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Martin H Bolli

Explore the profile of Martin H Bolli including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 28
Citations 373
Followers 0
Related Specialties
Chemistry
Biochemistry
Pharmacology
Top 10 Co-Authors
Oliver Nayler
John Gatfield
Patrick Hess
Alexander Treiber
Christoph Boss
Beat Steiner
Thomas Weller
Cyrille Lescop
Christopher Kohl
Christine Brotschi
Published In
J Med Chem
ChemMedChem
Bioorg Med Chem Lett
J Pharmacol Exp Ther
Xenobiotica
Affiliations
Soon will be listed here.
Recent Articles
1.
The novel lysophosphatidic acid receptor 1-selective antagonist, ACT-1016-0707, has unique binding properties that translate into effective antifibrotic and anti-inflammatory activity in different models of pulmonary fibrosis
Birker-Robaczewska M, Boucher M, Ranieri G, Poirey S, Studer R, Freti D, et al.
J Pharmacol Exp Ther . 2025 Mar; 392(3):103396. PMID: 40073729
Pulmonary fibrosis encompasses different chronic interstitial lung diseases, and the predominant form, idiopathic pulmonary fibrosis, remains to have a poor prognosis despite 2 approved therapies. Although the exact pathobiological mechanisms...
2.
Discovery of Galactopyranose-1-Carboxamides as a New Class of Small, Novel, Potent, Selective, and Orally Active Galectin-3 Inhibitors
Zumbrunn C, Remen L, Sager C, Grisostomi C, Stamm C, Krusi D, et al.
ChemMedChem . 2025 Mar; :e202401012. PMID: 40071533
Galectin-3 (Gal-3), a β-galactoside-binding lectin, is implicated in diverse cellular functions ranging from immune response modulation to tissue homeostasis. Notably, increased Gal-3 expression has been linked to the progression of...
3.
Reversible oxidation/reduction steps in the metabolic degradation of the glycerol side chain of the S1P modulator ponesimod
Treiber A, Seeland S, Segrestaa J, Lescop C, Bolli M
Xenobiotica . 2024 Feb; 54(4):182-194. PMID: 38400854
1. Ponesimod is a selective modulator of the sphingosine 1-phosphate receptor 1 (S1P) approved for the treatment of active relapsing forms of multiple sclerosis. The chemical structure of ponesimod contains...
4.
Discovery of the Novel, Orally Active, and Selective LPA1 Receptor Antagonist ACT-1016-0707 as a Preclinical Candidate for the Treatment of Fibrotic Diseases
Lescop C, Birker M, Brotschi C, Burki C, Morrison K, Froidevaux S, et al.
J Med Chem . 2024 Feb; 67(4):2397-2424. PMID: 38349250
Piperidine is a potent and selective lysophosphatidic acid receptor subtype 1 receptor (LPAR1) antagonist that has shown efficacy in a skin vascular leakage target engagement model in mice. However, compound...
5.
Discovery of a Novel Orally Active, Selective LPA Receptor Type 1 Antagonist, 4-(4-(2-Isopropylphenyl)-4-((2-methoxy-4-methylphenyl)carbamoyl)piperidin-1-yl)-4-oxobutanoic Acid, with a Distinct Molecular Scaffold
Lescop C, Brotschi C, Williams J, Sager C, Birker M, Morrison K, et al.
J Med Chem . 2024 Feb; 67(4):2379-2396. PMID: 38349223
Lysophosphatidic acid receptor 1 (LPAR1) antagonists show promise as potentially novel antifibrotic treatments. In a human LPAR1 β-arrestin recruitment-based high-throughput screening campaign, we identified urea as a hit with a...
6.
Discovery of Nivasorexant (ACT-539313): The First Selective Orexin-1 Receptor Antagonist (SO1RA) Investigated in Clinical Trials
Williams J, Bolli M, Brotschi C, Sifferlen T, Steiner M, Treiber A, et al.
J Med Chem . 2024 Feb; 67(4):2337-2348. PMID: 38331429
The orexin system consists of two neuropeptides (orexins A and B) and two receptors (OX1 and OX2). Selective OX1 receptor antagonists (SO1RA) are gaining interest for their potential use in...
7.
Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure-activity-relationship, and sleep-promoting properties in rats
Brotschi C, Bolli M, Gatfield J, Roch C, Sifferlen T, Treiber A, et al.
RSC Med Chem . 2024 Jan; 15(1):344-354. PMID: 38283232
Selective orexin 2 receptor antagonists (2-SORA) such as seltorexant (15) are in clinical development for the treatment of insomnia and other conditions such as depression. Herein, we report our structure-activity-relationship...
8.
From Oxadiazole to Triazole Analogues: Optimization toward a Dual Orexin Receptor Antagonist with Improved in vivo Efficacy in Dogs
Brotschi C, Bolli M, Gatfield J, Heidmann B, Jenck F, Roch C, et al.
ChemMedChem . 2020 Jan; 15(5):430-448. PMID: 31945272
The orexin system is responsible for regulating the sleep-wake cycle. Suvorexant, a dual orexin receptor antagonist (DORA) is approved by the FDA for the treatment of insomnia disorders. Herein, we...
9.
Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure-Activity Relationships, and Sleep-Promoting Properties in Rats
Brotschi C, Roch C, Gatfield J, Treiber A, Williams J, Sifferlen T, et al.
ChemMedChem . 2019 May; 14(13):1257-1270. PMID: 31066976
The orexin system plays an important role in the regulation of wakefulness. Suvorexant, a dual orexin receptor antagonist (DORA) is approved for the treatment of primary insomnia. Herein, we outline...
10.
Cenerimod, a novel selective S1P receptor modulator with unique signaling properties
Piali L, Birker-Robaczewska M, Lescop C, Froidevaux S, Schmitz N, Morrison K, et al.
Pharmacol Res Perspect . 2017 Dec; 5(6). PMID: 29226621
Sphingosine-1-phosphate receptor 1 (S1P ) modulators sequester circulating lymphocytes within lymph nodes, thereby preventing potentially pathogenic autoimmune cells from exiting into the blood stream and reaching inflamed tissues. S1P receptor...