Recent Advances in Structure-Based Virtual Screening of G-Protein Coupled Receptors

In addition to the rhodopsin crystal structure, high-resolution crystal structures of ligand-mediated G-protein-coupled receptors (GPCRs) have recently become available, and these have become attractive templates for developing homology models of several GPCRs of therapeutic interest. These crystal structures and the homology models derived from them have provided significant insights into ligand–receptor interactions. Moreover, several studies have demonstrated that the structural models are indeed suitable for virtual screening of compound databases to identify new ligands for various GPCRs. Recent examples of such virtual screening against GPCRs are discussed in this review.     

Characterization of bortezomib-adapted I-45 mesothelioma cells

Background  

Bortezomib, a proteasome-specific inhibitor, has emerged as a promising cancer therapeutic agent. However, development of resistance to bortezomib may pose a challenge to effective anticancer therapy. Therefore, characterization of cellular mechanisms involved in bortezomib resistance and development of effective strategies to overcome this resistance represent important steps in the advancement of bortezomib-mediated cancer therapy.     

试析陆懋修从阳明论治温病之特色

陆懋修（1818-1886），又名免研，字九芝，号江左下工，又号林屋山人，江苏元和（今江苏吴县）人，为清代后期著名的医学家。陆氏出身于官宦之家，儒医兼通，陆氏秉承家学，对先人的医学成就颇为敬重。他曾三十余年坚持潜心研究《内经》、《伤寒》等医学经典著作，终于贯通医理而成为一代名医。陆氏一生博览群书之余，著述不断，     

胶质细胞活化对慢性前列腺炎/慢性盆腔疼痛综合征(CP/CPPS)大鼠脊髓背角P物质的影响

目的探讨胶质细胞活化对慢性前列腺炎/慢性盆腔疼痛综合征（chronic prostatitis/chronic pelvic pain syndromes,CP/CPPS）大鼠脊髓背角P物质的影响。方法完全福氏佐剂和3%角叉菜胶前列腺内注射造成CP/CPPS模型,脊髓插管给药胶质细胞活化抑制剂Propentofylline干扰CP/CPPS模型大鼠,免疫组织化学方法观察正常组、疼痛模型组、药物干扰组脊髓节段（L6和S1）背角的胶质细胞的活化和P物质的定性定位,并用放射免疫的方法观察三组脊髓背角P物质的变化。结果脊髓背角胶质细胞活化阳性细胞数疼痛组明显增加,药物干扰组明显减少;P物质主要表达于脊髓背角且疼痛模型组明显增多,药物干扰组明显减少。结论胶质细胞活化是CP/CPPS大鼠脊髓背角P物质变化的重要原因,胶质细胞活化抑制剂的应用将是治疗CP/CPPS的新亮点。     

Feasibility of treating hyperfibrinogenemia with intermittently administered batroxobin in patients with ischemic stroke/transient ischemic attack for secondary prevention.

This study evaluated the safety and efficacy of batroxobin in treating hyperfibrinogenemia for secondary stroke prevention. Patients with ischemic stroke or transient ischemic attack (TIA) were measured for plasma fibrinogen levels. Selected participants had concomitant hyperfibrinogenemia (plasma fibrinogen > or = 3.0 g/l). Patients enrolled between 1 July 2003 and 31 December 2004 were treated with batroxobin; patients enrolled between 1 January 2002 and 30 June 2003 were treated without batroxobin. Batroxobin was administered intermittently via intravenous injection at 3-monthly intervals. Patients in both groups were followed for 1 year. Any cerebrovascular events and suspected adverse events were recorded. In total, 112 ischemic stroke/TIA patients with concomitant hyperfibrinogenemia were enrolled, 52 being treated with batroxobin and 60 without batroxobin. Six patients (11.5%) with batroxobin and 16 patients (26.7%) without batroxobin had recurrent cerebral ischemic events during follow-up. Stroke/TIA recurrence in patients without batroxobin was higher than that in patients with batroxobin (P < 0.05). Two patients with batroxobin and two patients without batroxobin developed hemorrhagic stroke during follow-up. There were five deaths (9.6%) in the batroxobin group, and seven deaths (11.7%) in the nonbatroxobin group during follow-up (P > 0.05). Intermittent intravenous injection of batroxobin can efficiently reduce the risk for stroke/TIA recurrence in patients with concomitant hyperfibrinogenemia.     

大脑中动脉支架内血栓形成1例报告

支架内血栓形成是支架置入术后的一种常见并发症。术后血管内皮损伤、胶原组织暴露和作为异物的支架均为引发血栓形成的可能机制。不能及时识别处理则成为再狭窄的重要原因。我们报告1例发生在大脑中动脉（middle cerebral artery，MCA）支架内的血栓形成，探讨其识别处理过程和可能的机制。     

臂丛加强化麻醉后并发颈部抽动9例分析

目的探讨臂丛加强化麻醉后颈部抽动的原因及防治。方法对近年来在麻醉方法、用药相同,术后颈部抽动患者的观察治疗过程进行分析。结果臂丛麻醉并发颈部抽动给予充分镇静后可完全治愈。结论麻醉后并发颈部抽动为药物副作用及颈局部刺激的综合作用。