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Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro- N 2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)- N 4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

Journal of medicinal chemistry, 2013-07, Vol.56 (14), p.5675-5690

2013

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Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5‑Chloro‑N2‑(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)‑N4‑(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

Journal of medicinal chemistry, 2013-07, Vol.56 (14), p.5675-5690

2013

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Midazolam Oxidation by Cytochrome P450 3A4 and Active-Site Mutants: an Evaluation of Multiple Binding Sites and of the Metabolic Pathway That Leads to Enzyme Inactivation

Molecular pharmacology, 2002-03, Vol.61 (3), p.495-506

2002

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Dual ALK and CDK4/6 Inhibition Demonstrates Synergy against Neuroblastoma

Clinical cancer research, 2017-06, Vol.23 (11), p.2856-2868

2017

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A modern in vivo pharmacokinetic paradigm: combining snapshot, rapid and full PK approaches to optimize and expedite early drug discovery

Drug discovery today, 2013-01, Vol.18 (1-2), p.71-78

2013

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Differential oxidation of mifepristone by cytochromes P450 3A4 and 3A5: selective inactivation of P450 3A4

Drug metabolism and disposition, 2002-09, Vol.30 (9), p.985-990

2002

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Mutagenesis and molecular dynamics suggest structural and functional roles for residues in the N-terminal portion of the cytochrome P450 2B1 I helix

Archives of biochemistry and biophysics, 2004-03, Vol.423 (2), p.266-276

2004

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Topological changes in the CYP3A4 active site probed with phenyldiazene: effect of interaction with NADPH-cytochrome P450 reductase and cytochrome b5 and of site-directed mutagenesis

Drug metabolism and disposition, 2004-01, Vol.32 (1), p.155

2004

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Amino Acid Residues Critical for Differential Inhibition of CYP2B4, CYP2B5, and CYP2B1 by Phenylimidazoles

Molecular pharmacology, 2001-03, Vol.59 (3), p.475-484

2001

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Site-Directed Mutagenesis of Cytochrome P450eryF: Implications for Substrate Oxidation, Cooperativity, and Topology of the Active Site

Chemical research in toxicology, 2002-06, Vol.15 (6), p.843-853

2002

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The Role of Cytochrome 2B1 Substrate Recognition Site Residues 115, 294, 297, 298, and 362 in the Oxidation of Steroids and 7-Alkoxycoumarins

Archives of biochemistry and biophysics, 2001-10, Vol.394 (1), p.21-28

2001

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Escherichia coli Expression of Site-Directed Mutants of Cytochrome P450 2B1 from Six Substrate Recognition Sites: Substrate Specificity and Inhibitor Selectivity Studies

Chemical research in toxicology, 1995-06, Vol.8 (4), p.574-579

1995

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Identification of selective mechanism-based inactivators of cytochromes P-450 2B4 and 2B5, and determination of the molecular basis for differential susceptibility

The Journal of pharmacology and experimental therapeutics, 1999-07, Vol.290 (1), p.445

1999

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Identification of Three Key Residues in Substrate Recognition Site 5 of Human Cytochrome P450 3A4 by Cassette and Site-Directed Mutagenesis

Biochemistry (Easton), 1997-07, Vol.36 (29), p.8831-8839

1997

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Abstract 1000: Combination CDK4/6 and ALK inhibition demonstrates on-target synergy against neuroblastoma

Cancer research (Chicago, Ill.), 2014-10, Vol.74 (19_Supplement), p.1000-1000

2014

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Abstract B42: Combinatorial CDK4/6 and ALK inhibition demonstrates on-target synergy against neuroblastoma

Cancer research (Chicago, Ill.), 2014-10, Vol.74 (20_Supplement), p.B42-B42

2014

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The genetic determinants of the CYP3A5 polymorphism

Pharmacogenetics (London), 2001-12, Vol.11 (9), p.773-779

2001

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TOPOLOGICAL CHANGES IN THE CYP3A4 ACTIVE SITE PROBED WITH PHENYLDIAZENE: EFFECT OF INTERACTION WITH NADPH-CYTOCHROME P450 REDUCTASE AND CYTOCHROME B 5 AND OF SITE-DIRECTED MUTAGENESIS

Drug metabolism and disposition, 2004-01, Vol.32 (1), p.155-161

2004

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An Electrostatically Driven Conformational Transition Is Involved in the Mechanisms of Substrate Binding and Cooperativity in Cytochrome P450eryF

Biochemistry (Easton), 2004-06, Vol.43 (21), p.6475-6485

2004

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Elucidation of Amino Acid Residues Critical for Unique Activities of Rabbit Cytochrome P450 2B5 Using Hybrid Enzymes and Reciprocal Site-Directed Mutagenesis with Rabbit Cytochrome P450 2B4

