Cyclic lactam hybrid alpha-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.

Mayorov AV; Cai M; Palmer ES; Tanaka DK; Cain JP; Dedek MM; Tan B; Trivedi D; Hruby VJ

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Cyclic lactam hybrid alpha-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.

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Cyclic lactam hybrid alpha-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.

机译：在人类黑皮质素受体上具有纳摩尔范围结合亲和力的环状内酰胺杂合的α-MSH/ Agouti相关蛋白（AGRP）类似物。

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A novel hybrid melanocortin pharmacophore was designed based on the topographical similarities between the pharmacophores of Agouti related protein (AGRP) an endogenous melanocortin antagonist, and alpha-melanocyte-stimulating hormone (alpha-MSH), an endogenous melanocortin agonist. When employed in two different 23-membered macrocyclic lactam peptide templates, the designed hybrid AGRP/MSH pharmacophore yielded non-competitive ligands with nanomolar range binding affinities. The topography-based pharmacophore hybridization strategy will prove useful in development of unique non-competitive melanocortin receptor modulators.

机译：基于Agouti相关蛋白（AGRP）（一种内源性黑皮质素拮抗剂）和α-黑素细胞刺激激素（α-MSH）（一种内源性黑皮质素激动剂）之间的拓扑相似性，设计了一种新型的杂交黑皮质素药效基团。当在两个不同的23元大环内酰胺肽模板中使用时，设计的杂交AGRP / MSH药效基团产生具有纳摩尔范围结合亲和力的非竞争性配体。基于地形的药效团杂交策略将被证明可用于开发独特的非竞争性黑皮质素受体调节剂。

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《Bioorganic and Medicinal Chemistry Letters》 |2011年第10期|共4页
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Mayorov AV; Cai M; Palmer ES; Tanaka DK; Cain JP; Dedek MM; Tan B; Trivedi D; Hruby VJ;
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1. Cyclic lactam hybrid alpha-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors. [J] . Mayorov AV, Cai M, Palmer ES, Bioorganic and Medicinal Chemistry Letters . 2011,第10期

机译：在人类黑皮质素受体上具有纳摩尔范围结合亲和力的环状内酰胺杂合的α-MSH/ Agouti相关蛋白（AGRP）类似物。
2. Solid-phase peptide head-to-side chain cyclodimerization: discovery of C(2)-symmetric cyclic lactam hybrid alpha-melanocyte-stimulating hormone (MSH)/agouti-signaling protein (ASIP) analogues with potent activities at the human melanocortin receptors. [J] . Mayorov AV, Cai M, Palmer ES, Peptides: An International Journal . 2010,第10期

机译：固相肽头到侧链环二聚化：发现C（2）对称环状内酰胺杂合的α-黑素细胞刺激激素（MSH）/ agouti信号蛋白（ASIP）类似物对人类黑皮质素受体具有有效活性。
3. Solid-phase peptide head-to-side chain cyclodimerization: discovery of C(2)-symmetric cyclic lactam hybrid alpha-melanocyte-stimulating hormone (MSH)/agouti-signaling protein (ASIP) analogues with potent activities at the human melanocortin receptors. [J] . Mayorov AV, Cai M, Palmer ES, Peptides: An International Journal . 2010,第10期

机译：固相肽头到侧链环二聚化：发现C（2）对称环状内酰胺杂合的α-黑素细胞刺激激素（MSH）/ agouti信号蛋白（ASIP）类似物对人类黑皮质素受体具有有效活性。
4. The naturally occurring melanocortin antagonist agouti-related protein (AGRP) possesses similar and distinct interactions at the MC4 receptor compared with melanocortin agonist [C] . Carrie Haskell-Luevano, Eileen K.Monck, Y.P.Wan the International Peptide Symposium . 2001

机译：与Melanocortin激动剂相比，天然存在的黑色激素拮抗剂agouti相关蛋白（AgrP）具有与MC4受体相似明显的相互作用
5. Fungi-derived natural products with binding affinities for human opioid or cannabinoid receptors. [D] . Gao, Jiangtao. 2010

机译：对人阿片或大麻素受体具有结合亲和力的真菌衍生天然产物。
6. Cyclic Lactam Hybrid α-MSH/Agouti-Related Protein (AGRP) Analogues with Nanomolar Range Binding Affinities at the Human Melanocortin Receptors [O] . Alexander V. Mayorov, Minying Cai, Erin S. Palmer, -1

机译：循环内酰胺杂交α-MSH / agouti相关蛋白（AGRP）类似物在人黑色主酶受体中具有纳米摩尔系列结合亲和力的类似物
7. Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors [O] . Alexander V. Mayorov, Minying Cai, Erin S. Palmer, 2011

机译：循环内酰胺杂交α-MSH / agouti相关蛋白（AGRP）类似物在人黑色主酶受体中具有纳米摩尔系列结合亲和力的类似物
8. Vitamin D3 Analogues with Low Vitamin D Receptor Binding Affinity RegulateChondrocyte Proliferation, Proteoglycan Synthesis, and Protein Kinase C Activity [R] . Greising, D. M. 1997

机译：具有低维生素D受体结合亲和力的维生素D3类似物调节软骨细胞增殖，蛋白多糖合成和蛋白激酶C活性

Cyclic lactam hybrid alpha-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.

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