Cytochrome P450: genotype to phenotype

RH Waring - Xenobiotica, 2020 - Taylor & Francis
The cytochromes P450 comprise a family of enzymes that are responsible for around three-
quarters of all drug metabolism reactions that occur in human populations. Many isoforms of …

Frontiers of metal-coordinating drug design

G Palermo, A Spinello, A Saha… - Expert opinion on drug …, 2021 - Taylor & Francis
Introduction: The occurrence of metal ions in biomolecules is required to exert vital cellular
functions. Metal-containing biomolecules can be modulated by small-molecule inhibitors …

Synthesis, biological evaluation and in silico studies of novel N-substituted phthalazine sulfonamide compounds as potent carbonic anhydrase and …

C Türkeş, M Arslan, Y Demir, L Cocaj, AR Nixha… - Bioorganic …, 2019 - Elsevier
The synthesis, characterization and biological evaluation of a series of novel N-substituted
phthalazine sulfonamide (5a-l) are disclosed. Phthalazines which are nitrogen-containing …

Exploring the Anticancer Activity of Tamoxifen-Based Metal Complexes Targeting Mitochondria

V Scalcon, R Bonsignore, J Aupič… - Journal of Medicinal …, 2023 - ACS Publications
Two new 'hybrid'metallodrugs of Au (III)(AuTAML) and Cu (II)(CuTAML) were designed
featuring a tamoxifen-derived pharmacophore to ideally synergize the anticancer activity of …

[HTML][HTML] Targeting a cryptic allosteric site of SIRT6 with small-molecule inhibitors that inhibit the migration of pancreatic cancer cells

Q Zhang, Y Chen, D Ni, Z Huang, J Wei, L Feng… - … Pharmaceutica Sinica B, 2022 - Elsevier
SIRT6 belongs to the conserved NAD+-dependent deacetylase superfamily and mediates
multiple biological and pathological processes. Targeting SIRT6 by allosteric modulators …

[HTML][HTML] Molecular basis for endocrine disruption by pesticides targeting aromatase and estrogen receptor

C Zhang, T Schilirò, M Gea, S Bianchi… - International Journal of …, 2020 - mdpi.com
The intensive use of pesticides has led to their increasing presence in water, soil, and
agricultural products. Mounting evidence indicates that some pesticides may be endocrine …

Synthesis, biological evaluation, and docking study of indole aryl sulfonamides as aromatase inhibitors

M Fantacuzzi, B De Filippis, M Gallorini… - European journal of …, 2020 - Elsevier
In order to identify new aromatase enzyme inhibitors, thirty aryl sulfonamide derivatives
containing an indole nucleus have been synthesized. The enzyme inhibition assay showed …

High-affinity extended bisphosphonate-based coordination polymers as promising candidates for bone-targeted drug delivery

L Carmona-Sarabia, G Quiñones Vélez… - … Applied Materials & …, 2023 - ACS Publications
Extended bisphosphonate-based coordination polymers (BPCPs) were produced when 1,
1′-biphenyl-4, 4′-bisphosphonic acid (BPBPA), the analogue of 1, 1′-biphenyl-4, 4 …

Decrypting the information exchange pathways across the spliceosome machinery

A Saltalamacchia, L Casalino, J Borisek… - Journal of the …, 2020 - ACS Publications
Intron splicing of a nascent mRNA transcript by spliceosome (SPL) is a hallmark of gene
regulation in eukaryotes. SPL is a majestic molecular machine composed of an entangled …

Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast …

J Caciolla, S Martini, A Spinello, M Pavlin… - European Journal of …, 2021 - Elsevier
Breast Cancer (BC) is a leading cause of death in women, currently affecting 13% of female
population worldwide. First-line clinical treatments against Estrogen Receptor positive (ER+) …