In this study, A04, a compound targeting the degradation of metabolic enzyme PDK1, was developed by PROTAC technology, which significantly inhibited tumor proliferation by disrupting the Warburg effect in cancer cells. In the mouse model, A04 could prolong postoperative survival, and also remodel the immunosuppressive microenvironment, which could ...
Aohua Deng+9 more
wiley +1 more source
Disease-causing cystathionine β-synthase linker mutations impair allosteric regulation. [PDF]
Roman JV+4 more
europepmc +1 more source
Structure and allosteric regulation of the αXβ2 integrin I domain [PDF]
Thomas Vorup‐Jensen+4 more
openalex +1 more source
Therapeutic targeting of chromatin alterations in leukemia and solid tumors
Abstract Alterations in chromatin conformation and post‐translational modification of histones have become increasingly recognized as critical drivers of cancer development, progression, and therapy resistance. Recent advances in drug development have led to the establishment of several highly selective small molecule inhibitors, several of which are ...
Florian Perner+7 more
wiley +1 more source
Differential regulation of nitric oxide synthases and their allosteric regulators in heart and vessels of hypertensive rats [PDF]
Alina Piech+4 more
openalex +1 more source
Patient‐derived xenograft models in pan‐cancer: From bench to clinic
Abstract Patient‐derived xenograft (PDX) models provide a robust preclinical platform that preserves the genetic and phenotypic heterogeneity of patient tumors while mirroring their tumor genetic characteristics, which retain malignant cells and the tumor pathological structure, making them valuable for studying tumor progression and developing ...
Jiatong Li+5 more
wiley +1 more source
The Allosteric Regulation of Β-Ureidopropionase Depends on Fine-Tuned Stability of Active-Site Loops and Subunit Interfaces. [PDF]
Cederfelt D+5 more
europepmc +1 more source
Allosteric Regulation and Temperature Dependence of Oxygen Binding in Human Neuroglobin and Cytoglobin [PDF]
Angela Fago+5 more
openalex +1 more source
Noncanonical Nucleotides in the Genome Around the Maternal‐Zygotic Transition
In this paper, Kazzazi et al. provide a comprehensive review of the dynamics of nonconventional nucleotides in the genome during early developmental stages, hypothesizing a potential role for these nucleotides in the activation of the zygotic genome. ABSTRACT From the very moment of fertilization and throughout development, the cells of animal embryos ...
Latifa Kazzazy+7 more
wiley +1 more source