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，     

针刺推拿中药综合治疗颈性眩晕疗效观察

目的观察针刺推拿中药综合治疗颈性眩晕的疗效。方法设综合组80例、电针组42例、推拿组68例和中药组36例,进行疗效比较分析。结果综合组有效率为93.8%,电针组有效率为73.8%,推拿组有效率为86.8%,中药组有效率为69.4%,综合组有效率与其他几组比较差异均有统计学意义（P〈0.05）。结论采用电针、推拿、中药相结合的综合疗法治疗颈性眩晕集诸单一疗法之精华,避免单一疗法的局限性,可提高有效率。     

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。     

两种微创方法治疗股骨颈骨折的临床对照试验

目的分别应用三针锁针加压器外固定和空心拉力钉内固定疗法治疗股骨颈骨折,探讨股骨颈骨折最佳治疗方法.方法应用三针锁针加压器外固定治疗股骨颈骨折63例,其中男24例,女39例;年龄55～89岁,平均(64.5±3.2)岁;Garderl Ⅰ型2例,Ⅱ型15例,Ⅲ型38例,Ⅳ型8例.应用空心拉力钉内固定治疗63例,其中男29例,女34例;年龄45～76岁,平均(62.2±2.9)岁;Garden Ⅰ型4例,Ⅱ型24例,Ⅲ型28例,Ⅳ型7例.对其疗效进行分析.结果126例除2例死亡外均得到随访.115例愈合,其中10例股骨头坏死.外固定组愈合58例,股骨头坏死4例,死亡1例;内固定组愈合57例,股骨头坏死6例,死亡1例.根据Harris功能评定标准评价疗效,外固定组62例中优24例,良26例,可8例,差4例,优良率80.65%;内固定组62例中优23例,良27例,可6例,差6例,优良率80.65%.Harris评分外固定组平均(80.40±1.21)分,内固定组平均(79.14±1.47)分,两组Harris评分比较差异无统计学意义(P＞0.05).结论采用内外固定治疗股骨颈骨折疗效无明显差异,但外固定创伤小、费用低、可早期离床;而采用拉力钉内固定器医疗成本高,卧病时间相对较长,且需二次手术取内固定钉.     

兔内听动脉阻断与听觉改变的关系

目的 探讨实验性内听动脉阻断与术后听力改变的关系及术中听觉监控的方法。方法 实验兔乙状窦后进路暴露小脑桥脑角，下压小脑暴露内听道及第Ⅷ神经复合体，分辨出内听动脉，予阻断不同时间，分别行蜗神经直接复合动作电位(DCAP)和畸变产物耳声发射记录(DPOAE)。结果对照组DCAPN1波潜伏期值无明显改变。内耳血供阻断10s和30s组在压迫开始后3min，DCAPN1波潜伏期值均恢复为初始值。内耳血供阻断1min组在压迫开始后3h，DCAPN1波潜伏期值未恢复为初始值假手术组DPOAE幅值无明显改变，内耳血供阻断10s、30s对DPOAE幅值无影响，内耳血供阻断1min使得DPOAE幅值下降结论兔内耳血供阻断1min可能造成兔听觉不可逆损伤。DCAP、DPOAE能有效、持续地监控内耳血供阻断，是耳神经外科手术中实用的听觉监测手段。