Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain

Interactions of the Natural Product (+)-Avrainvillamide with Nucleophosmin and Exportin-1 Mediate the Cellular Localization of Nucleophosmin and its AML-Associated Mutants

(2015) Herschel Mukherjee et al.   ACS Chemical Biology

Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR

(2015) Debjit Basu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Identification and Characterization of an Irreversible Inhibitor of CDK2

(2015) Elizabeth Anscombe et al.   CHEMISTRY & BIOLOGY

Reversible Lysine Modification on Proteins by Using Functionalized Boronic Acids

(2015) Pedro M. S. D. Cal et al.   CHEMISTRY-A EUROPEAN JOURNAL

Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity

(2015) Milan Bruncko et al.   JOURNAL OF MEDICINAL CHEMISTRY

BH3 profiling identifies heterogeneous dependency on Bcl-2 family members in multiple myeloma and predicts sensitivity to BH3 mimetics

(2015) C Touzeau et al.   LEUKEMIA

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

Small molecule Mcl-1 inhibitors for the treatment of cancer

(2015) Johannes Belmar et al.   PHARMACOLOGY & THERAPEUTICS

Targeting bacteria via iminoboronate chemistry of amine-presenting lipids

(2015) Anupam Bandyopadhyay et al.   Nature Communications

Bcl-2 family proteins in breast development and cancer: could Mcl-1 targeting overcome therapeutic resistance?

(2015) Michelle M. Williams et al.   Oncotarget

Selective Inhibition of Mutant Ras Protein through Covalent Binding

(2014) Joachim Rudolph et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor

(2014) M. Raymond V. Finlay et al.   JOURNAL OF MEDICINAL CHEMISTRY

Overexpression of Mcl-1L Splice Variant Is Associated with Poor Prognosis and Chemoresistance in Oral Cancers

(2014) Vinayak Palve et al.   PLoS One

MCL1 and BCL-xL Levels in Solid Tumors Are Predictive of Dinaciclib-Induced Apoptosis

(2014) Robert N. Booher et al.   PLoS One

Drug discovery considerations in the development of covalent inhibitors

(2013) Robert Mah et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of Potent Mcl-1/Bcl-xL Dual Inhibitors by Using a Hybridization Strategy Based on Structural Analysis of Target Proteins

(2013) Yuta Tanaka et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of α-helix-mediated protein–protein interactions using designed molecules

(2013) Valeria Azzarito et al.   Nature Chemistry

Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy

(2013) Peter E. Czabotar et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

BAD Dephosphorylation and Decreased Expression of MCL-1 Induce Rapid Apoptosis in Prostate Cancer Cells

(2013) Dana Yancey et al.   PLoS One

Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

(2013) A. O. Walter et al.   Cancer Discovery

Reversible Covalent Inhibition of a Protein Target

(2012) Chang-Uk Lee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Chemical Genomics Identifies Small-Molecule MCL1 Repressors and BCL-xL as a Predictor of MCL1 Dependency

(2012) Guo Wei et al.   CANCER CELL

A Competitive Stapled Peptide Screen Identifies a Selective Small Molecule that Overcomes MCL-1-Dependent Leukemia Cell Survival

(2012) Nicole A. Cohen et al.   CHEMISTRY & BIOLOGY

Irreversible Protein Kinase Inhibitors: Balancing the Benefits and Risks

(2012) Tjeerd Barf et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design

(2012) Anders Friberg et al.   JOURNAL OF MEDICINAL CHEMISTRY

Iminoboronates: A New Strategy for Reversible Protein Modification

(2012) Pedro M. S. D. Cal et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Rational Design of Proteolytically Stable, Cell-Permeable Peptide-Based Selective Mcl-1 Inhibitors

(2012) Avinash Muppidi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

MCL1 is deregulated in subgroups of diffuse large B-cell lymphoma

(2012) S-S Wenzel et al.   LEUKEMIA

Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles

(2012) Iana M Serafimova et al.   Nature Chemical Biology

The resurgence of covalent drugs

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

Targeting protein–protein interactions for therapeutic intervention: a challenge for the future

(2010) Giovanna Zinzalla et al.   Future Medicinal Chemistry

Determinants of BH3 Binding Specificity for Mcl-1 versus Bcl-xL

(2010) Sanjib Dutta et al.   JOURNAL OF MOLECULAR BIOLOGY

The landscape of somatic copy-number alteration across human cancers

(2010) Rameen Beroukhim et al.   NATURE

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

(2010) Sungwook Choi et al.   Nature Chemical Biology

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

(2008) Peter J. Tummino et al.   BIOCHEMISTRY

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

Directing cancer cells to self-destruct with pro-apoptotic receptor agonists

(2008) Avi Ashkenazi   NATURE REVIEWS DRUG DISCOVERY