Covalent peptides and proteins for therapeutics

Covalent Targeting of Ras G12C by Rationally Designed Peptidomimetics

(2020) Daniel Y. Yoo et al.   ACS Chemical Biology

Developing Covalent Protein Drugs via Proximity-Enabled Reactive Therapeutics

(2020) Qingke Li et al.   CELL

Macrocyclic Peptides as Drug Candidates: Recent Progress and Remaining Challenges

(2019) Alexander A. Vinogradov 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

Genetically Introducing Biochemically Reactive Amino Acids Dehydroalanine and Dehydrobutyrine in Proteins

(2019) Bing Yang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Genetically Encoding Photocaged Quinone Methide to Multitarget Protein Residues Covalently in Vivo

(2019) Jun Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Stapled Peptides—A Useful Improvement for Peptide-Based Drugs

(2019) Mattia Moiola et al.   MOLECULES

Immune checkpoint blockade therapy for cancer: An overview of FDA-approved immune checkpoint inhibitors

(2018) Kristian M. Hargadon et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach

(2018) Carlo Baggio et al.   JOURNAL OF MEDICINAL CHEMISTRY

Site-Specific Incorporation of Selenocysteine Using an Expanded Genetic Code and Palladium-Mediated Chemical Deprotection

(2018) Jun Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Genetically Encoding Fluorosulfate-l-tyrosine To React with Lysine, Histidine, and Tyrosine via SuFEx in Proteins in Vivo

(2018) Nanxi Wang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

“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

A semi-synthetic organism that stores and retrieves increased genetic information

(2017) Yorke Zhang et al.   NATURE

Genetically encoding new bioreactivity

(2017) Lei Wang   New Biotechnology

Spontaneous and specific chemical cross-linking in live cells to capture and identify protein interactions

(2017) Bing Yang et al.   Nature Communications

Genetic Incorporation of a Reactive Isothiocyanate Group into Proteins

(2016) Weimin Xuan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Targeted Covalent Inhibitors for Drug Design

(2016) Thomas A. Baillie   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Proximity-enabled bioreactivity to generate covalent peptide inhibitors of p53–Mdm4

(2016) Christian Hoppmann et al.   CHEMICAL COMMUNICATIONS

Using Protein-Confined Proximity To Determine Chemical Reactivity

(2016) Tomonori Kobayashi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Arylfluorosulfates Inactivate Intracellular Lipid Binding Protein(s) through Chemoselective SuFEx Reaction with a Binding Site Tyr Residue

(2016) Wentao Chen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Accurate de novo design of hyperstable constrained peptides

(2016) Gaurav Bhardwaj et al.   NATURE

Electrophilic Helical Peptides That Bond Covalently, Irreversibly, and Selectively in a Protein–Protein Interaction Site

(2016) Aline Dantas de Araujo et al.   ACS Medicinal Chemistry Letters

Hydrocarbon Stapled Peptides as Modulators of Biological Function

(2015) Philipp M. Cromm et al.   ACS Chemical Biology

Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies

(2015) Renato A. Bauer   DRUG DISCOVERY TODAY

In Situ Formation of an Azo Bridge on Proteins Controllable by Visible Light

(2015) Christian Hoppmann et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A two-component 'double-click' approach to peptide stapling

(2015) Yu Heng Lau et al.   Nature Protocols

The drug–target residence time model: a 10-year retrospective

(2015) Robert A. Copeland   NATURE REVIEWS DRUG DISCOVERY

Sulfonyl fluorides as privileged warheads in chemical biology

(2015) Arjun Narayanan et al.   Chemical Science

Genetically Encoding an Electrophilic Amino Acid for Protein Stapling and Covalent Binding to Native Receptors

(2014) Xiao-Hua Chen et al.   ACS Chemical Biology

Sulfur(VI) Fluoride Exchange (SuFEx): Another Good Reaction for Click Chemistry

(2014) Jiajia Dong et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Proximity-Enabled Protein Crosslinking through Genetically Encoding Haloalkane Unnatural Amino Acids

(2014) Zheng Xiang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Genetically Encoding Photoswitchable Click Amino Acids inEscherichia coliand Mammalian Cells

(2014) Christian Hoppmann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Modulators of Protein–Protein Interactions

(2014) Lech-Gustav Milroy et al.   CHEMICAL REVIEWS

Hydrocarbon-Stapled Peptides: Principles, Practice, and Progress

(2014) Loren D. Walensky et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Genetically Encoded aza-Michael Acceptor for Covalent Cross-Linking of Protein–Receptor Complexes

(2014) Jennifer L. Furman et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structure-Based Design of Covalent Siah Inhibitors

(2013) John L. Stebbins et al.   CHEMISTRY & BIOLOGY

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

(2013) Jonathan M. Ostrem et al.   NATURE

Adding an unnatural covalent bond to proteins through proximity-enhanced bioreactivity

(2013) Zheng Xiang et al.   NATURE METHODS

Plucking the high hanging fruit: A systematic approach for targeting protein–protein interactions

(2012) Monika Raj et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Expanding the Number of ‘Druggable’ Targets: Non-Enzymes and Protein-Protein Interactions

(2012) Leah N. Makley et al.   Chemical Biology & Drug Design

The Future of Peptide-based Drugs

(2012) David J. Craik et al.   Chemical Biology & Drug Design

Molecular Pathways: Targeting Mdm2 and Mdm4 in Cancer Therapy

(2012) Q. Li et al.   CLINICAL CANCER RESEARCH

RF1 knockout allows ribosomal incorporation of unnatural amino acids at multiple sites

(2011) David B F Johnson et al.   Nature Chemical Biology

The resurgence of covalent drugs

(2011) Juswinder Singh et al.   NATURE REVIEWS DRUG DISCOVERY

Adding New Chemistries to the Genetic Code

(2010) Chang C. Liu et al.   Annual Review of Biochemistry

Photoreactive Stapled BH3 Peptides to Dissect the BCL-2 Family Interactome

(2010) Craig R. Braun et al.   CHEMISTRY & BIOLOGY

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

(2010) Douglas S Johnson et al.   Future Medicinal Chemistry

Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine

(2010) Margit Hagel et al.   Nature Chemical Biology

Electrophilic Affibodies Forming Covalent Bonds to Protein Targets

(2009) Lotta Holm et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Covalent Modifiers: An Orthogonal Approach to Drug Design

(2009) Michele H. Potashman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Genetic Incorporation of a Small, Environmentally Sensitive, Fluorescent Probe into Proteins inSaccharomyces cerevisiae

(2009) Hyun Soo Lee et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A Hydrogen Bond Surrogate Approach for Stabilization of Short Peptide Sequences in α-Helical Conformation

(2008) Anupam Patgiri et al.   ACCOUNTS OF CHEMICAL RESEARCH

Beyond Picomolar Affinities: Quantitative Aspects of Noncovalent and Covalent Binding of Drugs to Proteins

(2008) Adam J. T. Smith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protein therapeutics: a summary and pharmacological classification

(2007) Benjamin Leader et al.   NATURE REVIEWS DRUG DISCOVERY