Archives of biochemistry and biophysics, 1996-03, Vol.327 (2), p.308-318

1996

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Interconversion of the Androstenedione Hydroxylase Specificities of Cytochromes P450 2B4 and 2B5 upon Simultaneous Site-Directed Mutagenesis of Four Key Substrate Recognition Residues

Archives of biochemistry and biophysics, 1996-11, Vol.335 (1), p.152-160

1996

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Importance of Amino Acid Residue 474 for Substrate Specificity of Canine and Human Cytochrome P450 3A Enzymes

Archives of biochemistry and biophysics, 2001-05, Vol.389 (2), p.264-270

2001

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Structural Determinants of Progesterone Hydroxylation by Cytochrome P450 2B5: The Role of Nonsubstrate Recognition Site Residues

Archives of biochemistry and biophysics, 1998-02, Vol.350 (2), p.333-339

1998

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Use of chimeric enzymes and site-directed mutagenesis for identification of three key residues responsible for differences in steroid hydroxylation between canine cytochromes P-450 3A12 and 3A26

Molecular pharmacology, 1999-02, Vol.55 (2), p.241-247

1999

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Substrate Routes to the Buried Active Site May Vary among Cytochromes P450: Mutagenesis of the F−G Region in P450 2B1

Chemical research in toxicology, 2002-11, Vol.15 (11), p.1407-1413

2002

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Midazolam Oxidation by Cytochrome P450 3A4 and Active-Site Mutants: an Evaluation of Multiple Binding Sites and of the Metabolic Pathway That Leads to Enzyme Inactivation

Dual ALK and CDK4/6 Inhibition Demonstrates Synergy against Neuroblastoma

A modern in vivo pharmacokinetic paradigm: combining snapshot, rapid and full PK approaches to optimize and expedite early drug discovery

Differential oxidation of mifepristone by cytochromes P450 3A4 and 3A5: selective inactivation of P450 3A4

Mutagenesis and molecular dynamics suggest structural and functional roles for residues in the N-terminal portion of the cytochrome P450 2B1 I helix

Topological changes in the CYP3A4 active site probed with phenyldiazene: effect of interaction with NADPH-cytochrome P450 reductase and cytochrome b5 and of site-directed mutagenesis

Amino Acid Residues Critical for Differential Inhibition of CYP2B4, CYP2B5, and CYP2B1 by Phenylimidazoles

Site-Directed Mutagenesis of Cytochrome P450eryF: Implications for Substrate Oxidation, Cooperativity, and Topology of the Active Site

The Role of Cytochrome 2B1 Substrate Recognition Site Residues 115, 294, 297, 298, and 362 in the Oxidation of Steroids and 7-Alkoxycoumarins

Escherichia coli Expression of Site-Directed Mutants of Cytochrome P450 2B1 from Six Substrate Recognition Sites: Substrate Specificity and Inhibitor Selectivity Studies

Identification of selective mechanism-based inactivators of cytochromes P-450 2B4 and 2B5, and determination of the molecular basis for differential susceptibility

Identification of Three Key Residues in Substrate Recognition Site 5 of Human Cytochrome P450 3A4 by Cassette and Site-Directed Mutagenesis

Abstract 1000: Combination CDK4/6 and ALK inhibition demonstrates on-target synergy against neuroblastoma

Abstract B42: Combinatorial CDK4/6 and ALK inhibition demonstrates on-target synergy against neuroblastoma

The genetic determinants of the CYP3A5 polymorphism

TOPOLOGICAL CHANGES IN THE CYP3A4 ACTIVE SITE PROBED WITH PHENYLDIAZENE: EFFECT OF INTERACTION WITH NADPH-CYTOCHROME P450 REDUCTASE AND CYTOCHROME B 5 AND OF SITE-DIRECTED MUTAGENESIS

An Electrostatically Driven Conformational Transition Is Involved in the Mechanisms of Substrate Binding and Cooperativity in Cytochrome P450eryF

Elucidation of Amino Acid Residues Critical for Unique Activities of Rabbit Cytochrome P450 2B5 Using Hybrid Enzymes and Reciprocal Site-Directed Mutagenesis with Rabbit Cytochrome P450 2B4

Interconversion of the Androstenedione Hydroxylase Specificities of Cytochromes P450 2B4 and 2B5 upon Simultaneous Site-Directed Mutagenesis of Four Key Substrate Recognition Residues

Importance of Amino Acid Residue 474 for Substrate Specificity of Canine and Human Cytochrome P450 3A Enzymes

Structural Determinants of Progesterone Hydroxylation by Cytochrome P450 2B5: The Role of Nonsubstrate Recognition Site Residues

Use of chimeric enzymes and site-directed mutagenesis for identification of three key residues responsible for differences in steroid hydroxylation between canine cytochromes P-450 3A12 and 3A26

Substrate Routes to the Buried Active Site May Vary among Cytochromes P450: Mutagenesis of the F−G Region in P450 2B1

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