Lysine-targeted inhibitors and chemoproteomic probes

A Cuesta, J Taunton - Annual Review of Biochemistry, 2019 - annualreviews.org
Covalent inhibitors are widely used in drug discovery and chemical biology. Although
covalent inhibitors are frequently designed to react with noncatalytic cysteines, many ligand …

Ligand conformational bias drives enantioselective modification of a surface-exposed lysine on Hsp90

A Cuesta, X Wan, AL Burlingame… - Journal of the American …, 2020 - ACS Publications
Targeted covalent modification of surface-exposed lysines is challenging due to their low
intrinsic reactivity and high prevalence throughout the proteome. Strategies for optimizing the …

Discovery of lysine-targeted eIF4E inhibitors through covalent docking

X Wan, T Yang, A Cuesta, X Pang… - Journal of the …, 2020 - ACS Publications
Eukaryotic translation initiation factor 4E (eIF4E) binds the m7GTP cap structure at the 5′-end
of mRNAs, stimulating the translation of proteins implicated in cancer cell growth and …

Digoxin and its derivatives suppress TH17 cell differentiation by antagonizing RORγt activity

…, J Chow, N Manel, M Ciofani, SV Kim, A Cuesta… - Nature, 2011 - nature.com
CD4 + T helper lymphocytes that express interleukin-17 (T H 17 cells) have critical roles in
mouse models of autoimmunity, and there is mounting evidence that they also influence …

Microbiota restricts trafficking of bacteria to mesenteric lymph nodes by CX3CR1hi cells

…, RS Longman, JX Zhang, B Breart, C Galan, A Cuesta… - Nature, 2013 - nature.com
The intestinal microbiota has a critical role in immune system and metabolic homeostasis,
but it must be tolerated by the host to avoid inflammatory responses that can damage the …

Direct mapping of ligandable tyrosines and lysines in cells with chiral sulfonyl fluoride probes

Y Chen, GB Craven, RA Kamber, A Cuesta… - Nature Chemistry, 2023 - nature.com
Advances in chemoproteomic technology have revealed covalent interactions between small
molecules and protein nucleophiles, primarily cysteine, on a proteome-wide scale. Most …

Reversible lysine-targeted probes reveal residence time-based kinase selectivity

T Yang, A Cuesta, X Wan, GB Craven… - Nature chemical …, 2022 - nature.com
The expansion of the target landscape of covalent inhibitors requires the engagement of
nucleophiles beyond cysteine. Although the conserved catalytic lysine in protein kinases is an …

Determination of ubiquitin fitness landscapes under different chemical stresses in a classroom setting

…, L Deming, SD Axen, E Caceres, W Chen, A Cuesta… - Elife, 2016 - elifesciences.org
10.7554/eLife.15802.001 Ubiquitin is essential for eukaryotic life and varies in only 3 amino
acid positions between yeast and humans. However, recent deep sequencing studies …

Gas phase decomposition of t-butyl methyl ether catalyzed by different hydrogen halides: A dft study

SA Cuesta, J Mora, E Márquez - infoANALÍTICA, 2022 - dialnet.unirioja.es
… GAS PHASE DECOMPOSITION OF T-BUTYL METHYL ETHER CATALYZED BY
DIFFERENT HYDROGEN HALIDES: A DFT STUDY Cuesta et al., 65–79 … GAS PHASE …

Diseño de una red IMS para la ciudad de Ica

CF Cabrejos Escajadillo, EA Cuesta Alvear - 2009 - tesis.pucp.edu.pe
El primer capítulo muestra el estado del arte de la tecnología IMS (IP Multimedia Subsystem),
es decir, su estandarización, la evolución de su arquitectura y algunas aplicaciones o …