Strategies for structural modification of small molecules to improve blood–brain barrier penetration: a recent perspective

B Xiong, Y Wang, Y Chen, S Xing, Q Liao… - Journal of Medicinal …, 2021 - ACS Publications
In the development of central nervous system (CNS) drugs, the blood–brain barrier (BBB)
restricts many drugs from entering the brain to exert therapeutic effects. Although many …

Recent advances in drug delivery and targeting to the brain

B Sethi, V Kumar, K Mahato, DW Coulter… - Journal of Controlled …, 2022 - Elsevier
Our body keeps separating the toxic chemicals in the blood from the brain. A significant
number of drugs do not enter the central nervous system (CNS) due to the blood-brain …

[HTML][HTML] Therapeutic strategies of glioblastoma (GBM): The current advances in the molecular targets and bioactive small molecule compounds

H Liu, W Qiu, T Sun, L Wang, C Du, Y Hu, W Liu… - … Pharmaceutica Sinica B, 2022 - Elsevier
Glioblastoma (GBM) is the most common aggressive malignant tumor in brain
neuroepithelial tumors and remains incurable. A variety of treatment options are currently …

EGFR, the Lazarus target for precision oncology in glioblastoma

B Lin, J Ziebro, E Smithberger, KR Skinner… - Neuro …, 2022 - academic.oup.com
The Lazarus effect is a rare condition that happens when someone seemingly dead shows
signs of life. The epidermal growth factor receptor (EGFR) represents a target in the fatal …

Discovery of a Hydroxylamine-Based Brain-Penetrant EGFR Inhibitor for Metastatic Non-Small-Cell Lung Cancer

J Hill, RM Jones, D Crich - Journal of Medicinal Chemistry, 2023 - ACS Publications
Metastases to the brain remain a significant problem in lung cancer, as treatment by most
small-molecule targeted therapies is severely limited by efflux transporters at the blood …

EGFR as a potent CAR T target in triple negative breast cancer brain metastases

S Subham, JD Jeppson, C Worcester… - Breast cancer research …, 2023 - Springer
Purpose There is currently no curative treatment for patients diagnosed with triple-negative
breast cancer brain metastases (TNBC-BM). CAR T cells hold potential for curative treatment …

[HTML][HTML] Current chemical, biological, and physiological views in the development of successful brain-targeted pharmaceutics

M Markowicz-Piasecka, A Markiewicz, P Darłak… - …, 2022 - Elsevier
One of the greatest challenges with successful pharmaceutical treatments of central nervous
system (CNS) diseases is the delivery of drugs into their target sites with appropriate …

18 F-Labeled brain-penetrant EGFR tyrosine kinase inhibitors for PET imaging of glioblastoma

MK Narayanam, JE Tsang, S Xu, DA Nathanson… - Chemical …, 2023 - pubs.rsc.org
Significant evidence suggests that the failure of clinically tested epidermal growth factor
receptor (EGFR) tyrosine kinase inhibitors (eg erlotinib, lapatinib, gefitinib) in glioblastoma …

Designing drugs optimized for both blood–brain barrier permeation and intra-cerebral partition

M Dichiara, G Cosentino, G Giordano… - Expert Opinion on …, 2024 - Taylor & Francis
Introduction With the increasing incidence and prevalence of neurological disorders
globally, there is a paramount need for new pharmacotherapies. BBB effectively protects the …

Targeting deoxycytidine kinase improves symptoms in mouse models of multiple sclerosis

BY Chen, JR Salas, AO Trias, A Perez Rodriguez… - …, 2023 - Wiley Online Library
Multiple sclerosis (MS) is an autoimmune disease driven by lymphocyte activation against
myelin autoantigens in the central nervous system leading to demyelination and …