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Philippe Piechon

Explore the profile of Philippe Piechon including associated specialties, affiliations and a list of published articles. Areas
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Articles 10
Citations 118
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Recent Articles
1.
Salcius M, Tutter A, Fouche M, Koc H, King D, Dhembi A, et al.
RSC Chem Biol . 2025 Mar; PMID: 40059881
Many disease-relevant and functionally well-validated targets are difficult to drug. Their poorly defined 3D structure without deep hydrophobic pockets makes the development of ligands with low molecular weight and high...
2.
Thoma G, Vangrevelinghe E, Luneau A, Piechon P, Beerli C, Zerwes H
ACS Med Chem Lett . 2023 Jun; 14(6):841-845. PMID: 37312861
We present a novel concept for the design of supersoft topical drugs. Enzymatic cleavage of the carbonate ester of the potent pan Janus kinase (JAK) inhibitor releases hydroxypyridine . Due...
3.
Lapointe G, Skepper C, Holder L, Armstrong D, Bellamacina C, Blais J, et al.
J Med Chem . 2021 Apr; 64(9):6329-6357. PMID: 33929852
Herein, we describe the discovery and optimization of a novel series that inhibits bacterial DNA gyrase and topoisomerase IV binding to, and stabilization of, DNA cleavage complexes. Optimization of this...
4.
Cho H, Shen Q, Zhang L, Okumura M, Kawakami A, Ambrose J, et al.
Cell Chem Biol . 2021 Apr; 28(10):1407-1419.e6. PMID: 33794192
Three limonoid natural products with selective anti-proliferative activity against BRAF(V600E) and NRAS(Q61K)-mutation-dependent melanoma cell lines were identified. Differential transcriptome analysis revealed dependency of compound activity on expression of the mitochondrial...
5.
Velcicky J, Wilcken R, Cotesta S, Janser P, Schlapbach A, Wagner T, et al.
J Med Chem . 2020 Aug; 63(17):9856-9875. PMID: 32856916
G-protein-coupled receptor SUCNR1 (succinate receptor 1 or GPR91) senses the citric cycle intermediate succinate and is implicated in various pathological conditions such as rheumatoid arthritis, liver fibrosis, or obesity. Here,...
6.
Sager E, Tzvetkova P, Gossert A, Piechon P, Luy B
Chemistry . 2020 Aug; 26(63):14435-14444. PMID: 32744785
NMR-based determination of the configuration of complex molecules containing many stereocenters is often not possible using traditional NOE data and coupling patterns. Making use of residual dipolar couplings (RDCs), we...
7.
Gu X, Zhao J, Chen L, Li Y, Yu B, Tian X, et al.
J Org Chem . 2020 May; 85(11):6844-6853. PMID: 32412751
LCZ696 is a novel treatment for patients suffering from heart failure that combines the two active pharmaceutical ingredients sacubitril and valsartan in a single chemical compound. While valsartan is an...
8.
Reggane M, Wiest J, Saedtler M, Harlacher C, Gutmann M, Zottnick S, et al.
Eur J Pharm Biopharm . 2018 May; 128:290-299. PMID: 29733951
Realizing the full potential of co-crystals enhanced kinetic solubility demands a comprehensive understanding of the mechanisms of dissolution, phase conversion, nucleation and crystal growth, and of the complex interplay between...
9.
Fouche M, Schafer M, Berghausen J, Desrayaud S, Blatter M, Piechon P, et al.
ChemMedChem . 2016 May; 11(10):1048-59. PMID: 27154275
Permeability and oral bioavailability of macrocyclic peptides still represent difficult challenges in drug discovery. Despite the recognized potential of macrocyclic peptides as therapeutics, their use is still restricted to extracellular...
10.
Bill A, Hall M, Borawski J, Hodgson C, Jenkins J, Piechon P, et al.
J Biol Chem . 2014 Mar; 289(16):11029-11041. PMID: 24599954
ANO1, a calcium-activated chloride channel, is highly expressed and amplified in human cancers and is a critical survival factor in these cancers. The ANO1 inhibitor CaCCinh-A01 decreases proliferation of ANO1-amplified...