arylacrylamides: 1. Effects of Aryl Substitution
- (2015) Victor J. Cee et al. JOURNAL OF MEDICINAL CHEMISTRY
- Theory and Applications of Covalent Docking in Drug Discovery: Merits and Pitfalls
- (2015) Hezekiel Kumalo et al. MOLECULES
- The FTMap family of web servers for determining and characterizing ligand-binding hot spots of proteins
- (2015) Dima Kozakov et al. Nature Protocols
- The drug–target residence time model: a 10-year retrospective
- (2015) Robert A. Copeland NATURE REVIEWS DRUG DISCOVERY
- Covalent docking using autodock: Two-point attractor and flexible side chain methods
- (2015) Giulia Bianco et al. PROTEIN SCIENCE
- Sulfur(VI) Fluoride Exchange (SuFEx): Another Good Reaction for Click Chemistry
- (2014) Jiajia Dong et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Docking Covalent Inhibitors: A Parameter Free Approach To Pose Prediction and Scoring
- (2014) Kai Zhu et al. Journal of Chemical Information and Modeling
- Chemical and Computational Methods for the Characterization of Covalent Reactive Groups for the Prospective Design of Irreversible Inhibitors
- (2014) Mark E. Flanagan et al. JOURNAL OF MEDICINAL CHEMISTRY
- A Chemical Tuned Strategy to Develop Novel Irreversible EGFR-TK Inhibitors with Improved Safety and Pharmacokinetic Profiles
- (2014) Guangxin Xia et al. JOURNAL OF MEDICINAL CHEMISTRY
- Chemistry: Chemical con artists foil drug discovery
- (2014) Jonathan Baell et al. NATURE
- Covalent docking of large libraries for the discovery of chemical probes
- (2014) Nir London et al. Nature Chemical Biology
- Therapeutic Targeting of Oncogenic K-Ras by a Covalent Catalytic Site Inhibitor
- (2013) Sang Min Lim et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Drug discovery considerations in the development of covalent inhibitors
- (2013) Robert Mah et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Afatinib: First Global Approval
- (2013) Rosselle T. Dungo et al. DRUGS
- K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions
- (2013) Jonathan M. Ostrem et al. NATURE
- Reversible Covalent Inhibition of a Protein Target
- (2012) Chang-Uk Lee et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- A Comprehensive Survey of Ras Mutations in Cancer
- (2012) I. A. Prior et al. CANCER RESEARCH
- Drug discovery for a new generation of covalent drugs
- (2012) Amit S Kalgutkar et al. Expert Opinion on Drug Discovery
- CovalentDock: Automated covalent docking with parameterized covalent linkage energy estimation and molecular geometry constraints
- (2012) Xuchang Ouyang et al. JOURNAL OF COMPUTATIONAL CHEMISTRY
- Consensus Induced Fit Docking (cIFD): methodology, validation, and application to the discovery of novel Crm1 inhibitors
- (2012) Ori Kalid et al. JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN
- Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles
- (2012) Iana M Serafimova et al. Nature Chemical Biology
- An efficient randomised, placebo-controlled clinical trial with the irreversible fatty acid amide hydrolase-1 inhibitor PF-04457845, which modulates endocannabinoids but fails to induce effective analgesia in patients with pain due to osteoarthritis of the knee
- (2012) John P. Huggins et al. PAIN
- Measurement and Estimation of Electrophilic Reactivity for Predictive Toxicology
- (2011) Johannes A. H. Schwöbel et al. CHEMICAL REVIEWS
- Diazabicyclooctanes (DBOs): a potent new class of non-β-lactam β-lactamase inhibitors
- (2011) Ken Coleman CURRENT OPINION IN MICROBIOLOGY
- The resurgence of covalent drugs
- (2011) Juswinder Singh et al. NATURE REVIEWS DRUG DISCOVERY
- Quantitative reactivity profiling predicts functional cysteines in proteomes
- (2010) Eranthie Weerapana et al. NATURE
- Covalent Modifiers: An Orthogonal Approach to Drug Design
- (2009) Michele H. Potashman et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structural basis for leucine-rich nuclear export signal recognition by CRM1
- (2009) Xiuhua Dong et al. NATURE
- Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: Structure–activity relationship and mechanism of action
- (2008) Tine Van Neck et al. BIOORGANIC & MEDICINAL CHEMISTRY
- Disparate proteome reactivity profiles of carbon electrophiles
- (2008) Eranthie Weerapana et al. Nature Chemical Biology
- BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models
- (2008) D Li et al. ONCOGENE
Find the ideal target journal for your manuscript
Explore over 38,000 international journals covering a vast array of academic fields.
SearchAsk a Question. Answer a Question.
Quickly pose questions to the entire community. Debate answers and get clarity on the most important issues facing researchers.
Get Started