Lianggesan was first recorded in Taiping Huimin Heji Jufang， which was composed of Rhei Radix et Rhizoma， Natrii Sulfas， Gardeniae Fructus， Forsythiae Fructus， Scutellariae Radix， Glycyrrhizae Radix et Rhizoma（GRR）， Menthae Haplocalycis Herba， Lophatheri Herba and Mel. It was clinically applied to treat fire-heat syndrome in the upper and middle Jiao， and the curative effect was positive. In this study， the bibliometric method was used to conduct a detailed textual research on the formula name， medicinal composition， dosage evolution， origin and processing， functional indications and other aspects of Lianggesan. Research revealed that Lianggesan has six other names， such as Lianqiao Yinzi， Lianqiao Jiedusan， Jufang Lianggesan， Jiegu Lianggesan， Hejian Lianggesan and Qingji Lianggesan. Based on the edition of Taiping Huimin Heji Jufang， an analysis of the evolution of its formula composition revealed that the missing Chinese medicines were predominantly bamboo leaves and honey， while the added Chinese medicines were primarily supplements introduced to address changes in disease manifestations. After textual research， the dosage for one dose of Lianggesan from Taiping Huimin Heji Jufang was as follows：826 g of Rhei Radix et Rhizoma， 826 g of Natrii Sulfas， 826 g of GRR， 413 g of Gardeniae Fructus， 413 g of Menthae Haplocalycis Herba， 413 g of Scutellariae Radix， and 1652 g of Forsythiae Fructus. Decocting method was as following：Grinding the Chinese medicines into coarse powder（2-4 mm）， taking 8.16 g per dose， adding 300 mL of water， along with 2 g of Lophatheri Herba and 5 g of Mel， and decocting to 140 mL. The residue was removed and taken warmly 30 min after meals. It was recommended to take it three times daily until improvement was achieved. The origins of the 9 Chinese medicines were consistent with the 2020 edition of Pharmacopoeia of the People's Republic of China. Except for GRR， which required single frying（stir-frying）， the remaining medicines were all raw products. The description of the function of this formula in ancient books was summarized as purging fire and promoting bowel movements， clearing heat from the upper body and purging the lower body， and the main syndromes included facial redness， tongue swelling， red eyes， etc. In modern applications， the formula is primarily used for respiratory and digestive system diseases， including acute lung injury， chronic obstructive pulmonary disease， herpetic angina and aphthous stomatitis， covering 142 types of diseases. In summary， this paper can provide a basis for further research and development of Lianggesan through the literature review and key information combing.

Mitochondrial shape rapidly changes by dynamic balance of fusion and fission to adjust to constantly changing energy demands of cancer cells. Mitochondrial dynamics balance is exactly regulated by molecular motor consisted of myosin and actin cytoskeleton proteins. Thus, targeting myosin-actin molecular motor is considered as a promising strategy for anti-cancer. In this study, we performed a proof-of-concept study with a natural-derived small-molecule J13 to test the feasibility of anti-cancer therapeutics

Genomic alterations are commonly found in the signaling pathways of fibroblast growth factor receptors (FGFRs). Although there is no selective FGFR inhibitors in market, several promising inhibitors have been investigated in clinical trials, and showed encouraging efficacies in patients. By designing a hybrid between the FGFR-selectivity-enhancing motif dimethoxybenzene group and our previously identified novel scaffold, we discovered a new series of potent FGFR inhibitors, with the best one showing sub-nanomolar enzymatic activity. After several round of optimization and with the solved crystal structure, detailed structure-activity relationship was elaborated. Together with metabolic stability tests and pharmacokinetic profiling, a representative compound () was selected and tested in xenograft mouse model, and the result demonstrated that inhibitor was effective against tumors with FGFR genetic alterations, exhibiting potential for further development.

Background and objective Video-assisted thoracoscopic surgery (VATS) lobectomy is generally ac-cepted for patients with lung cancer. hTe aim of this study is to explore the feasibility of the single-operation-hole thoraco-scopic lobectomy in the treatment of non-small cell lung cancer. Methods To review and analyze the single-operation-hole thoracoscopic lobectomy performed in our hospital for 113 non-small cell lung cancer (NSCLC) cases from October 2010 to October 2013. hTe incision for observation was 1.5 cm the eighth intercostal at the rear of the midaxillary line and the incision for operation was 2.0 cm-4.0 cm at the fourth or iftfh intercostal of the anterior axillary line. hTe operations were performed through the single-operation-hole. Result hTe operation processes were smooth for all the patients without any operative mor-tality occurrence. Only in 5 cases was the operation hole expanded because of the occurrence of massive hemorrhage during the operation;3 patients with postoperative complications underwent thoracoscopic lobectomy again, including 2 cases of de-layed hemorrhage and 1 case of chylothorax. hTe average surgical duration was (178.24±31.17) min, the average blood loss was (213.56±62.38) mL, and the number of lymph nodes dissected was from 5-22. All diagnose were conifrmed by pathology atfer operation. hTe average length of stay was (8.17±2.93) d. All cases recovered well during the follow-up of (2-38) months, only 5 cases had recurrence or metastasis. Conclusion hTe single-operation-hole thomcoscopic lobectomy for lung cancer is safe and feasible, further reducing the trauma, and can be used as a conventional treatment for early-or medium-term NSCLC.

As an extension of the structure-based drug discovery, fragment-based drug discovery is matured increasingly, and plays an important role in drug development. Fragments in a small library, with lower molecular mass and high "ligand efficiency", are detected by SPR, MS, NMR, X-ray crystallography technologies and other biophysical methods. Then they are considered as starting points for chemical optimization with the guidance of structural biology methods to get good "drug-like" lead and candidate compounds. In this article, we reviewed the current progress of fragment-based drug discovery and detailed a number of examples to illustrate the novel strategies.

To obtain higher potency and specificity, a series of 7-alkoxy analogues of illudalic acid was synthesized on the base of structure-activity relationship (SAR). All of these compounds exhibited submicromolar inhibition of the enzyme when tested against human leukocyte common antigen-related phosphatase (LAR) (for example, for 15e, IC50 = 180 nmol x L(-1)). They represent the most potent small-molecule inhibitors of LAR so far. These analogues also display excellent selectivity for LAR over other protein tyrosine phosphatases (PTPs) except for the highly homologous PTPsigma. The compound 15f is of 120-fold selectivity for LAR versus PTP-1B inhibition. The development of potent enzyme-specific inhibitors is so important that they may serve both as tools to study the role of LAR and as therapeutic agents for treatment of type II diabetes.