Small molecule inhibitors for cancer immunotherapy and associated biomarkers – the current status

Autor: Lisa Schlicher, Luke G. Green, Andrea Romagnani, Florian Renner

Publikováno v: Frontiers in Immunology, Vol 14 (2023)

Following the success of cancer immunotherapy using large molecules against immune checkpoint inhibitors, the concept of using small molecules to interfere with intracellular negative regulators of anti-tumor immune responses has emerged in recent ye

Externí odkaz: https://doaj.org/article/a95de092546d44f89ad16bface7d5304

In Vitro Characterization of Sphingosine 1-Phosphate Receptor 1 (S1P1) Expression and Mediated Migration of Primary Human T and B Cells in the Context of Cenerimod, a Novel, Selective S1P1 Receptor Modulator

Autor: Lisa Schlicher, Paulina Kulig, Audrey von Münchow, Mark J. Murphy, Marcel P. Keller

Publikováno v: International Journal of Molecular Sciences, Vol 23, Iss 1191, p 1191 (2022)
International Journal of Molecular Sciences; Volume 23; Issue 3; Pages: 1191

Cenerimod is a potent, selective sphingosine 1-phosphate receptor 1 (S1P1) modulator currently investigated in a Phase IIb study in patients with systemic lupus erythematosus (SLE) (NCT03742037). S1P1 receptor modulators sequester circulating lymphoc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e225f551d22cb676b697aa67152686b6
https://www.mdpi.com/1422-0067/23/3/1191

Design of pyrido[2,3-d]pyrimidin-7-one inhibitors of receptor interacting protein kinase-2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling

Autor: Ioannis Siokas, Mads Gyrd-Hansen, Alexei Degterev, Sameer Nikhar, Gregory D. Cuny, Seungheon Lee, Lisa Schlicher

Publikováno v: Eur J Med Chem

Receptor interacting protein kinase-2 (RIPK2) is an enzyme involved in the transduction of pro-inflammatory nucleotide-binding oligomerization domain (NOD) cell signaling, a pathway implicated in numerous chronic inflammatory conditions. Herein, a py

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82d7c8d5c938d8ef7eb229c7c86a4bd7
https://pubmed.ncbi.nlm.nih.gov/33601309

Regulation of CYLD activity and specificity by phosphorylation and ubiquitin-binding CAP-Gly domains

Autor: Sarah L. Maslen, Mads Gyrd-Hansen, Derek Leske, Stefan M.V. Freund, Jane L. Wagstaff, Biao Ma, Paul R. Elliott, Georgina Berridge, Lisa Schlicher, Roman Fischer, Frederik Timmermann, David Komander

Publikováno v: Cell Reports
Cell Reports, Vol 37, Iss 1, Pp 109777-(2021)
Elliott, P R, Leske, D, Wagstaff, J, Schlicher, L, Berridge, G, Maslen, S, Timmermann, F, Ma, B, Fischer, R, Freund, S M V, Komander, D & Gyrd-Hansen, M 2021, ' Regulation of CYLD activity and specificity by phosphorylation and ubiquitin-binding CAP-Gly domains ', Cell Reports, vol. 37, no. 1, 109777 . https://doi.org/10.1016/j.celrep.2021.109777

Summary Non-degradative ubiquitin chains and phosphorylation events govern signaling responses by innate immune receptors. The deubiquitinase CYLD in complex with SPATA2 is recruited to receptor signaling complexes by the ubiquitin ligase LUBAC and r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a26d276d1dad7d6fa715882b1dcaada9
https://doi.org/10.1016/j.celrep.2021.109777

Small molecule inhibitors reveal an indispensable scaffolding role of RIPK 2 in NOD 2 signaling

Autor: Sarah Picaud, Sameer Nikhar, Gregory D. Cuny, Chalada Suebsuwong, Panagis Filippakopoulos, Mads Gyrd-Hansen, Alexei Degterev, Daniel M. Pinkas, Lisa Schlicher, Alex N. Bullock, Joshua C. Bufton, Bing Dai, Kilian Huber, Jennifer A. Ward, Catherine Rogers, Matous Hrdinka

Publikováno v: Hrdinka, M, Schlicher, L, Dai, B, Pinkas, D M, Bufton, J C, Picaud, S, Ward, J A, Rogers, C, Suebsuwong, C, Nikhar, S, Cuny, G D, Huber, K V M, Filippakopoulos, P, Bullock, A N, Degterev, A & Gyrd-Hansen, M 2018, ' Small molecule inhibitors reveal an indispensable scaffolding role of RIPK2 in NOD2 signaling ', EMBO Journal, vol. 37, no. 17, e99372 . https://doi.org/10.15252/embj.201899372
The EMBO Journal

RIPK2 mediates inflammatory signaling by the bacteria‐sensing receptors NOD1 and NOD2. Kinase inhibitors targeting RIPK2 are a proposed strategy to ameliorate NOD‐mediated pathologies. Here, we reveal that RIPK2 kinase activity is dispensable for

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d525dbc840945c9e13b0f0df01042759
https://doi.org/10.15252/embj.201899372