J. Verheijen

发表

Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.

N. Brooijmans, L. Toral-Barza, K. Curran, 2009, Journal of medicinal chemistry.

Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases

S. McLeod, R. Tommasi, M. Sacco, 2020, Journal of medicinal chemistry.

ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.

R. Abraham, N. Brooijmans, J. Gibbons, 2009, Journal of medicinal chemistry.

Transition metal derivatives of peptide nucleic acid (PNA) oligomers-synthesis, characterization, and DNA binding.

G. A. van der Marel, J. V. van Boom, N. Metzler‐Nolte, 2000, Bioconjugate chemistry.

Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.

Kevin Curran, Judy Lucas, John Ellingboe, 2009, Cancer research.

Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kalpha.

A. Zask, J. Verheijen, D. J. Richard, 2010, Bioorganic & medicinal chemistry letters.

Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

N. Brooijmans, L. Toral-Barza, A. Zask, 2010, Bioorganic & medicinal chemistry letters.

Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors.

L. Toral-Barza, J. Lucas, K. Curran, 2010, Bioorganic & medicinal chemistry letters.

2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.

K. Curran, A. Zask, Joshua A Kaplan, 2010, Bioorganic & medicinal chemistry letters.

Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent.

L. Toral-Barza, J. Lucas, K. Curran, 2010, Bioorganic & medicinal chemistry letters.

Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K.

L. Toral-Barza, A. Zask, J. Verheijen, 2010, Bioorganic & medicinal chemistry letters.

mTOR Inhibitors in Oncology

A. Zask, J. Verheijen, Ker Yu, 2008 .

Safety and efficacy of the cystic fibrosis transmembrane conductance regulator potentiator icenticaftor (QBW251)

R. Strieter, D. Rowlands, J. Nick, 2020, Journal of cystic fibrosis : official journal of the European Cystic Fibrosis Society.

A short phosphodiester window is sufficient to direct RNase H-dependent RNA cleavage by antisense peptide nucleic acid.

B. Lebleu, I. Robbins, L. Bastide, 2000, Antisense & nucleic acid drug development.

Synthesis and RNase L Binding and Activation of a 2-5A-(5′)-DNA-(3′)-PNA Chimera, a Novel Potential Antisense Molecule

J. V. van Boom, Gijs A. van der Marel, P. Torrence, 2000, Nucleosides, nucleotides & nucleic acids.

An expeditious liquid-phase synthesis of cyclic peptide nucleic acids

J. H. Boom, G. Grotenbreg, G. A. Marel, 2000 .

2-5A-PNA complexes: a novel class of antisense compounds.

G. A. van der Marel, M. Player, J. V. van Boom, 1999, Nucleosides & nucleotides.

Synthesis of DNA-(3′)-PNA Chimeras with Conformationally Restricted Linkers Based on 4-Hydroxyproline

J. H. Boom, G. A. Marel, A. V. Roon, 1999 .

2,5-oligoadenylate-peptide nucleic acids (2-5A-PNAs) activate RNase L.

G. A. van der Marel, M. Player, J. V. van Boom, 1999, Bioorganic & medicinal chemistry.

Recent advances in the discovery of small-molecule ATP competitive mTOR inhibitors: a patent review

A. Zask, J. Verheijen, D. J. Richard, 2011, Expert opinion on therapeutic patents.

Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.

N. Brooijmans, L. Toral-Barza, J. Lucas, 2009, Journal of medicinal chemistry.

New antibacterial agents: patent applications published in 2010.

M. Morningstar, J. Verheijen, S. Stokes, 2012, Pharmaceutical patent analyst.

Rhodium(II) catalyzed asymmetric cyclopropanation of glycals with ethyl diazoacetate

J. H. Boom, G. A. Marel, J. Verheijen, 1996 .

Incorporation of a 4-hydroxy-N-acetylprolinol nucleotide analogue improves the 3'-exonuclease stability of 2'-5'-oligoadenylate-antisense conjugates.

G. A. van der Marel, J. V. van Boom, P. Torrence, 2000, Bioorganic & medicinal chemistry letters.

New antibacterial agents: patent applications published in 2011.

T. Keating, T. Lister, J. Verheijen, 2014, Pharmaceutical patent analyst.

Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2.

R. Abraham, J. Gibbons, L. Toral-Barza, 2010, Cancer research.

Chapter 6:Non-Protein Kinases as Therapeutic Targets

A. Zask, J. Verheijen, D. J. Richard, 2011 .

4,5-Disubstituted 6-Aryloxy-1,3-dihydrobenzo[c][1,2]oxaboroles Are Broad-Spectrum Serine β-Lactamase Inhibitors.

C. Eyermann, A. Ferguson, R. Giacobbe, 2015, ACS infectious diseases.

Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.

L. Toral-Barza, J. Lucas, K. Curran, 2009, Bioorganic & medicinal chemistry letters.

Recent advances in the development of selective, ATP-competitive inhibitors of mTOR.

A. Zask, Arie Zask, David J Richard, 2010, Current opinion in drug discovery & development.

Alkylidene Oxapenem β-Lactamase Inhibitors Revisited: Potent Broad Spectrum Activity but New Stability Challenges.

Matthew D. Miller, S. Tentarelli, Minli Zhang, 2014, ACS medicinal chemistry letters.

Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.

V. Slepnev, S. Du, K. A. Wiig, 2009, Bioorganic & medicinal chemistry letters.

Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.

Joshua Kaplan, Irwin Hollander, Natasja Brooijmans, 2009, Journal of medicinal chemistry.

Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.

R. Abraham, J. Gibbons, J. Lucas, 2009, Cancer Research.