Journal: Clinical and Translational Medicine

Article Title: Oncogenic driver and therapeutic target: Prolactin signalling axis in retroperitoneal sarcoma

doi: 10.1002/ctm2.70669

Figure Lengend Snippet: Functional characterisation of PRL‐mediated proliferation and chemoresistance in sarcoma models. (A and B) Secretory PRL quantification by ELISA confirming knockdown efficiency in the culture medium, n = 3. (C–F) Growth suppression following PRL depletion: CCK‐8 time‐course assay ( n = 5) and colony formation capacity ( n = 3) in PRL‐knockdown models. (G–J) Recombinant PRL (50 ng/mL)‐induced proliferative enhancement: (G and H) CCK‐8 ( n = 5) and (I and J) colony formation ( n = 3) in HT1080 and SW872 lines. (K–P) PRLR‐dependent proliferation modulation: (K–N) CCK‐8 dose‐response ( n = 5) and (O‐P) colony formation ( n = 3) analysis post‐PRLR perturbation. (Q and R) After treating SW872 and HT1080 cells with PRLR antibody rolinsatamab talirine (20 µg/mL), the effect on cell proliferation was detected by the CCK8 method, with n = 5. (S and T) Xenograft tumourigenesis assay demonstrating impaired SW872 growth with PRL knockdown ( n = 9). (U) A single SW872 clone exhibiting the lowest PRL expression among the pooled PRL‐knockout cells was isolated by limiting dilution cloning, expanded in culture and validated for PRL protein levels via ELISA. (V) Cell proliferation was assessed using the CCK‐8 assay following stable PRL knockout ( n = 5 biological replicates). (W) Bromocriptine‐mediated antiproliferative effects were evaluated in parallel in wild‐type and PRL‐knockout SW872 cell lines using the CCK‐8 assay ( n = 5). (X) In vivo efficacy was determined in a subcutaneous xenograft mouse model, wherein tumour growth derived from wild‐type or PRL‐knockout SW872 cells was monitored following bromocriptine treatment, n = 7. (Y and Z) Chemosensitisation effects: PRL pretreatment (50 ng/mL) enhances cytotoxicity of RG7112/abemaciclib/doxorubicin/gemcitabine, n = 5, RG7112 (10 µM), abemaciclib (5 µM), doxorubicin (2 µM), gemcitabine (10 µM). (a) Western blot analysis was performed to detect MDM2 expression in human adipocytes, liposarcoma cell lines (SW872, 93T449, 94T778), fibrosarcoma cell line HT1080 and clinically isolated liposarcoma cell lines established in our laboratory. (b) Western blot analysis was performed to detect MDM2 in 12 clinical retroperitoneal liposarcoma tissues and its corresponding paracancerous tissues, 6 clinical retroperitoneal fibrosarcoma tissues and corresponding paracancerous tissues. (c) Therapeutic synergy evaluation: bromocriptine combined with RG7112 in WEHI164 fibrosarcoma murine model, RG7112: 100 mg/kg per day, bromocriptine: 10 mg/kg, twice daily, ( n = 6). Data expressed as mean ± SD unless specified; * p < .05, ** p < .01, *** p < .001 by two‐tailed Student's t ‐test; ns: not significant.

Article Snippet: Levodopa tablets (19230303, national medicine permission number: H31020888) were purchased from Shanghai Fuda Pharmaceutical Co., Ltd. Cisplatin (HY‐17394), doxorubicin (HY‐15142A), gemcitabine (HY‐17026), RG7112 (HY10959), Nutlin‐3a (HY10029), SAR405838 (HY18986), SP141 (HY141), 10058‐F4 (HY‐12702) and abemaciclib (HY16297A) were purchased from MedChemExpress LLC.

Techniques: Functional Assay, Enzyme-linked Immunosorbent Assay, Knockdown, CCK-8 Assay, Recombinant, Expressing, Knock-Out, Isolation, Cloning, In Vivo, Derivative Assay, Western Blot, Two Tailed Test

Journal: Frontiers in Pharmacology

Article Title: LPM3770277, a Potent Novel CDK4/6 Degrader, Exerts Antitumor Effect Against Triple-Negative Breast Cancer

doi: 10.3389/fphar.2022.853993

Figure Lengend Snippet: Effects of LPM3770277 on lysosome. (A) : The effect of LPM3770277, LPM3770277, LPM3770277 and lysosomal inhibitor Bafilomycin A1 (25 nM) in combination on HCC1806 and SUM159 cells. (B) : The concentration of the drug contained in the lysosome of HCC1806 cells. (C) : The effects of Abemaciclib and compound 277 on autophagy-related proteins LC3B, P62, LAMP2.

Article Snippet: Abemaciclib and Abemaciclib metabolite M2 were purchased from MedChemExpress (Monmouth Junction, NJ, United States, LY-2835219, LSN2839567).

Techniques: Concentration Assay

Journal: Frontiers in Pharmacology

Article Title: LPM3770277, a Potent Novel CDK4/6 Degrader, Exerts Antitumor Effect Against Triple-Negative Breast Cancer

doi: 10.3389/fphar.2022.853993

Figure Lengend Snippet: The effect of different concentrations of Abemaciclib and compound LPM3770277 on the cell cyle of HCC1806. * p < 0.05 vs. control Two-way ANOVA with a post-hoc Bonferroni test was used for all the statistical analyses. Abem: Abemaciclib, 277: LPM3770277.

