Qingbin Cui

Qingbin Cui
University of Toledo · Department of Biochemistry and Cancer Biology

Doctor of Pharmacy

About

41
Publications
3,865
Reads
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877
Citations
Introduction
My research interests fall in the two areas: 1) Medicinal Chemistry, design and synthesis of new small-molecule drugs; 2) Pharmacology, mechanism study. My long-term goals would be the discovery and development of small-molecule drugs, especially novel agents for the treatment of cancer.
Additional affiliations
September 2017 - August 2019
St. John's University
Position
  • PostDoc Position
July 2014 - June 2017
Sun Yat-Sen University Cancer Center
Position
  • Professor (Assistant)
Education
September 2008 - June 2014
Jinan University (Guangzhou, China)
Field of study
  • Medicinal Chemistry
September 2004 - June 2008
Zhengzhou University
Field of study
  • Pharmacy

Publications

Publications (41)
Article
A series of (R)-3,4-dihydroxyphenyllactic acid (Danshensu, DSS) derivatives were synthesized and their cardioprotective effects were evaluated in vitro and in vivo. Among the new derivatives, compound 14 showed significant protective effects in cultured myocardial cells and in the rat model of myocardial ischemia. The therapeutic efficacy of compou...
Article
Using an easily prepared triethylammonium N-benzyldithiocarbamate salt as a sulfur source, a dual C−S functionalization of cyclic diaryliodoniums to form tricyclic thioheterocycles is realized. Our method uses the readily available copper sulfate to accelerate the chemical transformation under mild conditions. A broad range of cyclic diaryliodonium...
Article
The development of multidrug resistance (MDR) to chemotherapy remains a major challenge in the treatment of cancer. Numerous mechanisms have been recognized that cause MDR, but one of the most important mechanisms is overexpression of adenosine triphosphate (ATP)-binding cassette (ABC) transporters, through which the efflux of various anticancer dr...
Article
The successful treatment of cancer has significantly improved as a result of targeted therapy and immunotherapy. However, during chemotherapy, cancer cells evolve and can acquire “multidrug resistance” (MDR), which significantly limits the efficacy of cancer treatment and impacts patient survival and quality of life. Among the approaches to reverse...
Article
Survivin, a member of the inhibitor of apoptosis protein family, exists as a homodimer and is aberrantly upregulated in a wide spectrum of cancers. It was thought to be an ideal target due to its lack of expression in most adult normal tissues and importance in cancer cell survival. However, it has been challenging to target survivin due to its “un...
Article
Drug resistance is the major obstacle that undermines effective cancer treatment. Recently, the application of gas signaling molecules, e.g., carbon monoxide (CO), in overcoming drug resistance has gained significant attention. Growing evidence showed that CO could inhibit mitochondria respiratory effect and glycolysis, two major ATP production pat...
Article
Full-text available
The KRAS-G12C inhibitor ARS-1620, is a novel specific covalent inhibitor of KRAS-G12C, possessing a strong targeting inhibitory effect on KRAS-G12C mutant tumors. Overexpression of ATP-binding cassette super-family B member 1 (ABCB1/P-gp) is one of the pivotal factors contributing to multidrug resistance (MDR), and its association with KRAS mutatio...
Chapter
Paclitaxel is a broad-spectrum chemotherapeutic drug which has been used clinically for three decades. Despite its potent anticancer efficacy, the emergence of drug resistance is inevitable. In this chapter, we include the mechanisms and clinical markers of paclitaxel resistance. Besides, several strategies aiming to overcome paclitaxel resistance...
Article
Full-text available
Heart failure (HF), the leading cause of death among men and women world-wide, causes great health and economic burdens. HF can be triggered by many factors, such as coronary artery disease, heart attack, cardiomyopathy, hypertension, obesity, etc., all of which have close relations with calcium signal and the level of reactive oxygen species (ROS)...
Article
Full-text available
ATP‐binding cassette (ABC) transporters superfamily mediates multidrug resistance in cancer by extruding structurally distinct chemotherapeutic agents, causing failure in chemotherapy. Among the 49 ABC transporters, multidrug resistance protein 7 (MRP7 or ABCC10) is relatively new and has been identified as the efflux pump of multiple anticancer ag...
Article
Full-text available
The overexpression of ATP-binding cassette transporter, ABCG2, plays an important role in mediating multidrug resistance (MDR) in certain types of cancer cells. ABCG2-mediated MDR can significantly attenuate or abrogate the efficacy of anticancer drugs by increasing their efflux from cancer cells. In this study, we determined the efficacy of the no...
Article
Full-text available
