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Page 1
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
Holzer P, Masuya K, Furet P, Kallen J, Valat-Stachyra T, Ferretti S, Berghausen J, Bouisset-Leonard M, Buschmann N, Pissot-Soldermann C, Rynn C, Ruetz S, Stutz S, Chène P, Jeay S, Gessier F. Holzer P, et al. Among authors: gessier f. J Med Chem. 2015 Aug 27;58(16):6348-58. doi: 10.1021/acs.jmedchem.5b00810. Epub 2015 Aug 5. J Med Chem. 2015. PMID: 26181851
A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097.
Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D. Jeay S, et al. Among authors: gessier f. Elife. 2015 May 12;4:e06498. doi: 10.7554/eLife.06498. Elife. 2015. PMID: 25965177 Free PMC article.
Structural States of Hdm2 and HdmX: X-ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes.
Kallen J, Izaac A, Chau S, Wirth E, Schoepfer J, Mah R, Schlapbach A, Stutz S, Vaupel A, Guagnano V, Masuya K, Stachyra TM, Salem B, Chene P, Gessier F, Holzer P, Furet P. Kallen J, et al. Among authors: gessier f. ChemMedChem. 2019 Jul 17;14(14):1305-1314. doi: 10.1002/cmdc.201900201. Epub 2019 May 27. ChemMedChem. 2019. PMID: 31066983
Correction: A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097.
Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D. Jeay S, et al. Among authors: gessier f. Elife. 2016 Nov 17;5:e19317. doi: 10.7554/eLife.19317. Elife. 2016. PMID: 27852439 Free PMC article. No abstract available.
Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV.
Namoto K, Sirockin F, Ostermann N, Gessier F, Flohr S, Sedrani R, Gerhartz B, Trappe J, Hassiepen U, Duttaroy A, Ferreira S, Sutton JM, Clark DE, Fenton G, Beswick M, Baeschlin DK. Namoto K, et al. Among authors: gessier f. Bioorg Med Chem Lett. 2014 Feb 1;24(3):731-6. doi: 10.1016/j.bmcl.2013.12.118. Epub 2014 Jan 6. Bioorg Med Chem Lett. 2014. PMID: 24439847
Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.
Pulz R, Angst D, Dawson J, Gessier F, Gutmann S, Hersperger R, Hinniger A, Janser P, Koch G, Revesz L, Vulpetti A, Waelchli R, Zimmerlin A, Cenni B. Pulz R, et al. Among authors: gessier f. ACS Med Chem Lett. 2019 Sep 6;10(10):1467-1472. doi: 10.1021/acsmedchemlett.9b00317. eCollection 2019 Oct 10. ACS Med Chem Lett. 2019. PMID: 31620235 Free PMC article.
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Angst D, Gessier F, Janser P, Vulpetti A, Wälchli R, Beerli C, Littlewood-Evans A, Dawson J, Nuesslein-Hildesheim B, Wieczorek G, Gutmann S, Scheufler C, Hinniger A, Zimmerlin A, Funhoff EG, Pulz R, Cenni B. Angst D, et al. Among authors: gessier f. J Med Chem. 2020 May 28;63(10):5102-5118. doi: 10.1021/acs.jmedchem.9b01916. Epub 2020 Mar 4. J Med Chem. 2020. PMID: 32083858
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.
Choi HS, Rucker PV, Wang Z, Fan Y, Albaugh P, Chopiuk G, Gessier F, Sun F, Adrian F, Liu G, Hood T, Li N, Jia Y, Che J, McCormack S, Li A, Li J, Steffy A, Culazzo A, Tompkins C, Phung V, Kreusch A, Lu M, Hu B, Chaudhary A, Prashad M, Tuntland T, Liu B, Harris J, Seidel HM, Loren J, Molteni V. Choi HS, et al. Among authors: gessier f. ACS Med Chem Lett. 2015 Mar 16;6(5):562-7. doi: 10.1021/acsmedchemlett.5b00050. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005534 Free PMC article.
16 results