Hormon receptor

Breast cancer is the most common malignancy and the second leading cause of death in women. While tamoxifen (TAM) remains to be a first-line agent for prevention and treatment of estrogenreceptor (ER) positive breast tumors, TAM resistance represents one of the biggest clinical challenges in breast cancer therapy.

9p vihyuga 04-03-2025 3 1   Download

Hiệu lực phụ thuộc vào:Tốc độ tổng hợp và bài tiết Vận chuyển trong huyết tương Receptor. VD ĐTĐ type II do giảm receptor của Insulin Tốc độ thoái hóa Nồng độ thấp: 10-10–10-12 mol (peptid),

50p fpt_12 21-05-2013 144 18   Download

Những hormon có tác dụng thúc đẩy sự đồng hóa, tích lũy protein và chất béo là các hormon sinh dục (Testosterone tích lủy protein, oestrogene tích lũy chất béo). Những loại hormon tự nhiên có cấu trúc khung vòng steran. Những hormon tổng hợp có cấu trúc khác với hormon tự nhiên. Tất cả chúng đều kết nối với receptor. Trong thí nghiệm gần đây người ta chỉ dùng hormon tự nhiên, nhận thấy rằng nếu trộn 3 loại lại: oestrogen, gestagen (kích tố nhao thai) và androgen thì sẽ cho kết quả tốt hơn...

123p peheo_1 31-07-2012 734 77   Download

-Hormon: “kích thích hoạt động” Một số hợp chất hữu cơ được tiết ra từ 1 số TB, đổ vào tuần hoàn, tác dụng lên Cơ quan đích - Tuyến nội tiết: tiết ra hormon (nội tiết tố), đổ thẳng vào hệ tuần hoàn, không có ống tiết. Receptor: gắn đặc hiệu, ái lực cao với Hormon  + phát tín hiệu truyền tin Protein vận chuyển: chỉ gắn hormon, không phát tín hiệu.

50p badaohatgao 28-05-2013 331 58   Download

+pH thay đổi: - thay đổi các liên kết hydro, LK disulfua (-S-S-)= thay đổi cấu trúc, CN của protein đặc biệt protein là enzym - rối loạn hướng, tốc độ và cường độ các f/ư mà E xúc tác. + pH ảnh hưởng: - Receptor/ màng Tb (nhận biết và v.c chất qua màng TB) - Hb & ái lực gắn O2 của Hb - Acid nucleic (AND, ARN)- Di truyền. - Kháng thể- bảo vệ cơ thể - Hormon ( ĐHCH)

25p fpt_12 21-05-2013 103 11   Download

Bài giảng Sinh lý hệ nội tiết được biên soạn nhằm giúp cho người học trình bày được các khái niệm về hormon, mô đích, receptor; phân loại hormon và nêu được đặc điểm chung trong quá trình sinh tổng hợp, bài tiết, vận chuyển, tác dụng của hormone; trình bày các cơ chế tác dụng của hormone; trình bày các cơ chế điều hoà hoạt động hệ nội tiết.

48p thaodien102 06-11-2015 285 57   Download

gp130 is the common signal transducing receptor subunit of interleukin (IL)-6-type cytokines. gp130 either homodimerizes in response to IL-6 and IL-11 or forms heterodimers with the leukemia inhibitory factor (LIF) receptor (LIFR) in response to LIF, oncostatin M (OSM), ciliary neurotrophic factor (CNTF), cardiotrophin-1 (CT-1) or cardiotrophinlike cytokine resulting in the onset of cytoplasmic tyrosine phosphorylation cascades. The extracellular parts of both gp130 and LIFR consist of several Ig-like and fibronectin type III-like domains.

11p system191 01-06-2013 48 4   Download

Nuclear receptors (NRs) are ligand-regulated, DNA-binding transcription factors that function in the chromatin environment of the nucleus to alter the expression of subsets of hormone-responsive genes. It is clear that chromatin, rather than being a passive player, has a profound effect on both transcriptional repression and activation mediated by NRs.

9p research12 01-06-2013 32 2   Download

A series of chimeric receptors was generated between the epidermal growth factor (EGF) receptor, ErbB-1, and its homologue, ErbB-4, to investigate the roles of the extracellular domains (I–IV) in the ligand specificities. As compared with ErbB-1 and the chimeras with both domains I and III of ErbB-1, the chimeras with only one of these domains exhibited reduced binding of 125I-labeled EGF. Particularly, the contribution of domain III was appreciably larger than that of domain I of ErbB-1 in 125I-labeled EGF binding.

7p research12 01-06-2013 50 5   Download

Insulin is the principal regulatory hormone involved in the tight regulation of fuel metabolism. In response to blood glucose levels, it is secreted by the b cells of the pancreas and exerts its effects by binding to cell surface receptors that are present on virtually all cell types and tissues. In humans, perturbations in insulin function and/or secretion lead to diabetes mellitus, a severe disorder primarily characterized by an inability to maintain blood glucose homeostasis. Furthermore, it is estimated that 90–95% of diabetic patients exhibit resistance to insulin action....

