Cancer cell metabolism in hypoxia: role of HIF-1 as key regulator and therapeutic target

V Infantino, A Santarsiero, P Convertini… - International journal of …, 2021 - mdpi.com
In order to meet the high energy demand, a metabolic reprogramming occurs in cancer cells.
Its role is crucial in promoting tumor survival. Among the substrates in demand, oxygen is …

Understanding cell penetration of cyclic peptides

PG Dougherty, A Sahni, D Pei - Chemical Reviews, 2019 - ACS Publications
Approximately 75% of all disease-relevant human proteins, including those involved in
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …

In situ hypoxia-induced supramolecular perylene diimide radical anions in tumors for photothermal therapy with improved specificity

H Wang, KF Xue, Y Yang, H Hu, JF Xu… - Journal of the American …, 2022 - ACS Publications
Considering that hypoxia is closely associated with tumor proliferation, invasion, metastasis,
and drug resistance, it is of great significance to overcome hypoxia in tumor treatment …

Pharmacologic targeting of hypoxia-inducible factors

GL Semenza - Annual review of pharmacology and toxicology, 2019 - annualreviews.org
Hypoxia-inducible factors (HIFs) control transcriptional responses to reduced O2 availability.
HIFs are heterodimeric proteins composed of an O2-regulated HIF-α subunit and a …

Targeting hypoxia-inducible factors: therapeutic opportunities and challenges

X Yuan, W Ruan, B Bobrow, P Carmeliet… - Nature Reviews Drug …, 2024 - nature.com
Hypoxia-inducible factors (HIFs) are highly conserved transcription factors that are crucial for
adaptation of metazoans to limited oxygen availability. Recently, HIF activation and …

New modalities for challenging targets in drug discovery

E Valeur, SM Guéret, H Adihou… - Angewandte Chemie …, 2017 - Wiley Online Library
Our ever‐increasing understanding of biological systems is providing a range of exciting
novel biological targets, whose modulation may enable novel therapeutic options for many …

Efficient genetic code expansion without host genome modifications

A Costello, AA Peterson, DL Lanster, Z Li… - Nature …, 2024 - nature.com
Supplementing translation with noncanonical amino acids (ncAAs) can yield protein
sequences with new-to-nature functions but existing ncAA incorporation strategies suffer …

Genetically programmed cell-based synthesis of non-natural peptide and depsipeptide macrocycles

M Spinck, C Piedrafita, WE Robertson, TS Elliott… - Nature …, 2023 - nature.com
The direct genetically encoded cell-based synthesis of non-natural peptide and
depsipeptide macrocycles is an outstanding challenge. Here we programme the encoded …

Methods for generating and screening libraries of genetically encoded cyclic peptides in drug discovery

C Sohrabi, A Foster, A Tavassoli - Nature Reviews Chemistry, 2020 - nature.com
Drug discovery has traditionally focused on using libraries of small molecules to identify
therapeutic drugs, but new modalities, especially libraries of genetically encoded cyclic …

RNA display methods for the discovery of bioactive macrocycles

Y Huang, MM Wiedmann, H Suga - Chemical reviews, 2018 - ACS Publications
The past two decades have witnessed the emergence of macrocycles, including macrocyclic
peptides, as a promising yet underexploited class of de novo drug candidates. Both …