ATP-binding cassette (ABC) transporters mediate the ATP-driven translocation of structurally and mechanistically distinct substrates against steep concentration gradients. Among the seven human ABC subfamilies namely ABCA-ABCG, ABCC is the largest subfamily with 13 members. In this respect, 9 of the ABCC members are termed “multidrug resistance pro...
Article
Full-text available
Overexpression of ABCG2 remains a major impediment to successful cancer treatment, because ABCG2 functions as an efflux pump of chemotherapeutic agents and causes clinical multidrug resistance (MDR). Therefore, it is important to uncover effective modulators to circumvent ABCG2-mediated MDR in cancers. In this study, we reported that AZ-628, a RAF...
Article
eIF3i, a 36-kDa protein, is a putative subunit of the eIF3 complex important for translation initiation of mRNAs. It is a WD40 domain-containing protein with seven WD40 repeats that forms a β-propeller structure with an important function in pre-initiation complex formation and mRNA translation initiation. In addition to participating in the eIF3 c...
Article
Full-text available
The efficacy of anti-cancer drugs in patients can be attenuated by the development of multi-drug resistance (MDR) due to ATP-binding cassette (ABC) transporters overexpression. In this in vitro study, we determined the reversal efficacy of the epidermal growth factor receptor (EFGR) inhibitor, saptinib, in SW620 and SW720/Ad300 colon cancer cells a...
Article
Full-text available
Multidrug resistance (MDR) is a major challenge in the treatment of tumors. It refers to cancer cells become resistant to not only the therapeutic drug, but also cross-resistant to multiple drugs with distinct structures and mechanisms of action when they are exposed to a drug for a period of time. An essential mechanism of MDR is the aberrant expr...
Article
Full-text available
While cancer treatment has improved dramatically, it has also encountered many critical challenges, such as disease recurrence, metastasis, and drug resistance, making new drugs with novel mechanisms an urgent clinical need. The term “drug repositioning,” also known as old drugs for new uses, has emerged as one practical strategy to develop new ant...
Article
Full-text available
ABCB1 overexpression is known to contribute to multidrug resistance (MDR) in cancers. Therefore, it is critical to find effective drugs to target ABCB1 and overcome MDR. Erdafitinib is a tyrosine kinase inhibitor (TKI) of fibroblast growth factor receptor (FGFR) that is approved by the FDA to treat urothelial carcinoma. Previous studies have demons...
Article
Full-text available
Background Overexpression of ATP‐binding cassette (ABC) transporter is a major contributor to multidrug resistance (MDR), in which cancer cells acquire resistance to a wide spectrum of chemotherapeutic drugs. In this work, we evaluated the sensitizing effect of sitravatinib, a broad‐spectrum tyrosine kinase inhibitor (TKI), on ATP‐binding cassette...
Article
Full-text available
Previous studies have shown that small-molecule BCL-2 inhibitors can have a synergistic interaction with ABCG2 substrates in chemotherapy. Venetoclax is a potent and selective BCL-2 inhibitor, approved by the FDA in 2016 for the treatment of patients with chronic lymphocytic leukemia (CLL). This study showed that, at a non-toxic concentration, vene...
Article
Full-text available
Failure of cancer chemotherapy is mostly due to multidrug resistance (MDR). Overcoming MDR mediated by overexpression of ATP binding cassette (ABC) transporters in cancer cells remains a big challenge. In this study, we explore whether NVP-TAE684, a novel ALK inhibitor which has the potential to inhibit the function of ABC transport, could reverse...
Article
Drug resistance is a major obstacle in the field of pre-clinical and clinical therapeutics. The development of novel technologies and targeted therapies have yielded new modalities to overcome drug resistance, but multidrug resistance (MDR) remains one of the major challenges in the treatment of cancer. The ubiquitin-proteasome system (UPS) has a c...
Article
Full-text available
P-glycoprotein (P-gp), which is encoded by the ATP-binding cassette (ABC) transporter subfamily B member 1 (ABCB1) gene, is one of the most pivotal ABC transporters that transport its substrates across the cell membrane. Its overexpression is one of the confirmed causes of multidrug resistance (MDR), which results in the failure of cancer treatment...
Article
Full-text available
Overexpression of ABC transporters in cancer cells is an underlying mechanism of multidrug resistance (MDR), leading to insensitive response to chemotherapeutic strategies. Thus, MDR is often results in treatment failure in the clinic. In this study, we found midostaurin, a Food and Drug Administration (FDA)-approved anti-leukemia drug, can antagon...
Article
Full-text available
Curcumin [(1E,6E)‑1,7‑bis(4‑hydroxy‑3‑-methoxyphenyl) hepta‑1,6‑diene‑3,5‑dione] is a natural polyphenol that is derived from the turmeric plant (curcuma longa L.). Curcumin is widely used in food coloring, preservatives, and condiments. Curcumin possesses anti‑tumor, anti‑oxidative and anti‑inflammatory efficacy, as well as other pharmacological e...
Article
Full-text available
Multidrug resistance (MDR) is one of the leading causes of treatment failure in cancer chemotherapy. One major mechanism of MDR is the overexpressing of ABC transporters, whose inhibitors hold promising potential in antagonizing MDR. Glesatinib is a dual inhibitor of c-Met and SMO that is under phase II clinical trial for non-small cell lung cancer...
Article
Multidrug resistance (MDR) in cancer remains a critical obstacle for efficient chemotherapy. Many MDR reversal agents have been discovered but failed in clinical trials due to severe toxic effects. Gaseous signaling molecules (GSMs), such as oxygen, nitric oxide, hydrogen sulfide and carbon monoxide, play key roles in regulating cell biological fun...
Article
Mitochondria play a key role in ATP generation, redox homeostasis and regulation of apoptosis. Due to the essential role of mitochondria in metabolism and cell survival, targeting mitochondria in cancer cells is considered as an attractive therapeutic strategy. However, metabolic flexibility in cancer cells may enable the upregulation of compensato...
Article
Full-text available
In this study, a series of novel Danshensu-tetramethylpyrazine derivatives were synthesized, and their cardioprotective effects and water solubility in vitro were evaluated. The results illustrated that esterification at phenol hydroxyl group was superior to etherification in biological activity. The modification with short-chain fatty acids at the...
Patent
Full-text available
The invention discloses a kind of Novel phosphine gold complex and its antitumor application thereof.Its structural formula such as following formula(I):Wherein, R1 is glucose, arabinose, mannose, rhamnose, 2, the dioxolanes ylmethyl of 2 dimethyl 1,3 or cyclohexyl;R3 is ethyl, carboxyethyl, ethyoxyl, cyclohexyl, phenyl, o-methyl-phenyl or p-methox...
Article
Full-text available
A series of molecular hybrids of Danshensu-tetramethylpyrazine-hydrogen sulfide donors have been synthesized and evaluated in vitro as potent antimyocardial ischemia agents. The pharmacological data demonstrated that compound DTA-2 exhibited the most potent protective activities against tert-butyl hydroperoxide (t-BHP) induced injury in H9c2 cells....
Article
Doxorubicin (Dox) is an anthracycline antibiotic widely used in clinics as an anticancer agent. However, the use of Dox is limited by its cardiotoxicity. We have previously shown that a Danshensu (DSS) derivative, ADTM, displayed strong cardioprotective effects. With improved chemical stability and activity, a novel DSS derivative, D006, based on t...
Patent
Full-text available
The invention provides an inhibitor of glyceraldehyde-3-phosphate dehydrogenase, a preparation method and anticancer application thereof. According to the invention, pharmacological experiments show that the compound has strong killing effect on human colon cancer cells, human gastric cancer cells and leukemia cells, and can significantly induce th...
Article
Full-text available
The phenolic and carboxyl groups of Danshensu were protected by benzyl ,and then the hydroxyl group underwent reaction with different catalysts to get hydroxyl modified derivatives through ether and ester bonds ,then benzyl groups were removed to get target derivatives.These derivatives were evaluated in H9c2cells against tert-butyl hydroperoxide i...
Article
Full-text available
Objective To improve the physicochemical properties and pharmacological activities of Danshensu by structure modification. Methods We synthethized Danshensu derivates and tested their protective effect against oxidative damage induced by t-BHP with MTT method. Results Five new Danshensu derivatives (2, 3, 4, 7 and 8) were synthesized and confirmed...
Article
Full-text available
Objective To study the selectivity of the Lewis acid boron trifluoride diethyl etherate used in debenzylation. Methods Naturally active ingredients Danshensu, ferulic acid and salicylic acid were used as the starting materials to synthesize compounds containing both benzyl ether and ester. Boron trifluoride diethyl etherate was chosen for the remov...
Article
Full-text available
In this research, phosphate and thiophosphate prodrugs 3a, 3b of anti-HIV agent AZT were synthesized, and their anti-HIV activities and cytotoxicities were investigated in vitro. Results showed that the prodrugs 3a and 3b with an IC50 value of 11.0 and 4.0 micromol x L(-1), respectively, were less toxic than AZT (1.0 micromol x L(-1)). Although the...

Questions

Question (1)
Question
I use immunofluorescence assay to check the location of certain enzyme in cells. After treated with 4% formaldehyde in PBS, 0.1% Triton, and antibodies (both primary and second), PI, I sealed the sample with glycerol, and stored in 4 oC in dark last week. Due to the issue of microscope, I have not checked them at that time. How long it usually can stay stable under such conditions? Thank you.

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Projects (2)
Project
Rational new chemical entities design, and synthesis methods optimization.