PB1(PB1) - 药物靶点：EGFR_在研适应症：肿瘤_专利_临床

概要

基本信息

药物类型

前抗体

别名-

靶点

EGFR

作用方式

拮抗剂

作用机制

EGFR拮抗剂(表皮生长因子受体erbB1拮抗剂)

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症-

原研机构-

在研机构

CytomX Therapeutics, Inc.

非在研机构-

权益机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 PB1 相关的临床结果

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100 项与 PB1 相关的转化医学

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100 项与 PB1 相关的专利（医药）

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44

项与 PB1 相关的文献（医药）

2025-10-28·ACS Omega

Fast-Track Crystallization of PB-1 with Sorbitol-Based Nucleating Agent

Article

作者: Gajzlerova, Lenka ; Navratilova, Jana ; Polaskova, Martina ; Cermak, Roman

The work is focused on crystallization and phase transition of polybut-1-ene (PB-1) homopolymer and random copolymer in the presence of commonly used nucleating agent (NA) 1,3:2,4-bis-(3,4-dimethylbenzylidene) sorbitol, primarily designed for polypropylene. The crystallization and subsequent phase transition from kinetically preferred tetragonal form II into thermodynamically stable trigonal form I in defined times of aging at room temperature is studied. It was found that NA accelerates phase transition, particularly in homopolymer. In the copolymer, moreover, the addition of NA dramatically increases the crystallization temperature and narrows the crystallization peak as well as the melting peak, which corresponds to the formation of a more uniform structure. At the same time, the addition of NA increases the haze significantly, confirming the formation of a two-form structure. However, NA was found to be soluble in a low concentration (0.2 wt %) in PB-1 melt at a sufficiently high temperature of melting. The solubility then affects the crystallization behavior. Finally, it can be confirmed that the addition of commercial sorbitol-based NA has a significant effect on the crystallization and phase transition of both the PB-1 homopolymer and the copolymer.

2024-06-01·Phytomedicine : international journal of phytotherapy and phytopharmacology

N-Cinnamoylpyrrole-derived alkaloids from the genus Piper as promising agents for ischemic stroke by targeting eEF1A1

Article

作者: Hou, Yue ; Lan, Qian ; Wang, Yaqi ; Su, Baojun ; Zhu, Shanshan ; Huang, Gaowu ; Liang, Dong

BACKGROUND:

Ischemic stroke (IS) is a serious cerebrovascular disease characterized by significantly elevated mortality and disability rates, and the treatments available for this disease are limited. Neuroinflammation and oxidative stress are deemed the major causes of cerebral ischemic injury. N-Cinnamoylpyrrole alkaloids form a small group of natural products from the genus Piper and have not been extensively analyzed pharmacologically. Thus, identifying the effect and mechanism of N-cinnamoylpyrrole-derived alkaloids on IS is worthwhile.

PURPOSE:

The present research aimed to explore the antineuroinflammatory and antioxidative stress effects of N-cinnamoylpyrrole-derived alkaloids isolated from the genus Piper and to explain the effects and mechanism on IS.

METHODS:

N-cinnamoylpyrrole-derived alkaloids were isolated from Piper boehmeriaefolium var. tonkinense and Piper sarmentosum and identified by various chromatographic methods. Lipopolysaccharide (LPS)-induced BV-2 microglia and a mouse model intracerebroventricularly injected with LPS were used to evaluate the antineuroinflammatory and antioxidative stress effects. Oxygen‒glucose deprivation/reperfusion (OGD/R) and transient middle cerebral artery occlusion (tMCAO) models were used to evaluate the effect of PB-1 on IS. To elucidate the fundamental mechanism, the functional target of PB-1 was identified by affinity-based protein profiling (ABPP) strategy and verified by cellular thermal shift assay (CETSA), drug affinity responsive target stability (DARTS), and circular dichroism (CD) analyses. The effect of PB-1 on the NF-κB and NRF2 signaling pathways was subsequently evaluated via western blotting and immunofluorescence staining.

RESULTS:

The results showed that N-cinnamoylpyrrole-derived alkaloids significantly affected neuroinflammation and oxidative stress. The representative compound, PB-1 not only inhibited neuroinflammation and oxidative stress induced by LPS or OGD/R insult, but also alleviated cerebral ischemic injury induced by tMCAO. Further molecular mechanism research found that PB-1 promoted antineuroinflammatory and antioxidative stress activities via the NF-κB and NRF2 signaling pathways by targeting eEF1A1.

CONCLUSION:

Our research initially unveiled that the therapeutic impact of PB-1 on cerebral ischemic injury might rely on its ability to target eEF1A1, leading to antineuroinflammatory and antioxidative stress effects. The novel discovery highlights eEF1A1 as a potential target for IS treatment and shows that PB-1, as a lead compound that targets eEF1A1, may be a promising therapeutic agent for IS.

2024-04-01·The Journal of prosthetic dentistry

Fit and retention of complete denture bases: Part I – Conventional versus CAD-CAM methods: A clinical controlled crossover study

Article

作者: Müller, Frauke ; Chebib, Najla ; Srinivasan, Murali ; El Osta, Nada ; Imamura, Yoshiki ; Maniewicz, Sabrina

STATEMENT OF PROBLEM:

Clinical evidence is sparse on whether dentures fabricated by computer-aided design and computer-aided manufacturing (CAD-CAM) methods afford superior fit and retention when compared with those fabricated conventionally.

PURPOSE:

The purpose of this clinical controlled crossover study was to evaluate the peak retention force and fit of CAD-CAM manufactured (3D printed and milled) maxillary complete denture bases and conventional heat-polymerized bases (control).

MATERIAL AND METHODS:

Twenty participants with edentulous maxillary arches were recruited. Impressions were made with a border-molded custom tray, and the resulting definitive cast was scanned. The conventional base was manufactured on the definitive cast with a hook and a 45-degree platform with a central notch and 2 lateral notches. The scan of the definitive cast was used for the fabrication of a milled and a printed base. The platform and hook position on the conventional base were transferred digitally to the milled and printed bases. All bases were scanned. A traction dynamometer was orientated into the notches, and retention was evaluated in the post dam and tuberosity areas. Scans were imported into a comparison software program which matched scans to their corresponding reference and performed a 3-dimensional comparison. The Friedman and Wilcoxon tests were used to compare between groups (confidence interval: 95%, α=.05).

RESULTS:

Nineteen participants with a mean ±standard deviation age of 64.1 ±14.7 years completed all clinical sessions. No significant difference in peak retention was measured between milled (MB1), printed (PB1), and conventional (CB) bases in the post dam (CB: 12.44 ±9.62 N, PB1: 16.08 ±15.28 N, MB1: 14.52 ±17.07 N) and right tuberosity area (CB: 8.99 ±7.82 N, PB1: 11.28 ±9.57 N, MB1: 11.99 ±12.10 N). In the left tuberosity area, peak retention was lower for CB (10.03 ±8.39 N) than PB1 (14.98 ±14.72 N) and MB1 (13.55 ±15.53 N; P=.05). Compared with the definitive cast, the fit of the conventional base (0.18 ±0.01 mm) was closer than the printed (0.21 ±0.03 mm) and milled bases (0.21 ±0.02 mm) (P<.001).

CONCLUSIONS:

The CD bases manufactured by CAD-CAM techniques provided retention and fit similar to that of conventionally manufactured bases and can therefore be considered suitable techniques.

100 项与 PB1 相关的药物交易

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