Identification of a stable chemerin analog with potent activity toward ChemR23.

Chemerin is a novel peptide that was identified as a natural ligand for ChemR23. As it has been reported to be involved in the regulation of immune responses and adipogenesis, chemerin may have a variety of physiological functions. Chemerin is synthesized as a precursor (prochemerin) and is proteolytically activated and inactivated in sequential steps, which control its physiological roles in a coordinated manner.

Antagonism of central melanin-concentrating hormone 1 receptor alleviates steatohepatitis in mice.

Blockade of brain melanin-concentrating hormone 1 receptor (MCH1R) significantly ameliorates fatty liver as well as obesity. However, the mode of action of this effect is unknown. This study examined the effect of a MCH1R antagonist in murine steatohepatitis models with and without obesity and clarified whether these pharmacological effects were attributed to anti-obesity effects.

[Patient of advanced age with synclonus liver metastases from colon cancer effectively treated with intraarterial chemotherapy of 5-FU].

An 85-year-old man received ileocecal resection and cholecystectomy for ascending colon cancer with synclonus liver metastases. After a catheter for intraarterial injection into liver was inserted and it fixed to the gastroduodenal artery, an intraarterial chemotherapy of 5-FU 750 mg/body/5 hr biweekly was performed for liver metastases. He had no system trouble and side effects, and liver metastases had been estimated as stable disease for 23 months.

Plk3 phosphorylates topoisomerase IIalpha at Thr(1342), a site that is not recognized by Plk1.

The Plk (polo-like kinase) family is involved in cell-cycle machinery. Despite the possible overlapping involvement of Plk1 and Plk3 in cell-cycle distribution, the precise role of each Plk might be different. To investigate mechanisms that may differentiate their physiological roles, we compared the substrate specificities of Plk1 and Plk3 using synthetic peptides.

Development of a potent and selective GPR7 (NPBW1) agonist: a systematic structure-activity study of neuropeptide B.

Neuropeptide B (NPB) has been recently identified as an endogenous ligand for GPR7 (NPBW1) and GPR8 (NPBW2) and has been shown to possess a relatively high selectivity for GPR7. In order to identify useful experimental tools to address physiological roles of GPR7, we synthesized a series of NPB analogs based on modification of an unbrominated form of 23 amino acids with amidated C-terminal, Br(-)NPB-23-NH(2). We confirmed that truncation of the N-terminal Trp residue resulted in almost complete loss of the binding affinity of NPB for GPR7 and GPR8, supporting the special importance of this residue for binding.

RFamide peptide QRFP43 causes obesity with hyperphagia and reduced thermogenesis in mice.

QRFP, an RFamide peptide, was recently identified as an endogenous ligand of an orphan G protein-coupled receptor, GPR103. Recent investigation revealed that acute intracerebroventricular (ICV) administration of QRFP26/P518/26RFa, a constitutive part of QRFP43 (43-amino acid-residue form of QRFP), increases appetite in mice, but its role in long-term energy homeostasis remains unknown. In the present study, we examined the effects of chronic administration of QRFP43 on feeding behavior, body weight regulation, and energy expenditure in mice.

Hemosuccus pancreaticus caused by rupture of a true splenic artery aneurysm following a failure of coil embolization.

Hemosuccus pancreaticus, particularly that caused by a primary aneurysm, is rarely encountered. Thus, its clinical characteristics are not well known. We report the case of a 53-year old man, who presented with hemosuccus pancreaticus caused by the rupture of an atherosclerotic aneurysm of the splenic artery and underwent distal pancreatectomy with splenectomy.

Antiobesity effect of a melanin-concentrating hormone 1 receptor antagonist in diet-induced obese mice.

Melanin-concentrating hormone (MCH) is a cyclic orexigenic peptide expressed in the lateral hypothalamus, which plays an important role in regulating energy balance. To elucidate the physiological role of MCH in obesity development, the present study examined the effect of a selective MCH1 receptor (MCH1R) antagonist in the diet-induced obesity mouse model. The MCH1R antagonist has high affinity and selectivity for MCH-1R and potently inhibits intracerebroventricularly injected MCH-induced food intake in Sprague Dawley rats.

Primary choriocarcinoma of the jejunum: report of a case.

We report a case of primary choriocarcinoma of the jejunum in a 45-year-old man, which was finally diagnosed by immunohistochemical analysis of a surgically resected specimen. Despite combined systemic chemotherapy, the patient died of progressive liver metastases 5 months after surgery. The serum human chorionic gonadotropin (HCG) level increased dramatically as the liver tumor progressed.

Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.

Investigation of L-alanine and D-amino acid replacement of orexin-B revealed that three L-leucine residues at the positions of 11, 14, and 15 in orexin-B were important to show selectivity for the orexin-2 receptor (OX(2)) over the orexin-1 receptor (OX(1)). L-Alanine substitution at position 11 and D-leucine substitution at positions 14 and 15 maintained the potency of orexin-B to mobilize [Ca(2+)](i) in CHO cells expressing the OX(2), while their potency for the OX(1) was significantly reduced. In combined substitutions, we identified that [Ala(11), D-Leu(15)]orexin-B showed a 400-fold selectivity for the OX(2) (EC(50)=0.