Alpha 2.0
Login Register
» Authors » Pascal Rigollier

Pascal Rigollier

Explore the profile of Pascal Rigollier including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 11
Citations 229
Followers 0
Related Specialties
Chemistry
Biochemistry
Oncology
Top 10 Co-Authors
Nissim-Claude Cohen
Joseph Rahuel
Jeanette M Wood
Hans-Peter Baum
Yasuchika Yamaguchi
Christian R Schnell
Jurgen Maibaum
Walter Schilling
Walter Fuhrer
Frederic Cumin
Published In
J Med Chem
Biochem Biophys Res Commun
ACS Med Chem Lett
Bioorg Med Chem Lett
J Biomol Screen
Affiliations
Soon will be listed here.
Recent Articles
1.
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS for the Treatment of Solid Tumors
Lorthiois E, Gerspacher M, Beyer K, Vaupel A, Leblanc C, Stringer R, et al.
J Med Chem . 2022 Nov; 65(24):16173-16203. PMID: 36399068
Rapid emergence of tumor resistance via RAS pathway reactivation has been reported from clinical studies of covalent KRAS inhibitors. Thus, inhibitors with broad potential for combination treatment and distinct binding...
2.
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C
Weiss A, Lorthiois E, Barys L, Beyer K, Bomio-Confaglia C, Burks H, et al.
Cancer Discov . 2022 Apr; 12(6):1500-1517. PMID: 35404998
Significance: JDQ443 is a structurally novel covalent KRASG12C inhibitor with a unique binding mode that demonstrates potent and selective antitumor activity in cell lines and in vivo models. In preclinical...
3.
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors
Velcicky J, Mathison C, Nikulin V, Pflieger D, Epple R, Azimioara M, et al.
ACS Med Chem Lett . 2019 Jun; 10(6):887-892. PMID: 31223443
SPPL2a (Signal Peptide Peptidase Like 2a) is an intramembrane aspartyl protease engaged in the function of B-cells and dendritic cells. Despite being an attractive target for modulation of the immune...
4.
Discovery of the First Potent, Selective, and Orally Bioavailable Signal Peptide Peptidase-Like 2a (SPPL2a) Inhibitor Displaying Pronounced Immunomodulatory Effects In Vivo
Velcicky J, Bodendorf U, Rigollier P, Epple R, Beisner D, Guerini D, et al.
J Med Chem . 2018 Jan; 61(3):865-880. PMID: 29359565
Signal peptide peptidase-like 2a (SPPL2a) is an aspartic intramembrane protease which has recently been shown to play an important role in the development and function of antigen presenting cells such...
5.
Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39
Bassilana F, Carlson A, DaSilva J, Grosshans B, Vidal S, Beck V, et al.
Nat Chem Biol . 2014 Mar; 10(5):343-9. PMID: 24633354
Hedgehog (Hh) signaling determines cell fate during development and can drive tumorigenesis. We performed a screen for new compounds that can impinge on Hh signaling downstream of Smoothened (Smo). A...
6.
Fragment-based screening by biochemical assays: Systematic feasibility studies with trypsin and MMP12
Boettcher A, Ruedisser S, Erbel P, Vinzenz D, Schiering N, Hassiepen U, et al.
J Biomol Screen . 2010 Sep; 15(9):1029-41. PMID: 20855559
Fragment-based screening (FBS) has gained acceptance in the pharmaceutical industry as an attractive approach for the identification of new chemical starting points for drug discovery programs in addition to classical...
7.
Structural modification of the P2' position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets
Maibaum J, Stutz S, Goschke R, Rigollier P, Yamaguchi Y, Cumin F, et al.
J Med Chem . 2007 Sep; 50(20):4832-44. PMID: 17824680
Due to its function in the rate limiting initial step of the renin-angiotensin system, renin is a particularly promising target for drugs designed to control hypertension, a growing risk to...
8.
Novel 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamide transition state peptidomimetics are potent and orally active inhibitors of human renin
Goschke R, Stutz S, Rasetti V, Cohen N, Rahuel J, Rigollier P, et al.
J Med Chem . 2007 Sep; 50(20):4818-31. PMID: 17824679
The action of renin is the rate-limiting step of the renin-angiotensin system (RAS), a key regulator of blood pressure. Effective renin inhibitors directly block the RAS entirely at source and,...
9.
Key aspects of the Novartis compound collection enhancement project for the compilation of a comprehensive chemogenomics drug discovery screening collection
Jacoby E, Schuffenhauer A, Popov M, Azzaoui K, Havill B, Schopfer U, et al.
Curr Top Med Chem . 2005 May; 5(4):397-411. PMID: 15892682
The NIBR (Novartis Institutes for BioMedical Research) compound collection enrichment and enhancement project integrates corporate internal combinatorial compound synthesis and external compound acquisition activities in order to build up a...
10.
Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists
Rueeger H, Gerspacher M, Buehlmayer P, Rigollier P, Yamaguchi Y, Schmidlin T, et al.
Bioorg Med Chem Lett . 2004 Apr; 14(10):2451-7. PMID: 15109631
Combination of structural elements from a potent Y5 antagonist (2) with thiazole fragments that exhibit weak Y5 affinities followed by lead optimisation led to the discovery of (5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen-2-yl)-piperidin-4-ylmethyl-amino and (4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen-2-yl)-piperidin-4-ylmethyl-amino...