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Perspectives and challenges of small molecule inhibitor therapy for FLT3-mutated acute myeloid leukemia
Acute myeloid leukemia (AML) is a heterogeneous clonal disease characterized overall by an aggressive clinical course. The underlying genetic...
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A small molecule inhibitor of the UBE2F-CRL5 axis induces apoptosis and radiosensitization in lung cancer
Protein neddylation is catalyzed by a neddylation activating enzyme (NAE, E1), an E2 conjugating enzyme, and an E3 ligase. In various types of human...
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Antitumor effect of a small-molecule inhibitor of KRASG12D in xenograft models of mucinous appendicular neoplasms
Pseudomyxoma peritonei (PMP) is a rare disease characterized by a massive accumulation of mucus in the peritoneal cavity. The only effective...
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Gp130 is expressed in pancreatic cancer and can be targeted by the small inhibitor molecule SC144
PurposeInterleukin 6 (IL-6), Oncostatin M (OSM), and downstream effector STAT3 are pro-tumorigenic agents in pancreatic ductal adenocarcinoma (PDAC)....
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A combination of novel NSC small molecule inhibitor along with doxorubicin inhibits proliferation of triple-negative breast cancer through metabolic reprogramming
Treatment of patients with triple-negative breast cancer (TNBC) has been challenging due to the absence of well-defined molecular targets and the...
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Targeting PELP1 oncogenic signaling in TNBC with the small molecule inhibitor SMIP34
PurposeTriple-negative breast cancer (TNBC) is the most aggressive subtype of breast cancer. Oncogenic PELP1 is frequently overexpressed in TNBC, and...
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Characterization of a small-molecule inhibitor targeting NEMO/IKKβ to suppress colorectal cancer growth
NEMO/IKKβ complex is a central regulator of NF-κB signaling pathway, its dissociation has been considered to be an attractive therapeutic target....
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The Safety, Pharmacokinetics, and Pharmacodynamics of SHR2285, an Oral Small Molecule Factor XIa Inhibitor, in Healthy Chinese Volunteers
Background and ObjectiveThere is an unmet need for a safer anticoagulant since bleeding remains a concern with currently approved anticoagulants....
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A small-molecule pan-HER inhibitor alone or in combination with cisplatin exerts efficacy against nasopharyngeal carcinoma
The abnormal activation of HER family kinase activity is closely related to the development of human malignancies. In this study, we used HER kinases...
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Small molecule heat shock protein 27 inhibitor J2 decreases ovarian cancer cell proliferation via induction of apoptotic pathways
Heat shock protein 27 (Hsp27) is an important member of the chaperone protein family and its overexpression promotes cancer cell survival. Here, we...
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Update on Small Molecule Targeted Therapies for Acute Myeloid Leukemia
The search for effective therapies for the highly heterogenous disease acute myeloid leukemia (AML) has remained elusive. While cytotoxic therapies...
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A small molecule inhibitor of VSIG-8 prevents its binding to VISTA
The V-region immunoglobulin-containing suppressor of T cell activation (VISTA), a unique B7 family member, is an attractive immunotherapeutic target...
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Small molecule inhibitors targeting m6A regulators
As the most common form of epigenetic regulation by RNA, N 6 methyladenosine (m 6 A) modification is closely involved in physiological processes, such...
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Small-molecule anti-COVID-19 drugs and a focus on China’s homegrown mindeudesivir (VV116)
The coronavirus disease 2019 (COVID-19) pandemic has stimulated tremendous efforts to develop therapeutic agents that target severe acute respiratory...
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Efficacy and safety study of targeted small-molecule drugs in the treatment of systemic lupus erythematosus
BackgroundTargeted small-molecule drugs in the treatment of systemic lupus erythematosus (SLE) have attracted increasing attention from clinical...
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Application of physiologically based pharmacokinetics modeling in the research of small-molecule targeted anti-cancer drugs
IntroductionPhysiologically based pharmacokinetics (PBPK) models are increasingly used in the drug research and development, especially in...
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Small-molecule amines: a big role in the regulation of bone homeostasis
Numerous small-molecule amines (SMAs) play critical roles in maintaining bone homeostasis and promoting bone regeneration regardless of whether they...
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Small-Molecule Compounds Boost CAR-T Cell Therapy in Hematological Malignancies
Although chimeric antigen receptor T cell immunotherapy has been successfully applied in patients with hematological malignancies, several obstacles...
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Small molecule inhibitors of the VEGF and tyrosine kinase for the treatment of cervical cancer
Cervical cancer accounts for most deaths due to cancer in women, majorly in develo** nations. The culprit behind this disease is the human...
