The resurgence of covalent drugs

Iniparib plus Chemotherapy in Metastatic Triple-Negative Breast Cancer

(2011) Joyce O'Shaughnessy et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Structure-Guided Approach to Creating Covalent FGFR Inhibitors

(2010) Wenjun Zhou et al.   CHEMISTRY & BIOLOGY

Targeted covalent drugs of the kinase family

(2010) Juswinder Singh et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Drug–target residence time: critical information for lead optimization

(2010) Hao Lu et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Characterization of HKI-272 Covalent Binding to Human Serum Albumin

(2010) J. Wang et al.   DRUG METABOLISM AND DISPOSITION

Efficacy of abiraterone acetate in post-docetaxel castration-resistant prostate cancer

(2010) Paraskevi Vogiatzi et al.   Expert Review of Anticancer Therapy

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

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

Seguridad e interacciones de los inhibidores de la bomba de protones: lecciones aprendidas en millones de pacientes

(2010) Juan V. Esplugues et al.   Gastroenterologia y Hepatologia

Phase I Clinical Trial of the CYP17 Inhibitor Abiraterone Acetate Demonstrating Clinical Activity in Patients With Castration-Resistant Prostate Cancer Who Received Prior Ketoconazole Therapy

(2010) Charles J. Ryan et al.   JOURNAL OF CLINICAL ONCOLOGY

Neratinib, an Irreversible ErbB Receptor Tyrosine Kinase Inhibitor, in Patients With Advanced ErbB2-Positive Breast Cancer

(2010) Harold J. Burstein et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Trial of the Irreversible EGFR and HER2 Kinase Inhibitor BIBW 2992 in Patients With Advanced Solid Tumors

(2010) Timothy A. Yap et al.   JOURNAL OF CLINICAL ONCOLOGY

Efficacy of boceprevir, an NS3 protease inhibitor, in combination with peginterferon alfa-2b and ribavirin in treatment-naive patients with genotype 1 hepatitis C infection (SPRINT-1): an open-label, randomised, multicentre phase 2 trial

(2010) Paul Y Kwo et al.   LANCET

Chemoselective small molecules that covalently modify one lysine in a non-enzyme protein in plasma

(2010) Sungwook Choi et al.   Nature Chemical Biology

Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine

(2010) Margit Hagel et al.   Nature Chemical Biology

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

(2010) L. A. Honigberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery and Characterization of a Highly Selective FAAH Inhibitor that Reduces Inflammatory Pain

(2009) Kay Ahn et al.   CHEMISTRY & BIOLOGY

A Phase 1 Dose Escalation Study of the Safety and Pharmacokinetics of the Novel Proteasome Inhibitor Carfilzomib (PR-171) in Patients with Hematologic Malignancies

(2009) O. A. O'Connor et al.   CLINICAL CANCER RESEARCH

Covalent Modifiers: An Orthogonal Approach to Drug Design

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

The Development of HKI‐272 and Related Compounds for the Treatment of Cancer

(2008) Allan Wissner et al.   ARCHIV DER PHARMAZIE

Residence Time of Receptor−Ligand Complexes and Its Effect on Biological Function

(2008) Peter J. Tummino et al.   BIOCHEMISTRY

Immune-Mediated Adverse Drug Reactions

(2008) Jack Uetrecht   CHEMICAL RESEARCH IN TOXICOLOGY

Relationship between daily dose of oral medications and idiosyncratic drug-induced liver injury: Search for signals

(2008) Craig Lammert et al.   HEPATOLOGY

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

Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor

(2008) A. J. Gonzales et al.   MOLECULAR CANCER THERAPEUTICS

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

(2008) C.-H. Yun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Protein Damage by Reactive Electrophiles: Targets and Consequences

(2007) Daniel C. Liebler   CHEMICAL RESEARCH IN TOXICOLOGY