公开(公告)号：US09597299B2

公开(公告)日：2017-03-21

申请号：US14624574

申请日：2015-02-17

Applicant: Macau University of Science and Technology

Inventor： Lai-Han Leung ,  Xing-Xing Fan ,  Liang Liu ,  Zebo Jiang

IPC: A61K31/661 ,  A61K31/09

CPC classification number: A61K31/09

Abstract: The present invention relates to a method for treating gefitinib-resistant non-small-cell lung cancer (NSCLC) comprising administering an effective amount of a resveratrol analog, (Z)3,4,5,4′-tetramethoxystilbene (TMS), to a subject in need thereof. The present invention also relates to a method for inducing apoptosis in gefitinib-resistant NSCLC cells comprising contacting the resveratrol analog to the cells at an effective amount. The present methods are mediated by different signaling pathways connected to cell proliferation and differentiation such as mTOR, JNK, and certain EGFR phosphorylated tyrosine kinase.

公开(公告)号：US09439898B2

公开(公告)日：2016-09-13

申请号：US14296477

申请日：2014-06-05

Applicant: Macau University of Science and Technology

Inventor： Elaine Lai-Han Leung ,  Liang Liu ,  Xing-Xing Fan

IPC: C12Q1/68 ,  A61K31/4741 ,  A61K33/40 ,  G01N33/50

CPC classification number: A61K31/4741 ,  A61K33/40 ,  C12Q1/6886 ,  C12Q2600/136 ,  C12Q2600/156 ,  G01N33/5011 ,  G01N2333/90209 ,  G01N2333/91205 ,  A61K2300/00

Abstract: The present invention relates to methods for novel drug discovery, treatment and selective targeting for Gefitinib-resistant non-small-cell lung cancer (NSCLC) harboring an additional mutation, in particular, to the discovery of a drug candidate or agent identified by the presently claimed method for use in treating and selective targeting Gefitinib-resistant NSCLC harboring T790M mutation.

Abstract translation: 本发明涉及具有另外突变的吉非替尼耐药性非小细胞肺癌（NSCLC）的新药物发现，治疗和选择性靶向的方法，特别涉及目前鉴定的候选药物或药物的发现 所述方法用于治疗和选择性靶向具有T790M突变的吉非替尼耐药性NSCLC。

公开(公告)号：US20180348222A1

公开(公告)日：2018-12-06

申请号：US15610709

申请日：2017-06-01

Applicant: Macau University of Science and Technology

Inventor： Liang Liu ,  Lai-Han Elaine Leung ,  Xiao-Jun Yao ,  Run-Ze Li ,  Xing-Xing Fan

IPC: G01N33/574 ,  A61K31/56 ,  A61K31/585

Abstract: A method of treating a subject, in particular a human, suffering from non-small cell lung cancer includes administering a bufadienolide to the subject. A method of inhibiting the proliferation and inducing the cell death of non-small cell lung cancer cells, a method of inhibiting the Epidermal growth factor receptor (EGFR) kinase activity in non-small cell lung cancer cells harboring an abnormality in the EGFR gene, and a method of inhibiting Na+/K+-ATPase in non-small cell lung cancer cells includes contacting those cells with a bufadienolide. Proscillaridin A as bufadienolide, with the structure of Formula (III) has advantageously high cytotoxicity against EGFR-dependent non-small cell lung cancer at nano-molar levels while having low toxicity to normal lung cells.

公开(公告)号：US09913811B2

公开(公告)日：2018-03-13

申请号：US15186795

申请日：2016-06-20

Applicant: Macau University of Science and Technology

Inventor： Liang Liu ,  Lai Han Leung ,  Xia Li ,  Xing-Xing Fan

IPC: A61K31/122

CPC classification number: A61K31/122

Abstract: A compound suitable for treating EGFR-dependent non-small cell lung cancer exceptionally inhibits activity of the EGFR kinase, in particular in EGFR-dependent non-small cell lung cancer with intrinsic or acquired resistance against at least one EGFR inhibitor. Methods for inhibiting EGFR kinase activity in non-small cell lung cancer cells which harbor an abnormality in the EGFR gene and for targeting cancer cells harboring an abnormality in EGFR gene by contacting EGFR-dependent non-small cell lung cancer cells with said compound are also provided. The compounds allow for an advantageous inhibition of the EGFR kinase activity and induction of apoptosis of the non-small cell lung cancer cells with abnormality in the EGFR gene. Hence, said compounds represent a highly promising treatment option for patients harboring EGFR-dependent cancer.

公开(公告)号：US20170360721A1

公开(公告)日：2017-12-21

申请号：US15186795

申请日：2016-06-20

Applicant: Macau University of Science and Technology

Inventor： Liang Liu ,  Lai Han Leung ,  Xia Li ,  Xing-Xing Fan

IPC: A61K31/122

CPC classification number: A61K31/122

Abstract: A compound suitable for treating EGFR-dependent non-small cell lung cancer exceptionally inhibits activity of the EGFR kinase, in particular in EGFR-dependent non-small cell lung cancer with intrinsic or acquired resistance against at least one EGFR inhibitor. Methods for inhibiting EGFR kinase activity in non-small cell lung cancer cells which harbor an abnormality in the EGFR gene and for targeting cancer cells harboring an abnormality in EGFR gene by contacting EGFR-dependent non-small cell lung cancer cells with said compound are also provided. The compounds allow for an advantageous inhibition of the EGFR kinase activity and induction of apoptosis of the non-small cell lung cancer cells with abnormality in the EGFR gene. Hence, said compounds represent a highly promising treatment option for patients harboring EGFR-dependent cancer.