Richmond, VictoriaM. Michelini, FlaviaA. Bueno, CarlosE. Alche, LauraA. Ramirez, JavierCurrent Medicinal ChemistryRichmond V, Michelini FM, Bueno CA, Alche LE, Ramirez JA (2015) Small molecules as anti-TNF drugs. Curr Med Chem 22(25):2920-2942...
Metal complexes: Varieties of metal-containing small molecules have been demonstrated to interact with G-quadruplexes [104, 105]. As clinical drugs used in chemotherapy, cisplatin and its analogs have conceivable adverse effects, such as renal toxicity and treatment-induced resistance. It is thus in...
Tumour necrosis factor (TNF) is a trimeric protein which signals through two membrane receptors, TNFR1 and TNFR2. Previously, we identified small molecules that inhibit human TNF by stabilising a distorted trimer and reduce the number of receptors bound to TNF from three to two. Here we present...
Protein–RNA interactions have crucial roles in various cellular activities, which, when dysregulated, can lead to a range of human diseases. The identification of small molecules that target the interaction between RNA-binding proteins (RBPs) and RNA is
Protein–protein interactions (PPIs) have been sought as putative therapeutic targets for the advancement of various new treatments. This chapter deals with the various studies that have successfully discovered small-molecule inhibitors (SMIs) associated
The inhibition of protein tyrosine phosphatases 1B (PTP1B) and N2 (PTPN2) has emerged as an exciting approach for bolstering T cell anti-tumor immunity. ABBV-CLS-484 is a PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. Here we have explored the therapeutic potential of a rela...
TNF-α and IFN-γ play important roles in CM pathogenesis by up-regulating the expression of adhesion molecules such as ICAM-1 on the brain endothelia, facilitating the adherence of immune cells, particularly LFA-1+ T cells (8, 13). TNF-α and IFN-γ produced by myeloid and NK cells ...
Collectively, CSF1R inhibitors represent a novel category of immunomodulatory drugs, however, the clinical efficacy is limited because of the existence of other immunosuppressive molecules and cells in TME. The combination of CSF1R inhibitors with chemotherapy, anti-angiogenic drugs, or immunotherapy may...
The drugs currently used for the treatment of NSCLC regulate the immune response, target specific molecules, or are directly cytotoxic [5, 6]. Blockade of programmed cell death (PD)-1 has been extensively used as a standard treatment for NSCLC, but PD-1 blockade has been associated with ...
Tumour necrosis factor (TNF) is a cytokine belonging to a family of trimeric proteins; it has been shown to be a key mediator in autoimmune diseases such as rheumatoid arthritis and Crohn’s disease. While TNF is the target of several successful biologic