Recent advance in oxazole-based medicinal chemistry

HZ Zhang, ZL Zhao, CH Zhou - European journal of medicinal chemistry, 2018 - Elsevier
Oxazole compounds containing nitrogen and oxygen atoms in the five-membered aromatic
ring are readily able to bind with a variety of enzymes and receptors in biological systems …

d-lactate modulates M2 tumor-associated macrophages and remodels immunosuppressive tumor microenvironment for hepatocellular carcinoma

S Han, X Bao, Y Zou, L Wang, Y Li, L Yang, A Liao… - Science …, 2023 - science.org
The polarization of tumor-associated macrophages (TAMs) from M2 to M1 phenotype
demonstrates great potential for remodeling the immunosuppressive tumor …

Small molecule modulators of immune pattern recognition receptors

T Tsukidate, CW Hespen, HC Hang - RSC Chemical Biology, 2023 - pubs.rsc.org
Pattern recognition receptors (PRRs) represent a re-emerging class of therapeutic targets for
vaccine adjuvants, inflammatory diseases and cancer. In this review article, we summarize …

Structural evolution and translational potential for agonists and antagonists of endosomal toll-like receptors

A Talukdar, D Ganguly, S Roy, N Das… - Journal of Medicinal …, 2021 - ACS Publications
Toll-like receptors (TLRs) are members of a large family of evolutionarily conserved pattern
recognition receptors (PRRs), which serve as key components of the innate immune system …

Systematic optimization of potent and orally bioavailable purine scaffold as a dual inhibitor of toll-like receptors 7 and 9

B Kundu, D Raychaudhuri, A Mukherjee… - Journal of Medicinal …, 2021 - ACS Publications
Several toll-like receptors (TLRs) reside inside endosomes of specific immune cells—among
them, aberrant activation of TLR7 and TLR9 is implicated in myriad contexts of autoimmune …

Development, optimization, and in vivo validation of new imidazopyridine chemotypes as dual TLR7/TLR9 antagonists through activity-directed sequential …

N Das, P Bandopadhyay, S Roy, BP Sinha… - Journal of Medicinal …, 2022 - ACS Publications
Undesirable activation of endosomal toll-like receptors TLR7 and TLR9 present in specific
immune cells in response to host-derived ligands is implicated in several autoimmune …

[HTML][HTML] Integration of Ligand-Based and Structure-Based Methods for the Design of Small-Molecule TLR7 Antagonists

S Pal, U Ghosh Dastidar, T Ghosh, D Ganguly… - Molecules, 2022 - mdpi.com
Toll-like receptor 7 (TLR7) is activated in response to the binding of single-stranded RNA. Its
over-activation has been implicated in several autoimmune disorders, and thus, it is an …

Activity-guided development of potent and selective toll-like receptor 9 antagonists

B Paul, O Rahaman, S Roy, S Pal, S Satish… - European Journal of …, 2018 - Elsevier
TLR9 is one of the major innate immune receptors expressed in the endosomes of pDCs
and B cells in humans. Aberrant TLR9 activation is implicated in several autoimmune and …

Synthesis and characterization of new potent TLR7 antagonists based on analysis of the binding mode using biomolecular simulations

S Pal, B Paul, P Bandopadhyay, N Preethy… - European Journal of …, 2021 - Elsevier
Aberrant activation of the endosomal Toll-like receptor 7 (TLR7) has been implicated in
myriad autoimmune diseases and is an established therapeutic target in such conditions …

Mitigating hERG Liability of Toll‐Like Receptor 9 and 7 Antagonists through Structure‐Based Design

N Das, D Bhattacharya, P Bandopadhyay… - …, 2023 - Wiley Online Library
Abstract hERG is considered to be a primary anti‐target in the drug development process, as
the K+ channel encoded by hERG plays an important role in cardiac re‐polarization. It is …