4.5 Article

Proteome-wide Identification of Off-Targets of a Potent EGFRL858R/T790M Mutant Inhibitor

Related references

Note: Only part of the references are listed.
Article Chemistry, Medicinal

Novel Electrophilic Warhead Targeting a Triple-Negative Breast Cancer Driver in Live Cells Revealed by Inverse Drug Discovery

Youlong Fan et al.

Summary: The inverse drug discovery strategy utilizing cyclopropenone as a potent electrophile has led to the specific and efficient modification of the triple-negative breast cancer driver GSTP1 in live cells, resulting in the discovery of potential inhibitors through further optimization and pathway validation.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Review Biochemistry & Molecular Biology

Recent advances in identifying protein targets in drug discovery

Jaeyoung Ha et al.

Summary: Phenotype-based screening is a promising method for discovering first-in-class therapeutics, but understanding the mode of action has been a bottleneck for drug discovery. Recent strategies including covalent conjugation and label-free target identification have emerged to overcome limitations in target protein identification, leading to significant advancements in the field.

CELL CHEMICAL BIOLOGY (2021)

Review Chemistry, Multidisciplinary

Applications of Activity-Based Protein Profiling (ABPP) and Bioimaging in Drug Discovery

Jiaqian Xu et al.

CHEMISTRY-AN ASIAN JOURNAL (2020)

Article Chemistry, Multidisciplinary

2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells

Nan Ma et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)

Review Chemistry, Medicinal

Irreversible Kinase Inhibitors Targeting Cysteine Residues and their Applications in Cancer Therapy

Debasis Das et al.

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2020)

Article Chemistry, Multidisciplinary

Photocaged Cell-Permeable Ubiquitin Probe for Temporal Profiling of Deubiquitinating Enzymes

Weijun Gui et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)

Article Chemistry, Analytical

An Unbiased Immunoaffinity-Based Strategy for Profiling Covalent Drug Targets In Vivo

Xinyuan Wang et al.

ANALYTICAL CHEMISTRY (2019)

Review Chemistry, Multidisciplinary

The Cysteinome of Protein Kinases as a Target in Drug Development

Apirat Chaikuad et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2018)

Article Biochemistry & Molecular Biology

Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors

Sherry Niessen et al.

CELL CHEMICAL BIOLOGY (2017)

Article Psychiatry

Exome chip analyses in adult attention deficit hyperactivity disorder

T. Zayats et al.

TRANSLATIONAL PSYCHIATRY (2016)