Improvement of conventional anti-cancer drugs as new tools against multidrug resistant tumors

S Dallavalle, V Dobričić, L Lazzarato, E Gazzano… - Drug Resistance …, 2020 - Elsevier
Multidrug resistance (MDR) is the dominant cause of the failure of cancer chemotherapy.
The design of antitumor drugs that are able to evade MDR is rapidly evolving, showing that …

Mechanistic understanding from molecular dynamics in pharmaceutical research 2: lipid membrane in drug design

T Róg, M Girych, A Bunker - Pharmaceuticals, 2021 - mdpi.com
We review the use of molecular dynamics (MD) simulation as a drug design tool in the
context of the role that the lipid membrane can play in drug action, ie, the interaction …

Designing new antitubercular isoniazid derivatives with improved reactivity and membrane trafficking abilities

CF de Faria, T Moreira, P Lopes, H Costa… - Biomedicine & …, 2021 - Elsevier
Isoniazid (INH) is one of the two most effective first-line antitubercular drugs and is still used
at the present time as a scaffold for developing new compounds to fight TB. In a previous …

[HTML][HTML] Identifying isoniazid resistance markers to guide inclusion of high-dose isoniazid in tuberculosis treatment regimens

E Rivière, MG Whitfield, J Nelen, TH Heupink… - Clinical Microbiology …, 2020 - Elsevier
Objectives Effective use of antibiotics is critical to control the global tuberculosis pandemic.
High-dose isoniazid (INH) can be effective in the presence of low-level resistance. We …

Optimization of an in Silico Protocol Using Probe Permeabilities to Identify Membrane Pan-Assay Interference Compounds

PR Magalhães, PBPS Reis, D Vila-Viçosa… - Journal of Chemical …, 2022 - ACS Publications
Membrane pan-assay interference compounds (PAINS) are a class of molecules that
interact nonspecifically with lipid bilayers and alter their physicochemical properties. An …

Mitochondria-targeted prostate cancer therapy using a near-infrared fluorescence dye–monoamine oxidase A inhibitor conjugate

Q Lv, X Yang, M Wang, J Yang, Z Qin, Q Kan… - Journal of Controlled …, 2018 - Elsevier
Prostate cancer (PCa) is the most frequent malignant cancer among men in the USA,
leading to substantial morbidity and mortality, while the existing treatments have restricted …

Antimicrobial and anti tubercular activities of isolates and semi synthetic derivatives of lichen Ramalina leiodea (Nyl.) Nyl.

VB Tatipamula, GS Vedula - Journal of the Serbian Chemical Society, 2019 - shd-pub.org.rs
The chemical investigation of lichen Ramalina leiodea (Nyl.) Nyl. yielded five known
metabolites, ie., usnic acid (1), ethyl everninate (2), scrobiculin (3), methyl 2, 6-dihydroxy-4 …

Repurposing antitubercular agent isoniazid for treatment of prostate cancer

Q Lv, D Wang, Z Yang, J Yang, R Zhang, X Yang… - Biomaterials …, 2019 - pubs.rsc.org
The development of versatile antitumor agents with tumor-imaging, targeting and therapeutic
activity is promising for clinical cancer therapy. Prostate cancer is still the one of the leading …

Design, synthesis, and evaluation of monoamine oxidase a inhibitors–indocyanine dyes conjugates as targeted antitumor agents

XG Yang, YH Mou, YJ Wang, J Wang, YY Li, RH Kong… - Molecules, 2019 - mdpi.com
Monoamine oxidase A (MAOA) is an important mitochondria-bound enzyme that catalyzes
the oxidative deamination of monoamine neurotransmitters. Accumulating evidence …

Mutant p53 reactivator SLMP53-2 hinders ultraviolet B radiation-induced skin carcinogenesis

JB Loureiro, R Ribeiro, N Nazareth, T Ferreira… - Pharmacological …, 2022 - Elsevier
The growing incidence of skin cancer (SC) has prompted the search for additional
preventive strategies to counteract this global health concern. Mutant p53 (mutp53) …