Michael Kiffe
Novartis
27 Papers
229 Citations
Michael Kiffe is an academic researcher from Novartis. The author has contributed to research in topics: Chemistry & Medicine. The author has an hindex of 11, co-authored 23 publications.
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Papers
Targeted inhibition of the COP9 signalosome for treatment of cancer.
Anita Schlierf,Eva Altmann,Jean Quancard,Anne B. Jefferson,Rene Assenberg,Martin Renatus,Matthew Jones,Ulrich Hassiepen,Michael Schaefer,Michael Kiffe,Andreas Weiss,Christian Wiesmann,Richard Sedrani,Jörg Eder,Bruno Martoglio +14 more
TL;DR: CSN5i-3 is described, a potent, selective and orally available inhibitor of CSN5, the proteolytic subunit ofCSN, the largest enzyme family of the ubiquitin–proteasome system in humans, which provides insights into how CSN regulates CRLs and suggests that CSN 5 inhibition has potential for anti-tumour therapy.
FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer
Andreas Weiss,Flavia Adler,Alexandra Buhles,Christelle Stamm,Robin Alec Fairhurst,Michael Kiffe,Dario Sterker,Mario Centeleghe,Markus Wartmann,Jacqueline Kinyamu-Akunda,Heiko Schadt,Philippe Couttet,Armin Wolf,Youzhen Wang,Patrizia Barzaghi-Rinaudo,Masato Murakami,Audrey Kauffmann,Thomas Knoepfel,Nicole Buschmann,Catherine Leblanc,Robert Mah,Pascal Furet,Jutta Blank,Francesco Hofmann,William R. Sellers,Diana Graus Porta +25 more
TL;DR: FGF401, a highly potent and selective, first in class, reversible-covalent small-molecule inhibitor of the kinase activity of FGFR4, is described, showing a robust pharmacokinetic/pharmacodynamics/efficacy relationship.
N-Oxidation of Epothilone A-C and O-Acyl Rearrangement to C-19- and C-21-Substituted Epothilones.
TL;DR: A bothersome side reaction in the last step of a total synthesis of epothilone led to the formation of the thiazol-N-oxide, which allows the extremely short synthesis of the highly active epothILones 2 with modified side chains by an O-acyl rearrangement.
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Derivatization of the C12C13 functional groups of epothilones A, B and C
TL;DR: Epothilone A reacted with hydrohalic acids to C12 C13 halohydrin regioisomers (ratios: 2:1 − 4:1).
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Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.
Ying Huang,Martin Sendzik,Jeff Zhang,Zhenting Gao,Yongfeng Sun,Long Wang,Justin Gu,Kehao Zhao,Zhengtian Yu,Lijun Zhang,Qiong Zhang,Joachim Blanz,Zijun Chen,Valerie Dubost,Douglas D. Fang,Li-Shi Feng,Xingnian Fu,Michael Kiffe,Ling Li,Fang Luo,Xiao Luo,Yuan Mi,Prakash Mistry,David Pearson,Alessandro Piaia,Clemens Scheufler,Rémi Terranova,Andreas Weiss,Jue Zeng,Hailong Zhang,Mengxi Zhao,Michael Patrick Dillon,Sébastien Jeay,Wei Qi,Jonathan G. Moggs,Carole Pissot-Soldermann,En Li,Peter Atadja,Andreas Lingel,Counde Oyang +39 more
TL;DR: The stepwise optimization of the tool compound EED226 toward the potent and selective EED inhibitor MAK683 (compound 22) and its subsequent preclinical characterization are reported, based on a balanced PK/PD profile, efficacy, and mitigated risk of forming reactive metabolites, which has been selected for clinical development.
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