Výsledky vyhledávání - "Felix DeAnda"

Akademický článek

Dolutegravir interactions with HIV-1 integrase-DNA: structural rationale for drug resistance and dissociation kinetics.

Autor: Felix DeAnda, Kendra E Hightower, Robert T Nolte, Kazunari Hattori, Tomokazu Yoshinaga, Takashi Kawasuji, Mark R Underwood

Publikováno v: PLoS ONE, Vol 8, Iss 10, p e77448 (2013)

Signature HIV-1 integrase mutations associated with clinical raltegravir resistance involve 1 of 3 primary genetic pathways, Y143C/R, Q148H/K/R and N155H, the latter 2 of which confer cross-resistance to elvitegravir. In accord with clinical findings

Externí odkaz: https://doaj.org/article/c236911bda2245a0833c118568cf3e4c

Zobrazit plný text záznamu

Kinase-deficient BTK mutants confer ibrutinib resistance through activation of the kinase HCK

Autor: Kamaldeep Dhami, Anirban Chakraborty, Tarikere L. Gururaja, Leo W.-K. Cheung, Chaohong Sun, Felix DeAnda, XiaoDong Huang

Publikováno v: Science signaling. 15(736)

The Bruton’s tyrosine kinase (BTK) inhibitor ibrutinib irreversibly binds BTK at Cys481, inhibiting its kinase activity and thus blocking transduction of B cell receptor (BCR) signaling. Although ibrutinib is durably effective in patients with B ce

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68e1c9df287305535807f1cd52da6a5c
https://pubmed.ncbi.nlm.nih.gov/35639855

Zobrazit plný text záznamu

Inhibition of the Ribonuclease H Activity of HIV-1 Reverse Transcriptase by GSK5750 Correlates with Slow Enzyme-Inhibitor Dissociation

Autor: Greg L. Beilhartz, Peter Gerondelis, Felix Deanda, Brian A. Johns, Marianne Ngure, Matthias Götte

Publikováno v: Journal of Biological Chemistry. 289:16270-16277

Compounds that efficiently inhibit the ribonuclease (RNase) H activity of the human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) have yet to be developed. Here, we demonstrate that GSK5750, a 1-hydroxy-pyridopyrimidinone analog, b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::700f961467c7bda2583a69220caa2cfd
https://doi.org/10.1074/jbc.m114.569707

Zobrazit plný text záznamu

Prevalent Polymorphisms in Wild-Type HIV-1 Integrase Are Unlikely To Engender Drug Resistance to Dolutegravir (S/GSK1349572)

Autor: Louise Martin-Carpenter, Joseph Horton, Akihiko Sato, Samiul Hasan, Heather Madsen, Garrett Nichols, Shuguang Chen, Robert Cuffe, Cindy Vavro, Felix Deanda, Mark R. Underwood

Publikováno v: Antimicrobial Agents and Chemotherapy. 57:1379-1384

The majority of HIV-1 integrase amino acid sites are highly conserved, suggesting that most are necessary to carry out the critical structural and functional roles of integrase. We analyzed the 34 most variable sites in integrase (>10% variability) a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::550c787403f2ad97c7595de9329b01a8
https://doi.org/10.1128/aac.01791-12

Zobrazit plný text záznamu

Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:360-364

The SAR of C5′ functional groups with terminal basic amines at the C6 aniline of 4,6-bis-anilino-1 H -pyrrolo[2,3- d ]pyrimidines is reported. Examples demonstrate potent inhibition of IGF-1R with 1000-fold selectivity over JNK1 and 3 in enzymatic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee84f30be2cd8cafb0fa1bbaf2738997
https://doi.org/10.1016/j.bmcl.2008.11.077

Zobrazit plný text záznamu

Kinase-Targeted Library Design through the Application of the PharmPrint Methodology

Autor: Michael J. Reno, Eugene L. Stewart, Felix Deanda, David H. Drewry

Publikováno v: Journal of Chemical Information and Modeling. 48:2395-2403

The PharmPrint methodology, as modified and implemented by Deanda and Stewart, was prospectively evaluated for use as a virtual high-throughput screening tool by applying it to the design of target-focused arrays. To this end, PharmPrint quantitative

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c76b0df91dc4f3fede3a84a9e959810
https://doi.org/10.1021/ci800276t

Zobrazit plný text záznamu

Discovery of Bioavailable 4,4-Disubstituted Piperidines as Potent Ligands of the Chemokine Receptor 5 and Inhibitors of the Human Immunodeficiency Virus-1

Autor: Pat Wheelan, Brian A. Chauder, Christian Watson, Terrence Peter Kenakin, Robert M. Ferris, Cecilia S. Koble, Deborah K. Jones-Hertzog, Michael Youngman, Hanbiao Yang, Christopher J Aquino, Felix Deanda, Wieslaw M. Kazmierski

Publikováno v: Journal of Medicinal Chemistry. 51:6538-6546

We describe robust chemical approaches toward putative CCR5 scaffolds designed in our laboratories. Evaluation of analogues in the (125)I-[MIP-1beta] binding and Ba-L-HOS antiviral assays resulted in the discovery of 64 and 68 in the 4,4-disubstitite

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::342620a21dc2e3f0195bfb53c185b26b
https://doi.org/10.1021/jm800598a

Zobrazit plný text záznamu

Aza-stilbenes as potent and selective c-RAF inhibitors

Autor: Ronda G. Davis-Ward, Felix Deanda, Octerloney B. McDonald, Robert N. Hunter, Patrick R. Maloney, Edgar R. Wood, Vicente Samano, Karen Lackey

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:5378-5383

The synthesis of several novel aza-stilbene derivatives was carried out. The compounds were tested for their c-RAF enzyme inhibition. Compound 27 possesses significant potency against c-RAF and demonstrates selectivity over other protein kinases. A h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1af6b219f0fd17fd42af625350f538e
https://doi.org/10.1016/j.bmcl.2006.07.063

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání