| Title |
Development of small-molecule therapeutics and strategies for targeting RAF kinase in BRAF-mutant colorectal cancer
|
|---|---|
| Published in |
Cancer Management and Research, August 2018
|
| DOI | 10.2147/cmar.s170105 |
| Pubmed ID | |
| Authors |
Jing-hua Pan, Hong Zhou, Sheng-bin Zhu, Jin-lian Huang, Xiao-xu Zhao, Hui Ding, Yun-long Pan |
| Abstract |
RAF kinase is crucially involved in cell proliferation and survival in colorectal cancer (CRC). Patients with metastatic CRC (mCRC) harboring BRAF mutations (BRAFms) not only experience a poor prognosis but also benefit less from therapeutics targeting ERK signaling. With advances in RAF inhibitors and second-generation inhibitors including encorafenib and vemurafenib, which have been approved for treating BRAF-V600E malignancies, the combinatorial therapeutic strategies of RAF inhibitors elicit remarkable responses in patients with BRAF-V600E mCRC. However, the therapeutic efficacy is restricted by resistance, which might be due to RAF dimerization and reactivation of the MAPK pathway. In addition, the next-generation RAF inhibitors, which are characterized by varying structural and biochemical properties, have achieved preclinical and clinical advances. Herein, we summarize the existing mechanism of RAF kinases in CRC, including MAPK feedback reactivation of resistance to RAF inhibitors. We additionally summarize the development of three generations of RAF inhibitors and different therapeutic strategies including the combination of EGFR, BRAF, and PI3K inhibitors for BRAFm CRC treatment. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 51 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 51 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 8 | 16% |
| Student > Master | 7 | 14% |
| Researcher | 7 | 14% |
| Student > Bachelor | 3 | 6% |
| Student > Postgraduate | 3 | 6% |
| Other | 5 | 10% |
| Unknown | 18 | 35% |
| Readers by discipline | Count | As % |
|---|---|---|
| Biochemistry, Genetics and Molecular Biology | 9 | 18% |
| Medicine and Dentistry | 8 | 16% |
| Chemistry | 7 | 14% |
| Pharmacology, Toxicology and Pharmaceutical Science | 4 | 8% |
| Agricultural and Biological Sciences | 3 | 6% |
| Other | 3 | 6% |
| Unknown | 17 | 33% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 04 August 2018.
All research outputs
#15,542,250
of 23,098,660 outputs
Outputs from Cancer Management and Research
#731
of 2,019 outputs
Outputs of similar age
#210,107
of 331,041 outputs
Outputs of similar age from Cancer Management and Research
#36
of 89 outputs
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So far Altmetric has tracked 2,019 research outputs from this source. They receive a mean Attention Score of 3.0. This one has gotten more attention than average, scoring higher than 53% of its peers.
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