10p research12 01-06-2013 36 4   Download

Chickenovalbuminupstreampromoter-transcriptionfactorI (COUP-TFI, or NR2F1) is an orphan nuclear receptor that plays amajor role in the development of the nervous system. We show here that three ETS response elements in the COUP-TFIpromoter mediate its transcription. A reporter gene containing theseETSbinding sites is activatedbyEts-1, while the same reporter with point mutations on all three ETS response elements is not.

9p research12 29-04-2013 29 3   Download

Thyrotropin-releasing hormone receptor (TRHR) has already been cloned in mammals where thyrotropin-releas-inghormone (TRH) isknowntoactasapowerful stimulator of thyroid-stimulating hormone (TSH) secretion. The TRH receptor of amphibians has not yet been characterized, although TRH is specifically important in the adaptation of skin color to environmental changes via the secretion of a-melanocyte-stimulating hormone (a-MSH).

11p research12 23-04-2013 33 4   Download

Structurally tachykinin-related peptides have been isolated fromvarious invertebrate species and shown to exhibit their biological activities through a G-protein-coupled receptor (GPCR) for a tachykinin-related peptide. In this paper, we report the identification of a novel tachykinin-related pep-tide receptor, the urechistachykinin receptor (UTKR) from the echiuroidworm,Urechis unitinctus.

9p research12 23-04-2013 26 2   Download

Thea-melanocyte-stimulating hormone (aMSH) receptor (MC1R) is amajordeterminant ofmammalianskinandhair pigmentation. Binding ofaMSHtoMC1Rinhuman mel-anocytes stimulates cell proliferation and synthesis of pho-toprotective eumelanin pigments. Certain MC1Ralleles have been associated with increased riskof melanoma. This can be theoretically considered on two grounds. First, gain-of-function mutations may stimulate proliferation, thus promoting dysplastic lesions.

9p tumor12 22-04-2013 35 4   Download

N-tert-Butyl-N,N¢-dibenzoylhydrazine and its analogs are nonsteroidal ecdysone agonists that exhibit insect molting hormonal and larvicidal activities. The interaction mode of those ecdysone agonists with the heterodimer of the ecdy-sone receptor andultraspiracle has not been fully elucidated. We expressed the ecdysone receptor B1 and the ultraspiracle of the lepidopteran,Chilo suppressalis,using anin vitro transcription/translation system and confirmed, using gel-shift assays, that the proteins functionas ecdysone receptors. We also analyzed their ligand-binding affinity. ...

10p tumor12 20-04-2013 49 3   Download

Activating mutations of the thyroid-stimulating hormone receptor (TSHr) have been identified as a cause of toxic adenomas. Germline-inactivating TSHr mutations have beendescribedas a cause of congenital hypothyroidism. The effects of combining activating and inactivating mutations within a single receptor was studied. The double mutant T477I/P639S contained an activating TSHr mutation (P639S) togetherwithan inactivatingone (T477I). Theother one (I486M/P639S) contained two activating mutations.

9p tumor12 20-04-2013 39 3   Download

The currently accepted model of moult control in crusta-ceans relies entirely on the hypothesis that moult-inhibiting hormone (MIH) and crustacean hyperglycaemic hormone (CHH) repress ecdysteroid synthesis of the target tissue (Y-organ) only during intermoult, and that changes in syn-thesis and/or release of these neurohormones are central to moult control.

9p tumor12 20-04-2013 54 3   Download

The thyrotropin receptor (TSHR) undergoes a cleavage at the cell membrane, leading to a heterodimer, comprising an aextracellular and a b-transmembrane and intracellular subunits, held togetherbydisulfidebonds.Moreover, part of the a-subunit of the receptor is shed from thyroid and transfected L cells.To understand the role of cleavage and shedding, we constructed deletion mutants starting, respectively, at the most N-terminal (S314), and C-terminal (L378) cleavage sites previously mapped, corresponding to free b1orb2-subunits without further modification of receptor structure....

12p tumor12 20-04-2013 38 2   Download

Seven alleles of the chicken melanocortin (MC) 1 receptor were cloned into expression vectors, expressed in mam-malian cells and pharmacologicallycharacterized. Four of the clones e +R ,e +B&D ,e wh /e y ,E Rfayoumi gave receptors to which melanocortin stimulating hormone (a-MSH) and NDP-MSH bound with similar IC50values and responded toa-MSHbyincreasing intracellular cAMP levels in a dose-dependent manner.

9p tumor12 20-04-2013 33 3   Download

We report the cloning, expression, pharmacological char-acterization and tissue distribution of a melanocortin (MC) receptor gene in a shark, the spiny dogfish (Squalus acanth-ias) (Sac). Phylogenetic analysis showed that this receptor is anorthologof theMC4 subtype, sharing71%overall amino acid identity with the human (Hsa) MC4 receptor. When expressedandcharacterizedbyradioligandbindingassay for the natural MSH (melanocyte-stimulating hormone) pep-tides a-, b-, and c-MSH, the SacMC4 receptor showed pharmacological properties very similar to the HsaMC4 receptor. ...

9p tumor12 20-04-2013 52 3   Download