Paul A J Janssen
Overview
Explore the profile of Paul A J Janssen including associated specialties, affiliations and a list of published articles.
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12
Citations
420
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Recent Articles
1.
Njai H, Lewi P, Janssen C, Garcia S, Fransen K, Kestens L, et al.
Antivir Ther
. 2005 May;
10(2):255-62.
PMID: 15865220
In order to study the inhibitory effect of various reverse transcriptase inhibitors (RTIs) on cell-free HIV, we adapted a recently described in vitro system, based on co-cultures of dendritic cells...
2.
de Jonge M, Koymans L, Vinkers H, Daeyaert F, Heeres J, Lewi P, et al.
J Med Chem
. 2005 Mar;
48(6):2176-83.
PMID: 15771460
We have developed a fast and robust computational method for prediction of antiviral activity in automated de novo design of HIV-1 reverse transcriptase inhibitors. This is a structure-based approach that...
3.
Guillemont J, Pasquier E, Palandjian P, Vernier D, Gaurrand S, Lewi P, et al.
J Med Chem
. 2005 Mar;
48(6):2072-9.
PMID: 15771449
This paper reports the synthesis and the antiviral properties of new diarylpyrimidine (DAPY) compounds as nonnucleoside reverse transcriptase inhibitors (NNRTIs). The synthesis program around this new DAPY series was further...
4.
Frenkel Y, Clark Jr A, Das K, Wang Y, Lewi P, Janssen P, et al.
J Med Chem
. 2005 Mar;
48(6):1974-83.
PMID: 15771441
We have examined selected physicochemical properties of compounds from the diaryltriazine/diarylpyrimidine (DATA/DAPY) classes of non-nucleoside reverse transcriptase inhibitors (NNRTIs) and explored possible correlations with their bioavailability. In simple aqueous solutions...
5.
Heeres J, de Jonge M, Koymans L, Daeyaert F, Vinkers M, Van Aken K, et al.
J Med Chem
. 2005 Mar;
48(6):1910-8.
PMID: 15771435
A series of novel pyrazinones designed as non-nucleoside reverse transcriptase inhibitors (NNRTIs) was synthesized and their anti-HIV structure-activity relationship (SAR) was studied.
6.
Janssen P, Lewi P, Arnold E, Daeyaert F, De Jonge M, Heeres J, et al.
J Med Chem
. 2005 Mar;
48(6):1901-9.
PMID: 15771434
Ideally, an anti-HIV drug should (1) be highly active against wild-type and mutant HIV without allowing breakthrough; (2) have high oral bioavailability and long elimination half-life, allowing once-daily oral treatment...
7.
Lewi P, Arnold E, Andries K, Bohets H, Borghys H, Clark A, et al.
Drugs R D
. 2004 Sep;
5(5):245-57.
PMID: 15357624
Objective: To investigate the important factors that determine the bioavailability and the antiviral activity of the diaryltriazine (DATA) and diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitors (NNRTIs) of HIV-1 in animal...
8.
Das K, Clark Jr A, Lewi P, Heeres J, de Jonge M, Koymans L, et al.
J Med Chem
. 2004 Apr;
47(10):2550-60.
PMID: 15115397
Anti-AIDS drug candidate and non-nucleoside reverse transcriptase inhibitor (NNRTI) TMC125-R165335 (etravirine) caused an initial drop in viral load similar to that observed with a five-drug combination in naïve patients and...
9.
Daeyaert F, De Jonge M, Heeres J, Koymans L, Lewi P, Vinkers M, et al.
Proteins
. 2004 Jan;
54(3):526-33.
PMID: 14748000
The docking of small molecules into the binding site of a target protein is an important but difficult step in structure-based drug design. The performance of a docking algorithm is...
10.
Lewi P, De Jonge M, Daeyaert F, Koymans L, Vinkers M, Heeres J, et al.
J Comput Aided Mol Des
. 2003 Sep;
17(2-4):129-34.
PMID: 13677481
There are several indications that a given compound or a set of related compounds can bind in different modes to a specific binding site of a protein. This is especially...