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Fingerprint Fingerprint is based on mining the text of the person's scientific documents to create an index of weighted terms, which defines the key subjects of each individual researcher.

  • 2 Similar Profiles
Phosphodiesterase Inhibitors Medicine & Life Sciences
African Trypanosomiasis Medicine & Life Sciences
Phosphoric Diester Hydrolases Medicine & Life Sciences
Parasites Medicine & Life Sciences
Trypanosoma brucei brucei Medicine & Life Sciences
Cyclic Nucleotides Medicine & Life Sciences
Type 4 Cyclic Nucleotide Phosphodiesterase Medicine & Life Sciences
Phosphodiesterase 4 Inhibitors Medicine & Life Sciences

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Research Output 1999 2018

  • 6 Article
  • 1 PhD Thesis - Research VU, graduation VU

Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity

Blaazer, A. R. , Singh, A. K. , De Heuvel, E. , Edink, E. , Orrling, K. M. , Veerman, J. J. N. , Van Den Bergh, T. , Jansen, C. , Balasubramaniam, E. , Mooij, W. J. , Custers, H. , Sijm, M. , Tagoe, D. N. A. , Kalejaiye, T. D. , Munday, J. C. , Tenor, H. , Matheeussen, A. , Wijtmans, M. , Siderius, M. , De Graaf, C. & 7 others Maes, L., De Koning, H. P., Bailey, D. S., Sterk, G. J., De Esch, I. J. P., Brown, D. G. & Leurs, R., 10 May 2018, In : Journal of Medicinal Chemistry. 61, 9, p. 3870-3888 19 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Phosphodiesterase Inhibitors
Phosphoric Diester Hydrolases
Parasites
African Trypanosomiasis
Trypanosoma brucei brucei

The single cyclic nucleotide-specific phosphodiesterase of the intestinal parasite Giardia lamblia represents a potential drug target

Kunz, S., Balmer, V., Sterk, G. J., Pollastri, M. P., Leurs, R., Müller, N., Hemphill, A. & Spycher, C., 15 Sep 2017, In : PLoS Neglected Tropical Diseases. 11, 9, e0005891

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Giardia
Giardia lamblia
Cyclic Nucleotides
Phosphoric Diester Hydrolases
Parasites

Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.

Veerman, J., van den Bergh, T., Orrling, K. M., Jansen, C. J. W., Cos, P., Maes, L., Chatelain, E., Ioset, J. R., Edink, E. S. E., Tenor, H., Seebeck, T., de Esch, I. J. P., Leurs, R. & Sterk, G. J., 2016, In : Bioorganic and Medicinal Chemistry. 24, 7, p. 1573-1581

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
African Trypanosomiasis
Phosphodiesterase Inhibitors
Parasites
Trypanosoma brucei brucei
Phosphoric Diester Hydrolases

Fragment-based screening in tandem with phenotypic screening provides novel antiparasitic hits

Blaazer, A. R., Orrling, K. M., Shanmugham, A., Jansen, C., Maes, L., Edink, E., Sterk, G. J., Siderius, M., England, P., Bailey, D., de Esch, I. J. P. & Leurs, R., Jan 2015, In : Journal of Biomolecular Screening. 20, 1, p. 131-140 10 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Antiparasitic Agents
African Trypanosomiasis
Screening
Trypanosoma brucei brucei
Workflow

Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase b1

Orrling, K. M. , Jansen, C. J. W. , Vu, X. L. , Balmer, V. , Bregy, P. , Shanmugham, A. , England, P. , Bailey, D. , Cos, P. , Maes, L. , Adams, E. , van den Bogaart, E. , Chatelain, E. , Ioset, J. R. , van de Stolpe, A. , Zorg, S. , Veerman, J. , Seebeck, T. , Sterk, G. J. , de Esch, I. J. P. & 1 others Leurs, R., 2012, In : Journal of Medicinal Chemistry. 55, p. 8745-8756

Research output: Contribution to JournalArticleAcademicpeer-review

African Trypanosomiasis
Phosphodiesterase Inhibitors
Parasites
Pharmacology
Trypanosoma brucei brucei