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1. 薬物アレルギー：病因drug allergy pathogenesis [show details]
…region 2 (CDR2) of TCR-Vbeta 20-1 . This interaction alters the conformation of the TCR, and the allosteric effect leads to activation of the T cell. Interestingly, this binding site for sulfamethoxazole is …
2. 腎尿細管性アシドーシスの概要と病態生理、およびカリウムバランスへの影響overview and pathophysiology of renal tubular acidosis and the effect on potassium balance [show details]
…produce metabolic acidosis. Changes in potassium balance are commonly seen in patients with RTA. The effect on potassium secretion and the plasma potassium concentration varies among the different types of …
3. 尿失禁や骨盤臓器脱への妊娠と出産の影響effect of pregnancy and childbirth on urinary incontinence and pelvic organ prolapse [show details]
…managed conservatively with pessaries, pads, or no therapy. An area of intense investigation is the effect of pregnancy and childbirth on a woman risk of developing PFDs and whether this risk can be reduced …
4. 統合失調症に対する薬物療法：副作用マネージメントpharmacotherapy for schizophrenia side effect management [show details]
…side effects. Some of the side effects differ in likelihood and/or intensity across individual drugs This topic addresses the clinical manifestations and management of antipsychotic side effects in the …
5. 腎でのマグネシウム処理における利尿剤の有効性effect of diuretics on magnesium handling by the kidney [show details]
…apical membrane that are responsible for the entry of luminal sodium and chloride into the cell . The effect of thiazide diuretics on magnesium transport may vary with acute or chronic administration. In isolated …

English Journal

The chemical diversity and structure-based discovery of allosteric modulators for the PIF-pocket of protein kinase PDK1.

Xu X, Chen Y, Fu Q, Ni D, Zhang J, Li X, Lu S.
Journal of enzyme inhibition and medicinal chemistry. 2019 Dec;34(1)361-374.
Phosphoinositide-dependent protein kinase-1 (PDK1) is an important protein in mediating the PI3K-AKT pathway and is thus identified as a promising target. The catalytic activity of PDK1 is tightly regulated by allosteric modulators, which bind to the PDK1 Interacting Fragment (PIF) pocket of the kin
PMID 30734603

Comprehensive review on the interaction between natural compounds and brain receptors: Benefits and toxicity.

Silva AR, Grosso C, Delerue-Matos C, Rocha JM.
European journal of medicinal chemistry. 2019 Jul;174()87-115.
Given their therapeutic activity, natural products have been used in traditional medicines throughout the centuries. The growing interest of the scientific community in phytopharmaceuticals, and more recently in marine products, has resulted in a significant number of research efforts towards unders
PMID 31029947

Multiple actions of fenamates and other nonsteroidal anti-inflammatory drugs on GABA receptors.

Mansikkamäki S, Sinkkonen ST, Korpi ER, Lüddens H.
European journal of pharmacology. 2019 Jun;853()247-255.
The nonsteroidal anti-inflammatory drug (NSAID) niflumic acid, a fenamate in structure, has many molecular targets, one of them being specific subtypes of the main inhibitory ligand-gated anion channel, the GABA receptor. Here, we report on the effects of other fenamates and other classes of NSAIDs
PMID 30930251

Japanese Journal

Enhancing endogenous adenosine A2A receptor signaling induces slow-wave sleep without affecting body temperature and cardiovascular function

斉藤毅,村越伸行,杉山文博,長瀬博,ラザルスミハエル
Neuropharmacology (144), 122-132, 2019-01
… In the present study, we found that 3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzoic acid, denoted A2AR positive allosteric modulator (PAM)-1, enhanced adenosine signaling at the A2AR and induced slow wave sleep (SWS) without affecting body temperature in wild-type male mice after intraperitoneal administration, whereas the SWS-inducing effect of this benzoic acid derivative was abolished in A2AR KO mice. …
NAID 120006583051

Parkinson病および関連疾患の治療の進歩

村上秀友,河村満,小野賢二郎
神経治療学 34(5), 506-509, 2018
… Dipraglurant, a metabotropic glutamate receptor 5–negative allosteric modulator, but AQW051, a nicotinic acetylcholine receptor α7 agonist, reduced levodopa induced peak dose dyskinesia. … Nilotinib, a tyrosine kinase Abelson inhibitor, was suggested to have beneficial effect on motor and cognitive function in PD and Dementia with Lewy bodies. …
NAID 130006638881

Ignavine: a novel allosteric modulator of the μ opioid receptor

Ohbuchi Katsuya,Miyagi Chika,Suzuki Yasuyuki,Mizuhara Yasuharu,Mizuno Keita,Omiya Yuji,Yamamoto Masahiro,Warabi Eiji,Sudo Yuka,Yokoyama Akinobu,Miyano Kanako,Hirokawa Takatsugu,Uezono Yasuhito
Scientific reports (6), 31748, 2016-08
… Although it has been demonstrated that the κ opioid receptor (KOR) signaling pathway is a mediator of the analgesic effect of PAT, active components affecting opioid signaling have not yet been identified. … Additionally, ignavine alone showed an analgesic effect in vivo. … These data collectively suggest the possibility that ignavine could be a novel allosteric modulator of the MOR. …
NAID 120005851329