Synthesis and Pharmacological Evaluation of Novel Resorcinol Biphenyl Ether Analogs as Small Molecule Inhibitors of PD-1/PD-L1 with Benign Toxicity Profiles for Cancer Treatment

2021 ◽  
pp. 114522
Author(s):  
Hao Cao ◽  
Binbin Cheng ◽  
Ting Liu ◽  
Jianjun Chen
Keyword(s):  
Cancer Treatment ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Pharmacological Evaluation

Abstract 3516: Discovery of novel SHMT small molecule inhibitors for cancer treatment

2018 ◽  
Author(s):  
Anna Bartosik ◽  
Pawel Guzik ◽  
Marta Sowinska ◽  
Karolina Gluza ◽  
Marcin Krol ◽  
...  
Keyword(s):  
Cancer Treatment ◽  
Small Molecule ◽  
Small Molecule Inhibitors

scholarly journals Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers

2021 ◽  
Vol 22 (22) ◽  
pp. 12142
Author(s):  
Soonsil Hyun ◽  
Dongyun Shin
Keyword(s):  
Drug Resistance ◽  
Cancer Treatment ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Ras Gene ◽  
Tumor Patients ◽  
Kras Mutations ◽  
Ras Pathway ◽  
Ras Protein ◽  
Potential Applications

Drug resistance continues to be a major problem associated with cancer treatment. One of the primary causes of anticancer drug resistance is the frequently mutated RAS gene. In particular, considerable efforts have been made to treat KRAS-induced cancers by directly and indirectly controlling the activity of KRAS. However, the RAS protein is still one of the most prominent targets for drugs in cancer treatment. Recently, novel targeted protein degradation (TPD) strategies, such as proteolysis-targeting chimeras, have been developed to render “undruggable” targets druggable and overcome drug resistance and mutation problems. In this study, we discuss small-molecule inhibitors, TPD-based small-molecule chemicals for targeting RAS pathway proteins, and their potential applications for treating KRAS-mutant cancers. Novel TPD strategies are expected to serve as promising therapeutic methods for treating tumor patients with KRAS mutations.

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