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Open AccessStructural basis and selectivity of sulfatinib binding to FGFR and CSF-1R
Acquired drug resistance poses a challenge for single-target FGFR inhibitors, leading to the development of dual- or multi-target FGFR inhibitors. Sulfatinib is a multi-target kinase inhibitor for treating neu...
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Article
Open AccessStructures of p53/BCL-2 complex suggest a mechanism for p53 to antagonize BCL-2 activity
Mitochondrial apoptosis is strictly controlled by BCL-2 family proteins through a subtle network of protein interactions. The tumor suppressor protein p53 triggers transcription-independent apoptosis through d...
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Article
Open AccessTargeting p53 pathways: mechanisms, structures, and advances in therapy
The TP53 tumor suppressor is the most frequently altered gene in human cancers, and has been a major focus of oncology research. The p53 protein is a transcription factor that can activate the expression of multi...
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Article
Open AccessStructural insight into the ligand binding mechanism of aryl hydrocarbon receptor
The aryl hydrocarbon receptor (AHR), a member of the basic helix–loop–helix (bHLH) Per–Arnt–Sim (PAS) family of transcription factors, plays important roles in regulating xenobiotic metabolism, cellular differ...
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Article
Open AccessCharacterization of the cholangiocarcinoma drug pemigatinib against FGFR gatekeeper mutants
Fibroblast growth factor receptor (FGFR) dysregulation is involved in a variety of tumorigenesis and development. Cholangiocarcinoma is closely related with FGFR aberrations, and pemigatinib is the first drug ...
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Open AccessAuthor Correction: Structure-based design of a dual-warhead covalent inhibitor of FGFR4
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Article
Open AccessStructure-based design of a dual-warhead covalent inhibitor of FGFR4
The fibroblast growth factor 19 (FGF19)/fibroblast growth factor receptor 4 (FGFR4) signaling pathways play critical roles in a variety of cancers, such as hepatocellular carcinoma (HCC). FGFR4 is recognized a...
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Article
Open AccessStructural insights into the potency and selectivity of covalent pan-FGFR inhibitors
FIIN-2, TAS-120 (Futibatinib) and PRN1371 are highly potent pan-FGFR covalent inhibitors targeting the p-loop cysteine of FGFR proteins, of which TAS-120 and PRN1371 are currently in clinical trials. It is cri...
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Article
Open AccessTargeting MCL-1 in cancer: current status and perspectives
Myeloid leukemia 1 (MCL-1) is an antiapoptotic protein of the BCL-2 family that prevents apoptosis by binding to the pro-apoptotic BCL-2 proteins. Overexpression of MCL-1 is frequently observed in many tumor t...
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Article
Open AccessStructural insight into the molecular mechanism of p53-mediated mitochondrial apoptosis
The tumor suppressor p53 is mutated in approximately half of all human cancers. p53 can induce apoptosis through mitochondrial membrane permeabilization by interacting with and antagonizing the anti-apoptotic ...
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Article
Open AccessStructural basis of a novel PD-L1 nanobody for immune checkpoint blockade
The use of antibodies to target immune checkpoints, particularly PD-1/PD-L1, has made a profound impact in the field of cancer immunotherapy. Here, we identified KN035, an anti-PD-L1 nanobody that can strongly...