S. Middleton

发表

The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases.

S. Emanuel, C. Rugg, R. H. Gruninger, 2005, Cancer research.

3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.

S. Emanuel, R. H. Gruninger, R. Lin, 2005, Bioorganic & medicinal chemistry letters.

Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases.

Mary Adams, Niranjan Pandey, Terry V Hughes, 2008, Bioorganic & medicinal chemistry letters.

Chemotherapy-free, triple combination of obinutuzumab, venetoclax and idasanutlin: antitumor activity in xenograft models of non-Hodgkin lymphoma

C. Klein, S. Middleton, F. Herting, 2018, Leukemia & lymphoma.

Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).

S. Emanuel, R. H. Gruninger, Angel R. Fuentes-Pesquera, 2007, Bioorganic & medicinal chemistry letters.

Recent advances towards the discovery of ORL-1 receptor agonists and antagonists

G. Bignan, P. Connolly, S. Middleton, 2005 .

Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.

S. Emanuel, P. Connolly, L. Jolliffe, 2003, Journal of medicinal chemistry.

Identification of a Critical Ligand Binding Determinant of the Human Erythropoietin Receptor

R. H. Gruninger, L. Jolliffe, S. Middleton, 1996, The Journal of Biological Chemistry.

Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.

S. Emanuel, R. Lin, P. Connolly, 2007, Bioorganic & medicinal chemistry letters.

Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.

P. Connolly, S. Middleton, K. Mayo, 2007, Journal of medicinal chemistry.

Structural consequences of a one atom mutation on aspartate transcarbamylase from E. coli

J. Cherfils, R. Sweet, E. Kantrowitz, 1989, FEBS letters.

A loop involving catalytic chain residues 230-245 is essential for the stabilization of both allosteric forms of Escherichia coli aspartate transcarbamylase.

E. Kantrowitz, S. Middleton, J. Stebbins, 1989, Biochemistry.

Function of arginine-234 and aspartic acid-271 in domain closure, cooperativity, and catalysis in Escherichia coli aspartate transcarbamylase.

E. Kantrowitz, S. Middleton, 1988, Biochemistry.

Propagation of allosteric changes through the catalytic-regulatory interface of Escherichia coli aspartate transcarbamylase.

E. Kantrowitz, W. Xu, S. Middleton, 1988, Biochemistry.

Involvement of tryptophan 209 in the allosteric interactions of Escherichia coli aspartate transcarbamylase using single amino acid substitution mutants.

E. Kantrowitz, S. Middleton, K. Smith, 1986, Journal of molecular biology.

Synthesis, In Vitro Activities of (2-Cyclopropoxyphenyl)piperidine Derivatives for α1a and α1d Adrenergic Receptor Inhibitors

P. Connolly, S. Middleton, V. Pulito, 2009 .

(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).

P. Connolly, S. Middleton, V. Pulito, 2007, Bioorganic & medicinal chemistry letters.

Structural consequences of the replacement of Glu239 by Gln in the catalytic chain of Escherichia coli aspartate transcarbamylase.

E. Kantrowitz, P. Vachette, P. Tauc, 1990, Journal of molecular biology.

Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.

S. Emanuel, R. Lin, P. Connolly, 2006, Bioorganic & medicinal chemistry letters.

1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.

S. Emanuel, C. Rugg, R. H. Gruninger, 2005, Journal of medicinal chemistry.

3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.

G. Bignan, P. Connolly, S. Middleton, 2006, Bioorganic & medicinal chemistry letters.

Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.

S. Emanuel, R. H. Gruninger, Angel R. Fuentes-Pesquera, 2005, Journal of medicinal chemistry.

Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.

S. Emanuel, R. H. Gruninger, Angel R. Fuentes-Pesquera, 2005, Journal of medicinal chemistry.

Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.

S. Emanuel, R. H. Gruninger, R. Lin, 2007, Bioorganic & medicinal chemistry letters.

3-(4-Piperidinyl)indoles and 3-(4-Piperidinyl)pyrrolo[2,3-b]pyridines as Ligands for the ORL-1 Receptor.

G. Bignan, P. Connolly, S. Middleton, 2006 .

Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.

G. Bignan, P. Connolly, S. Middleton, 2005, Bioorganic & medicinal chemistry letters.

A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety.