Article Snippet: Abemaciclib and Abemaciclib metabolite M2 were purchased from MedChemExpress (Monmouth Junction, NJ, United States, LY-2835219, LSN2839567).

Techniques: Control

Journal: Frontiers in Pharmacology

Article Title: LPM3770277, a Potent Novel CDK4/6 Degrader, Exerts Antitumor Effect Against Triple-Negative Breast Cancer

doi: 10.3389/fphar.2022.853993

Figure Lengend Snippet: Results of xenograft tumor model of Abemaciclib and LPM3770277 in HCC1806 and SUM159 cells. (A,D) : Tumor volume. (B,E) : Tumor weight. (C,F) : Bodyweight were measured. * p < 0.01 vs. control, *** p < 0.001 vs. control, ## p < 0.01 vs. LPM3770277, Two-way ANOVA with a post-hoc Bonferroni test was used for all the statistical analyses.

Article Snippet: Abemaciclib and Abemaciclib metabolite M2 were purchased from MedChemExpress (Monmouth Junction, NJ, United States, LY-2835219, LSN2839567).

Techniques: Control

Journal: Frontiers in Pharmacology

Article Title: LPM3770277, a Potent Novel CDK4/6 Degrader, Exerts Antitumor Effect Against Triple-Negative Breast Cancer

doi: 10.3389/fphar.2022.853993

Figure Lengend Snippet: Effects of Abemaciclib and LPM3770277 on the blood of nude mice. HFR%, High fluorescence intensity reticulocyte percentage; IRF, Immature reticulocyte fraction; LFR%, Low fluorescence intensity reticulocyte percentage; MRF%, Medium fluorescence intensity reticulocyte percentage; WBC, White blood cell; LYMPH#, Lymphocyte-count; NEUT#, Neutrophil count; EO%, Percentage of basophils; MONO%, Percentage of Monocyte; MONO#, Monocyte count. * p ˂ 0.05 vs. control, ** p ˂ 0.01 vs. control, One-way ANOVA with a post-hoc Bonferroni test was used for all the statistical analysis.

Article Snippet: Abemaciclib and Abemaciclib metabolite M2 were purchased from MedChemExpress (Monmouth Junction, NJ, United States, LY-2835219, LSN2839567).

Techniques: Fluorescence, Control

Journal: Exploration of Targeted Anti-tumor Therapy

Article Title: Elacestrant in hormone receptor-positive metastatic breast cancer: a post-hoc analysis

doi: 10.37349/etat.2025.1002293

Figure Lengend Snippet: Identifier, interventions, outcome measures, participants, completion date and locations of ongoing/unreported trials

Article Snippet: 4 , NCT04791384 , Phase Ib/II Trial of Abemaciclib and Elacestrant in Patients With Brain Metastasis Due to HR+/Her2- Breast Cancer , Recruiting , Breast cancer , Abemaciclib; elacestrant , AE; efficacy of the combination abemaciclib and elacestrant; tumor response rates; duration of tumor response rates; completion rate , 1 & 2 , 44 , Sequential assignment, open label, interventional , June, 2023 , Criterium, Inc. , United States.

Techniques: Clinical Proteomics, Concentration Assay, Microarray, Gene Expression, Expressing

Journal: Journal of Experimental & Clinical Cancer Research : CR

Article Title: Targeting PEG10 as a novel therapeutic approach to overcome CDK4/6 inhibitor resistance in breast cancer

doi: 10.1186/s13046-023-02903-x

Figure Lengend Snippet: Ectopic overexpression of PEG10 augments EMT and leads to palbociclib resistance. A Immunoblot demonstrates ectopic overexpression of different PEG10 protein isoforms in MCF7 and T47D cells. Ectopic overexpression of PEG10 elevated the ZEB1 and suppressed the E-cadherin expression. B , C Representative images from a migration and invasion assay after ectopic overexpression of different PEG10 protein isoforms in MCF7 and T47D cells. The area of migratory and invading cells from three different non-overlapping 100 × microscopic fields is expressed as mean ± SD in the right panel. Independent sample t-test: * p < 0.05, ** p < 0.01, *** p < 0.001. D - I Cell viability (MTT) assay of MCF7 and T47D cells before and after ectopic overexpression of PEG10-RF1 and subsequent treatment with the indicated dose of palbociclib, abemaciclib, and ribociclib for 72 h. Three independently repeated experiments were performed with similar results. Independent sample t-test: * p < 0.05, ** p < 0.01, *** p < 0.001, Abbreviation: ns, not significant. J , K Cell cycle distribution of MCF7 and T47D cell line before and after the ectopic overexpression of different PEG10 protein isoforms and subsequent treatment with the IC 50 concentration of palbociclib for 48 h. Three independently repeated experiments were performed with similar results. Independent sample t-test: ** p < 0.01, Abbreviation: ns, not significant

Article Snippet: Palbociclib (cat# CS-0019), abemaciclib (cat# CS-1230) and ribociclib (cat# CS-1750) were purchased from ChemScene (Monmouth Junction, NJ, USA).

Techniques: Over Expression, Western Blot, Expressing, Migration, Invasion Assay, MTT Assay, Concentration Assay