G. Bignan, P. Connolly, S. Middleton, 2015, Bioorganic & medicinal chemistry letters.

(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.

Jian Li, Judith Baker, Hong-tao Lu, 2005, Journal of medicinal chemistry.

4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.

S. Emanuel, R. H. Gruninger, R. Lin, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.

R. Lin, Angel R. Fuentes-Pesquera, P. Connolly, 2009, Bioorganic & medicinal chemistry letters.

Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.

Xin Chen, Yan Zhang, S. Emanuel, 2005, Journal of medicinal chemistry.

Function of arginine-166 in the active site of Escherichia coli alkaline phosphatase.

E. Kantrowitz, S. Middleton, A. Chaidaroglou, 1988, Biochemistry.

Relationship between domain closure and binding, catalysis, and regulation in Escherichia coli aspartate transcarbamylase.

E. Kantrowitz, S. Middleton, M. Ladjimi, 1988, Biochemistry.

Crystallographic evidence for preformed dimers of erythropoietin receptor before ligand activation.

I. Wilson, O. Livnah, E. Stura, 1999, Science.

Shared and Unique Determinants of the Erythropoietin (EPO) Receptor Are Important for Binding EPO and EPO Mimetic Peptide*

I. Wilson, R. Thurmond, M. Goldsmith, 1999, The Journal of Biological Chemistry.

Acute myeloid leukemia patients’ clinical response to idasanutlin (RG7388) is associated with pre-treatment MDM2 protein expression in leukemic blasts

Michel Theron, W. Pierceall, B. Reis, 2016, Haematologica.

A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity.

S. Emanuel, P. Connolly, S. K. Wetter, 2008, Bioorganic & medicinal chemistry letters.

Pre-clinical evaluation of the MDM2-p53 antagonist RG7388 alone and in combination with chemotherapy in neuroblastoma

J. Lunec, D. Newell, S. Middleton, 2015, Oncotarget.

Identification of a 13 amino acid peptide mimetic of erythropoietin and description of amino acids critical for the mimetic activity of EMP1.

L S Mulcahy, I. Wilson, O. Livnah, 1998, Biochemistry.

Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor

A. Calcagno, S. Ambudkar, S. Emanuel, 2006, Molecular Cancer Therapeutics.

Phase 1/1b Study of RG7388, a Potent MDM2 Antagonist, in Acute Myelogenous Leukemia (AML) Patients (Pts)

W. Pierceall, G. Martinelli, B. Higgins, 2014 .

Phase 1 dose escalation, food effect, and biomarker study of RG7388, a more potent second-generation MDM2 antagonist, in patients (pts) with solid tumors.

J. Blay, Y. Bang, H. Hirte, 2014 .

A Vascular Endothelial Growth Factor Receptor-2 Kinase Inhibitor Potentiates the Activity of the Conventional Chemotherapeutic Agents Paclitaxel and Doxorubicin in Tumor Xenograft Models

M. Batchelor, G. Bignan, M. D'Andrea, 2004, Molecular Pharmacology.

Functional Mimicry of a Protein Hormone by a Peptide Agonist: The EPO Receptor Complex at 2.8 Å

Enrico A. Stura, Ian A. Wilson, William J. Dower, 1996, Science.

1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.

P. Connolly, S. Middleton, V. Pulito, 2007, Bioorganic & medicinal chemistry letters.

Effect of the MDM2 antagonist RG7112 on the P53 pathway in patients with MDM2-amplified, well-differentiated or dedifferentiated liposarcoma: an exploratory proof-of-mechanism study.

Jean-Yves Blay, J. Blay, L. Vassilev, 2012, The Lancet. Oncology.

Structurally diverse MDM2–p53 antagonists act as modulators of MDR-1 function in neuroblastoma

J. Lunec, Yan Zhao, D. Newell, 2014, British Journal of Cancer.

Phase Ib study of RG7112 with doxorubicin (D) in advanced soft tissue sarcoma (ASTS).

J. Blay, A. Cesne, A. Italiano, 2013 .

Results of the Phase 1 Trial of RG7112, a Small-Molecule MDM2 Antagonist, in Acute Leukemia

P. Vyas, L. Vassilev, Suzanne Cheng, 2012 .

Peptide mimetics of erythropoietin are powerful probes of receptor activation mechanisms

I. Wilson, O. Livnah, E. Stura, 2002 .

A peptide mimetic of erythropoietin: Critical residues and description of a minimal functional epitope

I. Wilson, O. Livnah, W. Dower, 2002 .

New epoetin molecules and novel therapeutic approaches.

A. Collins, L. Jolliffe, S. Middleton, 1999, Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association.

Refolding, purification, and characterization of human erythropoietin binding protein produced in Escherichia coli.

L. Jolliffe, S. Middleton, F. Barbone, 1996, Protein expression and purification.

Phase I study of RO4929097, a gamma secretase inhibitor of Notch signaling, in patients with refractory metastatic or locally advanced solid tumors.

James X. Song, A. Tolcher, G. Shapiro, 2012, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

MDM2 antagonist clinical response association with a gene expression signature in acute myeloid leukaemia

S. W. Han, W. Pierceall, L. Essioux, 2015, British journal of haematology.

Phase 1b Study Of The MDM2 Antagonist RG7112 In Combination With 2 Doses/Schedules Of Cytarabine

M. Dennis, G. Martinelli, J. Zhi, 2013 .

Structure of a single amino acid mutant of aspartate carbamoyltransferase at 2.5-A resolution: implications for the cooperative mechanism.

J. Gouaux, W. Lipscomb, E. Kantrowitz, 1989, Biochemistry.

Cellular and in Vivo Activity of JNJ-28871063, A Nonquinazoline Pan-ErbB Kinase Inhibitor That Crosses the Blood-Brain Barrier and Displays Efficacy against Intracranial Tumors

Mary Adams, Niranjan Pandey, Terry V Hughes, 2008, Molecular Pharmacology.

Mutagenesis Studies of the Human Erythropoietin Receptor

R. H. Gruninger, L. Jolliffe, S. Middleton, 1997, The Journal of Biological Chemistry.

α1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms

P. Connolly, S. Middleton, A. Reitz, 2008 .

(Phenylpiperazinyl)cyclohexylureas: discovery of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).

P. Connolly, S. Middleton, V. Pulito, 2008, Bioorganic & medicinal chemistry letters.

Aminocyclohexylsulfonamides: discovery of metabolically stable alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).

P. Connolly, S. Middleton, Sean X Peng, 2007, Bioorganic & medicinal chemistry letters.

(Arylpiperazinyl)cyclohexylsufonamides: discovery of alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS).

P. Connolly, S. Middleton, V. Pulito, 2007, Bioorganic & medicinal chemistry letters.

Clinical pharmacology characterization of RG7112, an MDM2 antagonist, in patients with advanced solid tumors

A. Tolcher, J. Nemunaitis, K. Bhalla, 2015, Cancer Chemotherapy and Pharmacology.

A phase I study of MDM2 antagonist RG7112 in patients (pts) with relapsed/refractory solid tumors.

J. Blay, L. Vassilev, R. Kurzrock, 2012 .

Pharmacokinetics (PK) and pharmacodynamics (PD) of RG7112, an oral murine double minute 2 (MDM2) antagonist, in patients with leukemias and solid tumors.

L. Vassilev, M. Andreeff, R. Kurzrock, 2011, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.

S. Emanuel, P. Connolly, S. Middleton, 2006, Bioorganic & medicinal chemistry letters.

7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.

S. Emanuel, C. Rugg, Angel R. Fuentes-Pesquera, 2008, Bioorganic & medicinal chemistry letters.

Pharmacokinetics (PK) and pharmacodynamics (PD) of RG7112, an oral murine double minute 2 (MDM2) antagonist, in patients with leukemias and solid tumors.

L. Vassilev, M. Andreeff, R. Kurzrock, 2011, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

The Nociceptin Pharmacophore Site for Opioid Receptor Binding Derived from the NMR Structure and Bioactivity Relationships*

P. Connolly, S. Middleton, K. Mayo, 2005, Journal of Biological Chemistry.

Clinical pharmacology characterization of RG7112, an MDM2 antagonist, in patients with advanced solid tumors

A. Tolcher, J. Nemunaitis, K. Bhalla, 2015, Cancer Chemotherapy and Pharmacology.

Prostaglandin-Induced Activation of Nociceptive Neurons via Direct Interaction with Transient Receptor Potential A1 (TRPA1)

E. Mazzon, D. Hamstra, J. Contessa, 2008, Molecular Pharmacology.